New derivatives of cyclourea, production and pharmaceutical application as kinase inhibitors

FIELD: medicine; pharmacology.

SUBSTANCE: compounds of this invention possess properties of protein kinase inhibitors. In the general formula p means integer within 0 to 2; R and R1 mean O; A1 and A2 mean single bond, (C1-C6)alkyl; B2 means monocyclic or bicyclic, saturated or unsaturated heterocyclic radical including 1 to several identical or different heteroatoms, chosen among O, S, N and NR7, probably substituted with one or several identical or different substitutes.

EFFECT: inhibiting effect on protein kinase, effective application of compounds of formula for medical products.

49 cl, 1 tbl, 6 dwg, 334 ex

 

The present invention relates to new derivatives of cyclooctene, method of production thereof, their use as medicaments containing them, pharmaceutical compositions and pharmaceutical use of such derivatives for the prevention and treatment of diseases that can be modulated by inhibition of the activity of protein kinases.

The present invention relates to new derivatives of cyclooctene with any abscopal effects on protein kinases.

The products according to the present invention, therefore, can be used, in particular, for the prevention or treatment of diseases that can be modulated by inhibition of the activity of protein kinases.

Inhibition and regulation of protein kinases represent, in particular, a powerful new mechanism of action for the treatment of a large number of solid tumors.

Such diseases can be cured products according to the present invention, therefore, are, in particular solid tumors.

Such protein kinases include, in particular, to the following group: EGFR, Fak, FLK-1, FGFR1, FGFR2, FGFR3, FGFR4, FGFR5, flt-1, IGF-1R, KDR, PLK, DERIVED, tie2, VEGFR, AKT, Raf.

In particular, you should specify the protein kinase IGF1-R (receptor insulinogenic growth factor 1).

Please also indicate the protein kinase FAK.

You must also specify about Encinas AKT.

Thus, the present invention particularly relates to new inhibitors of the receptor IGF-1R, which can be used for treatment in Oncology.

The present invention also relates to new inhibitors of the receptor, FAK, which can be used for treatment in Oncology.

The present invention also relates to new inhibitors of receptor ACT, which can be used for treatment in Oncology.

Cancer remains a disease for which existing treatments are totally inadequate. Some protein kinases, including, in particular, IGF-1R (receptor insulinogenic growth factor 1), play an important role in the case of many cancers. Inhibition of such proteinkinase is potentially important in the chemotherapy of cancer, in particular, to inhibit the growth or survival of tumors. The present invention therefore relates to the identification of new products, which inhibit protein kinases such.

Protein kinase involved in the alarm events that control the activation, growth and differentiation of cells in response to either the extracellular mediators, or to changes in the environment. Typically, these kinases belong to two groups: those that phosphorylate preferably serine and/or Treo the new balances, and those that phosphorylate preferably, the tyrosine residues [S.K. Hanks and T. Hunter, FASEB. J.,9, 576-596 (1995)]. Serine/trionychinae represent, for example, isoforms of protein kinases [A.C. Newton, J. Biol. Chem., 270, 28495-28498 (1995)] and a group of kinase-dependent tsiklonov as cdc2 [J. Pines, Trends in Biochemical Sciences,18, 195-197 (1995)]. Tyrosine kinase include the receptors of growth factors, as the receptor for epidermal growth factor (EGF) [S. Iwashita and M. Kobayashi, Cellular Signalling,4, 123-132 (1992)], and cytosolic kinases, as p56tck, p59fYn, ZAP-70 kinase csk [C. Chan and others, Ann. Rev. Immunol.,12, 555-592 (1994)].

Abnormally high levels of activity of protein kinase involved in numerous zabolevaniya arising from abnormal cell functions. This can happen either directly, or indirectly, by dysfunctionraven in the control mechanisms of kinase activity associated with, for example, mutation, overproduction or inappropriate activity of the enzyme, or by overproduction or insufficient production of cytokines or growth factors, are also actively involved in the transduction of signals above or below kinases. In all these cases, selective inhibition of kinase activity can be expected favorable effect.

Receptor type 1 insulinogenic growth factor (IGF-I-R) is a transmembrane receptor with tyrosine aznoe activity which is associated, first, with differs, as well as with IGFII and insulin with lower affinity. The binding of IGF1 to its receptor leads to receptor oligomerization, activation of tyrosine kinase, intermolecular autophosphorylation and phosphorylation of cellular substrates (main substrates: IRS1 and Shc). Activated by their ligand receptor induces mitogenic activity in normal cells. However, IGF-I-R plays an important role in the so-called abnormal growth.

Several clinical messages emphasize the importance of the path of IGF-I in the development of cancer people:

IGF-I-R often find overproduction in numerous tumor types (breast, colon, lung, sarcoma...), and its presence is often associated with a more aggressive phenotype.

High concentrations of circulating IGF1 highly correlated with risk of cancer of the prostate, lung and breast cancer.

Moreover, documentary evidence is widely confirmed that IGF-I-R is required to establish and preserve transformed in vitro, as in vivo phenotype [R. Baserga, Exp. Cell. Res.,253, 1-6 (1999)]. Kinase activity of IGF-I-R is required for activity of transformation of some oncogenes: EGFR, DERIVED, large T antigen of SV40 virus, activated Ras, Raf, and v-Src. The expression of IGF-I-R in the norm is lnyh fibroblasts induces neoplastic phenotype, which can then cause the formation of tumors in vivo. The expression of IGF-I-R plays an important role in the case of independent growth substrate. IGF-I-R also manifests itself as the protector of apoptosis induced by chemotherapy, radiation, and apoptosis induced by cytokines. Moreover, inhibition of endogenous IGF-I-R due to the negative dominant, triple helix formation or antisense expression provokes suppression transformants activity in vitro and reduced tumor growth in employees as animal models.

Of kinases, in which case the modulation of activity is desired, FAK (focal adhesion kinase) is also a preferred kinase.

FAK is a cytoplasmic tyrosinekinase, plays an important role in transduction of the transmission signal by integrins, a family of heterodimeric cell adhesion receptors. FAK and integrins malokalinovka in perimembrane structures, called "plaques" adhesion. In the case of multiple cell types is shown that the activation of FAK, as well as its phosphorylation by tyrosinase residues and, in particular, its autophosphorylation at tyrosine 397, are dependent on the binding of integrins to their extracellular ligands and, consequently, induced during cell adhesion [L. Kornberg and others, J. Biol. Chem.,267(33), 23439-23442 (1992)]. And topstoriesoivoee at tyrosine 397 FAK is a binding site for another tyrosine kinase, Src, through its SH2 domain [Schaller and others, Mol. Cell. Biol.,14, 1680-1688 (1994); Xing and others, Mol. Cell. Biol.,5, 413-421 (1994)]. Src can then be fosforilirovanii FAK at tyrosine 925, recrutare thus, adaptive protein Grb2 and inducyruya in some cell activation pathways ras and the map kinase, involved in the control of cell proliferation [Schlaepfer and others, Nature,372, 786-791 (1994); Schlaepfer and others, Prog. Biophy. Mol. Biol.,71, 435-478 (1999); Schaepfer and Hunter, J. Biol. Chem.,272, 13189-13195 (1997)].

Activation of FAK can also induce a path alarm jun NH2-terminal kinase (JNK) and promote cells to the G1 phase of the cell cycle [Oktay and others, J.Cell. Biol.,145, 1461-1469 (1999)]. Phosphatidylinositol-3-OH-kinase (PI3-kinase) is also associated with FAK at tyrosine 397, and this interaction may be required for the activation of PI3-kinase [Chen and Guan, Proc. Nat. Acad. Sci. USA91, 10148-10152 (1994); Ling and others, J. Cell. Biochem.,73, 533-544 (1999)]. Complex FAK/Src phosphorylates various substrates, as paxillin and 130S, in fibroblasts [Vuori and others, Mol. Cell. Biol.,16, 2606-2613 (1996)].

The results of numerous studies confirm the hypothesis that inhibitors of FAK may be suitable in the treatment of cancer. Studies suggest that FAK may play an important role in proliferation and/or survival of cells in vitro. In the case of cells of the Chinese hamster ovary (Cho), for example, some authors have shown that overproduction the e 125FAK leads to acceleration of the transition of G1 to S, allowing you to assume that 125FAK favors cell proliferation [J.-H. Zhao and others, J. Cell. Biol.,143, 1997-2008 (1998)]. Other authors have shown that tumor cells treated antimyeloma oligonucleotide-FAK, lose their adhesion, and apoptosis (Xu and others, Cell Growth Differ.,4, 413-418 (1996)]. It was also shown that FAK promotes cell migration in vitro. So, fibroblasts deficient for the expression of FAK ("scarce" FAK mouse)have a rounded morphology, lack of cell migration in response to chemotactically signals, and these drawbacks are eliminated by re-expression of FAK [D.J. Sieg and others, J. Cell. Science,112, 2677-2691 (1999)]. Overproduction C-terminal domain of FAK (FRNK) blocks the extrusion of adhesive cells and reduces cell migration in vitro [A. Richardson and J.T. Parsons, Nature,380, 538-540 (1996)]. Overproduction FAK in cells of Cho, COS or cells of human astrocytomas favors cell migration. The involvement of FAK in promotion of cell proliferation and cell migration in many cell types in vitro suggests the potential role of FAK in neoplastic processes. A recent study actually showed an increase in proliferation of tumor cells in vivo after induction of the expression of FAK in cells of the human astrocytomas [L.A. Cary and others, J. Cell. Sci.,109, 1787-1794 (1996); D. Wang and others, J. Cell. Sci.,113, 221-4230 (2000)]. Moreover, immunohistochemical studies of human biopsies showed that FAK overproduced in malignant tumors of the prostate, breast, thyroid, colon, melanoma, brain and lung, and the degree of FAK expression directly correlates with tumors with more aggressive phenotype [M. Weiner and others, Lancet,342(8878), 1024-1025 (1993); Owens and others, Cancer Research.,55, 2752-2755 (1995); K. Maung and others, Oncogene,18, 6824-6828 (1999); D. Wang and others, J. Cell. Sci.,113, 4221-4230 (2000)].

The protein kinase AKT (also known as the RKV) and phosphoinositide-3-kinase (PI3K) are actively involved in the transmission of cellular signal that transmits the signals originating from growth factors that activate membrane receptors.

This way transduction is actively involved in multiple cellular functions: regulation of apoptosis, control of transcription and translation, glucose metabolism, angiogenesis and mitochondrial integrity. Identified from the outset as an important active participant in insulin-dependent signaling pathways regulating metabolic responses, serine/trionychinae ACT was then identified as the mediator that plays a key role in survival induced by growth factors. It is shown that the ACT can inhibit death due to apoptosis induced by diverse and incentives, in the case of a number of cell types and tumor cells. In accordance with these observations it is shown that the ACT, by phosphorylation data serine residues, can inactivate BAD, GSK3β, caspase-9, the transcription factor Forkhead and activate Kalifa and e-NOS. It is of interest to note that protein is BAD again find hyperphosphorylation 11 human tumor cell lines of the 41 investigated. In addition, it is shown that hypoxia modulates the induction of VEGF transformed with Ha-ras cells, activating path PI3K/AKT and implicita sequence of fixation of the transcription factor HIF-1 (hypoxia-induced factor-1), referred to in abbreviated form from HRE "hypoxy-responsive-element" ("responsible for hypoxia element).

The ACT plays a very important role in cancerous pathologies. About amplification and/or overproduction ACT was notified in the case of many human tumors, such as carcinoma of the stomach (amplification ACT1), ovarian cancer, breast cancer or pancreatic cancer (amplification and overproduction ACT2) and breast carcinoma due to deficiency of estrogen-receptors, as well as carcinoma prostate cancer, independent of androgens (overproduction ACT). Moreover, the ACT constitutively activated in all tumors PTEN (-/-), and the phosphatase PTEN is subjected fact the AI or inactivation by mutations in many types of tumors, as carcinoma of the ovary, prostate, endometrium, glioblastoma and melanoma. The ACT also actively involved in the oncogenic activation of bcr-abl (reference: A. Khawaja, Nature,401, 33-34 (1999); Cardone and others, Neture,282, 1318-1321 (1998); S. Kitada, etc., Am. J. Pathol.,152(1), 51-61 (1998, January); N.M. Mazure, etc., Blood,90, 3322-3331 (1997); H. Zhong and others, Cancer Res.,60, 1541-1545 (2000)].

The object of the present invention, therefore, are the products of General formula (I):

in which

p means an integer from 0 to 2;

R and R1 are identical or different, denote O or NH;

R2 and R3, identical or different, denote a hydrogen atom, alkyl, alkenyl, quinil, cycloalkyl, aryl and heteroaryl, possibly substituted, or R2 and R3 together with the carbon atom to which they are attached, form a carbocyclic or heterocyclic radical, these radicals are 3-10-membered heterocyclic moiety includes one or more heteroatoms chosen among O, S, N and NR7, all these radicals possibly substituted;

A1 means a simple link, alkyl, alkenyl or quinil;

Y and Y1 are the same or different, are such that one of Y and Y1 is chosen among OCF3, -O-CF2-CHF2, -O-CHF2, -O-CH2CF3, -SO2NR5R6, SF5and-S(O)n-alkyl and the other of Y and Y1 is chosen among the same values and, in addition, among the following values: the om of hydrogen, halogen atom, hydroxyl, alkoxyl, nitrogroup, CN, NR5R6, possibly substituted alkyl, possibly substituted aryl and heteroaryl, CF3About alkenyl, quinil, O-cycloalkyl, S(O)nalkenyl, S(O)n-quinil, S(O)n-cycloalkyl; free, converted into a salt or esterified carboxyl and CONR5R6;

or phenyl radical with their substituents Y and Y1 form the following radicals:

where p means an integer 2, 3 or 4, and the thus obtained organic radical can be substituted by one or more alkyl radicals, which are possibly substituted;

R5 and R6, identical or different, chosen among hydrogen atom, alkyl, alkenyl, quinil, cycloalkyl, cycloalkenyl, geterotsiklicheskie, aryl and heteroaryl, possibly substituted, or R5 and R6 together with the nitrogen atom to which they are attached, form a 3-10-membered heterocyclic radical comprising one or more heteroatoms chosen among O, S, N and NR7, possibly substituted;

A2, identical to or different from A1, has values A1 and and SO2;

B2 means a monocyclic or bicyclic, saturated or unsaturated heterocyclic radical comprising from 1 to several identical or different heteroatoms chosen among O, S, N and NR7, possibly substituted by one or more, same or resumetemplates, choose among the values of Y2;

R7 means a hydrogen atom, alkyl, cycloalkyl, phenyl, acyl, S(O)2-Alk, S(O)2-aryl, S(O)2-heteroaryl and S(O)2-NR5R6;

Y2 denotes a hydrogen atom, halogen atom, hydroxyl, cyano, alkyl, alkoxyl, cycloalkyl, heteroseksualci, aryl, heteroaryl, alkenyl, -O-quinil, -O-cycloalkyl, -S(O)n-alkyl, -S(O)nalkenyl, -S(O)n-quinil, -S(O)n-cycloalkyl, COOR13, -OCOR13, NR5R6, CONR5R6, -S(O)n-NR5R6, -NR10-CO-R13, -NR10-SO2-R13, NH-SO2-NR5R6, -NR10-CO-NR5R6, -NR10-CS-NR5R6, -NR10-COOR13, all of these radicals may be substituted;

and

all the above alkyl, alkeline, alkyline, CNS radicals are linear or branched and containing at most 6 carbon atoms;

all of the above cycloalkyl, heterocytolysine radicals contain at most 7 carbon atoms;

all of the foregoing aryl and heteroaryl radicals containing at most 10 carbon atoms;

all the above alkyl, alkeline, alkyline, CNS, cycloalkyl, heterocytolysine, aryl and heteroaryl, carbocyclic and heterocyclic radicals, and the loop formed by R5 and R6 with the atom to which they are bound, can be substituted by one or more identical or different radicals, selected among halogen atoms and is ionography, hydroxyl, alkoxyl, CF3, nitro, aryl, heteroaryl, -C(=O)-OR9, -C(=O)-R8, -NR11R12, -C(=O)-NR11R12, -N(R10)-C(=O)-R8, -N(R10)-C(=O)-OR9, -N(R10)-C(=O)-NR11R12, -N(R10)-S(Oh)n-R8, -S(O)n-R8, -N(R10)-S(Oh)n-NR11R12 or-S(O)n-NR11R12;

all of the foregoing aryl and heteroaryl radicals even possibly substituted by one or more radicals selected from alkyl, CNS radicals and alkylenedioxy;

all abovementioned cyclic radicals, and the loop formed by R5 and R6 with the atom to which they relate, even possibly substituted by one or more radicals selected from oxo and tocography;

n means an integer from 0 to 2;

R8 denotes an alkyl, alkenyl, cycloalkyl, cycloalkenyl, heteroseksualci, geterotsiklicheskikh, aryl, arylalkyl, heteroaryl and heteroaromatic;

R9 has the values of R8 and hydrogen;

R10 denotes a hydrogen atom or alkyl;

R11 and R12, identical or different, denote a hydrogen atom, (C3-C6-cycloalkyl, (C1-C4)-alkyl or phenyl, possibly substituted by one or more identical or different radicals, selected among halogen atoms and ceanography, hydroxyl, alkoxyl, CF3, nitro, phenyl and free, turned into salt, esterified or liderando of carboxyl;

or R11 and R12 together with the nitrogen atom to which they relate, clicks the form a 5-7-membered cyclic radical, including one or more heteroatoms chosen among O, S, N and NR7, and preferably a cyclic amine; and

R13, identical or different from R5 or R6, is chosen among the values of R5 or R6;

bearing in mind that the products of formula (I) are as shown below in PP (a) - (d):

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3or S-alk; A2 means a simple bond or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3That SO-Alk , S(O)2-alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-alk, always replaced by hydroxamate-CO-NHOH;

(C) where p denotes the integer 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means S(O)n -Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

d) when R denotes an integer from 0 to 2, R and R1 denote oxygen atoms, A1 means a simple bond; Y and Y1 are the same or different, are such that one means S(O)2-Alk or SO2NH2and the other means NR5R6; A2 means a simple link or alkylene and B2 means maybe substituted 5-10-membered heterocyclic radical, then R2 and R3 are both not mean hydrogen atoms;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the present invention are the products of General formula (I), such as those mentioned above, in which

p means an integer from 0 to 2;

R and R1 are identical or different, denote O or NH;

R2 and R3, identical or different, denote a hydrogen atom, alkyl, alkenyl, quinil, cycloalkyl, aryl and heteroaryl, possibly substituted, or R2 and R3 together with the carbon atom to which they are attached, form a carbocyclic or heterocy the " radical, moreover, these radicals are 3-10-membered heterocyclic moiety includes one or more heteroatoms chosen among O, S, N and NR7, all these radicals possibly substituted;

A1 means a simple link, alkyl, allyl or PROPYNYL;

Y and Y1 are the same or different, are such that one of Y and Y1 is chosen among OCF3, S(O)nCF3, S(O)n-Alk, SO2CHF2, SO2CF2CF3and-SO2NR5R6, and the other of Y and Y1 is chosen among the same values and, in addition, among the following values: hydrogen atom, halogen atom, hydroxyl, alkoxy, NR5R6, possibly substituted alkyl, possibly substituted aryl and heteroaryl, CF3, O-allyl, PROPYNYL,-cycloalkyl, S(O)n-allyl, S(O)n-PROPYNYL, S(O)n-cycloalkyl; free, converted into a salt or esterified carboxyl and CONR5R6; and

R5 and R6, identical or different, chosen among hydrogen atom, alkyl, alkenyl, cycloalkyl, cycloalkenyl, geterotsiklicheskie, aryl and heteroaryl, possibly substituted, or R5 and R6 together with the nitrogen atom to which they are attached, form a 3-10-membered heterocyclic radical comprising one or more heteroatoms chosen among O, S, N and NR7, possibly substituted;

A2, identical to or different from A1, has values A1 and and SO2;

B2 means a saturated or unsaturated geterotsiklicheskikh is radical, comprising from 1 to several identical or different heteroatoms chosen among O, S, N and NR7, possibly substituted by one or more, same or different substituents selected from Y2;

R7 means a hydrogen atom, alkyl, cycloalkyl, phenyl, acyl, S(O)2-Alk, S(O)2-aryl, S(O)2-heteroaryl and S(O)2-NR5R6;

Y2 denotes a hydrogen atom, halogen atom, hydroxyl, alkyl, alkoxyl, cycloalkyl, heteroseksualci, aryl, heteroaryl, -O-allyl, -O-PROPYNYL, -O-cycloalkyl, -S(O)n-alkyl, -S(O)n-allyl, -S(O)n-PROPYNYL, -S(O)n-cycloalkyl, COOR9, -OCOR8, NR5R6, CONR5R6, -S(O)n-R5R6, NHCOR8, NH-S(O)n-R8 or NH-S(O)nCF3or NH-SO2-NR5R6, all these radicals may be substituted;

and

all the above alkyl, alkeline, alkyline, CNS radicals are linear or branched and containing at most 6 carbon atoms;

all of the above cycloalkyl, heterocytolysine radicals contain at most 7 carbon atoms,

all of the foregoing aryl and heteroaryl radicals containing at most 10 carbon atoms;

all the above alkyl, alkeline, alkyline, CNS, cycloalkyl, heterocytolysine, aryl and heteroaryl, carbocyclic and heterocyclic radicals can be substituted one who does several the same or different radicals, selected among halogen atoms and ceanography, hydroxyl, alkoxyl, CF3, nitro, aryl, heteroaryl, -C(=O)-OR9, -C(=O)-R8, -NR11R12, -C(=O)-NR11R12, -N(R10)-C(=O)-R8, -N(R10)-C(=O)-OR9, -N(R10)-C(=O)-NR11R12, -N(R10)-S(Oh)n-R8, -S(O)n-R8, -N(R10)-S(Oh)n-NR11R12 or-S(O)n-NR11R12;

all of the foregoing aryl and heteroaryl radicals even possibly substituted by one or more radicals selected from alkyl radicals and alkylenedioxy;

n means an integer from 0 to 2;

R8 denotes an alkyl, alkenyl, cycloalkyl, cycloalkenyl, heteroseksualci, geterotsiklicheskikh, aryl, arylalkyl, heteroaryl and heteroaromatic;

R9 has the values of R8 and hydrogen;

R10 denotes a hydrogen atom or alkyl;

R11 and R12, identical or different, denote a hydrogen atom, (C3-C6-cycloalkyl, (C1-C4)-alkyl and phenyl, possibly substituted by one or more identical or different radicals, selected among halogen atoms and ceanography, hydroxyl, alkoxyl, CF3, nitro, phenyl and free, turned into salt, esterified or liderando of carboxyl;

or R11 and R12 together with the nitrogen atom to which they are bound, form a 5-7-membered cyclic radical containing one or more heteroatoms chosen among O, S, N and NR7, and preferably qi is symbolic amine;

bearing in mind that the products of formula (I) are as listed in points a) - d):

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3or S-alk; A2 means a simple bond or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3That SO-Alk , S(O)2-alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-alk, always replaced by hydroxamate-CO-NHOH;

(C) where p denotes the integer 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means S(O)n-Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, and the silt and heteroaryl;

d) when R denotes an integer from 0 to 2, R and R1 denote oxygen atoms, A1 means a simple bond; Y and Y1 are the same or different, are such that one means S(O)2-Alk or SO2NH2and the other means NR5R6; A2 means a simple link or alkylene and B2 means maybe substituted 5-10-membered heterocyclic radical, then R2 and R3 are both not mean hydrogen atoms;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the present invention are the products of General formula (I), as specified above, in which

p means an integer from 0 to 2;

R and R1 are identical or different, denote O or NH;

R2 and R3, identical or different, denote a hydrogen atom, alkyl, alkenyl, cycloalkyl, phenyl and heteroaryl, possibly substituted, or R2 and R3 together with the carbon atom to which they are attached, form a carbocyclic or heterocyclic radical, these radicals are 3-10-membered heterocyclic moiety includes one or more heteroatoms chosen among O, S, N and NR7, all these radicals possibly substituted;

A1 OSN which includes a simple link, alkyl, allyl or PROPYNYL;

Y and Y1 are the same or different, are such that one of Y and Y1 is chosen among OCF3, S(O)n-CF3, S(O)n-Alk, SO2CHF2, SO2CF2CF3and-SO2NR5R6, and the other of Y and Y1 is chosen among the same values and, in addition, among the following values: hydrogen atom, halogen atom, hydroxyl, alkoxy, NR5R6, alkyl, and possibly substituted phenyl, possibly substituted pyrazolyl and pyridyl;

and

R5 and R6, identical or different, chosen among hydrogen atom, alkyl, alkenyl, cycloalkyl, geterotsiklicheskie, phenyl and heteroaryl, possibly substituted, or R5 and R6 together with the nitrogen atom to which they are attached, form a 3-10-membered heterocyclic radical comprising one or more heteroatoms chosen among O, S, N and NR7, possibly substituted;

A2, identical to or different from A1, has values A1 and and SO2;

B2 means a saturated or unsaturated heterocyclic radical comprising from 1 to several identical or different heteroatoms chosen among O, S, N and NR7, possibly substituted by one or more, same or different substituents selected from Y2;

R7 means a hydrogen atom, alkyl, cycloalkyl or phenyl;

Y2 denotes a hydrogen atom, halogen atom, hydroxyl, alkyl, alkoxyl, cycloalkyl, heteroseksualci, phenyl, n is Eroare, O-cycloalkyl, -S(O)n-alk, -S(O)n-cycloalkyl, COOR9, OCOR8, NR5R6, CONR5R6, -S(O)n-R5R6, -NH-CO-R8 and NH-S(O)nR8, all these radicals may be substituted;

and

all the above alkyl, alkeline, alkyline, CNS radicals are linear or branched and containing at most 6 carbon atoms;

all of the above cycloalkyl, heterocytolysine radicals contain at most 7 carbon atoms,

all of the foregoing aryl and heteroaryl radicals containing at most 10 carbon atoms;

all the above alkyl, alkeline, alkyline, CNS, cycloalkyl, heterocytolysine, aryl and heteroaryl, carbocyclic and heterocyclic radicals can be substituted by one or more identical or different radicals, selected among halogen atoms and ceanography, hydroxyl, alkoxyl, CF3, nitro, phenyl, heteroaryl, -C(=O)-OR9, -C(=O)-R8, -NR11R12, -C(=O)-NR11R12, -N(R10)-C(=O)-R8, -N(R10)-C(=O)-OR9, -N(R10)-C(=O)-NR11R12, -N(R10)-S(Oh)n-R8, -S(O)n-R8, -N(R10)-S(Oh)n-NR11R12 or-S(O)n-NR11R12;

all of the foregoing aryl and heteroaryl radicals even possibly substituted by one or more radicals selected from alkyl radicals and alkylenedioxy;

n means an integer from 0 to 2;

R8 denotes an alkyl, cycloalkyl, cyclol illlil, heteroseksualci, geterotsiklicheskikh, phenyl and phenylalkyl;

R9 has the values of R8 and hydrogen;

R10 denotes a hydrogen atom or alkyl;

R11 and R12, identical or different, denote a hydrogen atom, (C1-C4)-alkyl and phenyl, possibly substituted by one or more identical or different radicals, selected among halogen atoms and hydroxyl, alkoxyl, CF3, nitro, phenyl and free, turned into salt, esterified or liderando of carboxyl;

or R11 and R12 together with the nitrogen atom to which they are bound, form a 5-7-membered cyclic radical containing one or more heteroatoms chosen among O, S, N and NR7, and preferably a cyclic amine;

bearing in mind that the products of formula (I) are as listed in points a) - d):

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3or S-alkyl; A2 means a simple link or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are the two who are such at least one means OCF3That SO-Alk , S(O)2-alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-alk, always replaced by hydroxamate-CO-NHOH;

(C) where p denotes the integer 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means S(O)n-Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

d) when R denotes an integer from 0 to 2, R and R1 denote oxygen atoms, A1 means a simple bond; Y and Y1 are the same or different, are such that one is SO2-Alk or SO2NH2and the other means NR5R6; A2 means a simple link or alkylene and B2 means maybe substituted 5-10-membered heterocyclic radical, then R2 and R3 are both not mean hydrogen atoms;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or reorganizes the mi and organic bases of the above product of formula (I).

The object of the present invention are also the products of formula (I), as specified above, in which Y and Y1 are the same or different, are such that one of Y and Y1 is chosen among OCF3, -O-CF2-CHF2, -O-CHF2, -O-CH2-CF3, S(O)nCF3, -S-CF2-CF2-CF3, -S(O)n-Alk, -S-Alk-O-Alk, -S-Alk-IT, S-Alk-CN, -S-Alk-geterotsiklicheskie, -SO2CHF2, -SO2CF2CF3, -SO2NR5R6 and-SF5where Alk denotes an alkyl radical with 1-4 carbon atoms and the other of Y and Y1 is chosen among the following values: hydrogen atom, halogen atom, the nitro-group, NR5R6, free or esterified carboxyl and CONR5R6;

or phenyl radical with their substituents Y and Y1 forms one of the following radicals:

and thus the resulting radical possibly substituted by one or more alkyl radicals, which are possibly substituted;

and the other substituents of the above product of formula (I) is chosen among the values specified in claim 1 of the claims, mean that

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means a hydrogen atom, and the other means OCF3or S-alk; A2 Osnach is no simple relationship or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom, and the other means OCF3, SOAlk , S(O)2-alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-alk, always replaced by hydroxamate-CO-NHOH;

(C) where p denotes the integer 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom and the other denotes S(O)n-Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the present invention is also what I the products of General formula (I), as mentioned above, in which one of Y and Y1 denotes the hydrogen atom and the other is chosen among OCF3, S(O)nCF3, S(O)nAlk, -SO2CHF2, -SO2CF2CF3and-SO2NR5R6;

and the other substituents of the above product of formula (I) is chosen among the values specified in claim 1 of the claims, keeping in mind that

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom, and the other means OCF3or S-alk; A2 means a simple bond or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom, and the other means OCF3, SOAlk , S(O)2-alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-alk, always replaced by hydroxamate-CO-NHOH;

(C) where p denotes the integer 0, R and R1 denote oxygen atoms, A1 is simply the ligature or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom and the other denotes S(O)n-Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the present invention are also the products of formula (I), such as the above, which one of Y and Y1 denotes a hydrogen atom, and the other choose among S(O)nCF3, -SO-Alk, S(O)2Alk, -SO2CHF2, -SO2CF2CF3and-SO2NR5R6;

and the other substituents of the above product of formula (I) is chosen among the values specified above, and provided that the products of formula (I) are as described above in points a)-b).

a) when R denotes an integer of 0, R and R1 denote oxygen atoms; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom, and the other means SOAlk, S(O)2Alk or SO2NH2; And means CH 2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-alk, always replaced by hydroxamate-CO-NHOH ;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom, and the other means SOAlk or S(O)2Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the present invention are the products of General formula (I), such as the above, which one of Y and Y1 denotes a hydrogen atom, and the other choose among S(O)nCF3, -SO2CHF2, -SO2CF2CF3and-SO2NR5R6;

and the other substituents of the above product of formula (I) is chosen among the values specified above, and mean, Thu the, when R denotes an integer of 0, R and R1 denote oxygen atoms; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom, and the other means SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-alk, always replaced by hydroxamate-CO-NHOH;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

In the products of formula (I) and in the following context, these terms have the following meanings:

- the term "Hal", "Halo" or " halogen means fluorine atoms, chlorine, bromine or iodine;

the term alkyl, alk, Alk or ALK means a linear or branched radical containing at most 12 carbon atoms, selected among the radicals: methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, sec-pentyl, tert-pentyl, neopentyl, hexyl, isohexyl, sec-hexyl, tert-hexyl and heptyl, octyl, nonyl, decyl, undecyl and dodecyl, as well as their linear or OSVETLENIE isomers position.

In particular it should be called alkyl radicals at most 6 carbon atoms, and in particular the radicals: methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, tert-butyl, linear or branched pentyl, linear or branched hexyl;

- the term "alkenyl" means a linear or branched radical containing at most 12 carbon atoms and preferably 4 carbon atoms, chosen, for example, among the following values: ethynyl or vinyl, propenyl or allyl, 1-propenyl, n-butenyl, Isobutanol, 3-methylbut-2-enyl, n-pentenyl, hexenyl, heptenyl, octenyl, cyclohexylmethanol and decenyl, as well as their linear or branched position isomers.

From the values of alkenyl in particular should be called allyl or butenyl;

- the term "quinil" means a linear or branched radical containing at most 12 carbon atoms and preferably 4 carbon atoms, chosen, for example, among the following values: ethinyl, PROPYNYL or propargyl, butynyl, n-butinyl, Isobutanol, 3-methylbut-2-inyl, pentenyl or hexenyl, as well as their linear or branched position isomers.

From the values of quinil in particular should be called propargyl;

- the term "alkoxy" means a linear or branched radical containing at most 12 carbon atoms and preferably 6 carbon atoms, chosen, is for example, among the groups: methoxy group, ethoxypropan, propoxylate, isopropoxy, linear, secondary or tertiary butoxypropan, phenoxypropan, hexachrome and epoxypropan, as well as their linear or branched position isomers;

- the term "alkoxycarbonyl" or "alkyl-O-CO-" means a linear or branched radical containing at most 12 carbon atoms in which the alkyl moiety has the above meaning: can be called, for example, the radicals methoxy - and etoxycarbonyl;

- the term "alkylenedioxy" or "-O-alkylene-O-" means a linear or branched radical containing at most 12 carbon atoms, in which alkalinity moiety has the above meaning: can be called, for example, methylenedioxy and Ethylenedioxy;

- the term "alkylsulfonyl" or "alkyl-SO-" means a linear or branched radical containing at most 12 carbon atoms in which the alkyl moiety has the above meaning, and includes preferably 4 carbon atoms;

the term "alkylsulfonyl" or "alkyl-SO2-" means a linear or branched radical containing at most 12 carbon atoms in which the alkyl moiety has the above meaning, and includes preferably 4 carbon atoms;

- the term "alkylsulfonyl" or "alkyl-SO2-NH-C(=O)-" oz ACHAT linear or branched radical, containing at most 12 carbon atoms in which the alkyl moiety has the above meaning, and includes preferably 4 carbon atoms;

- the term "allylthiourea" or "alkyl-S-" means a linear or branched radical containing at most 12 carbon atoms, and means, in particular, methylthiourea, ethylthiourea, isopropylthio and reptiliomorpha;

- the term "cycloalkyl" means a 3 to 10-membered monocyclic or bicyclic carbocyclic radical and means, in particular, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;

- the term "-O-cycloalkyl" means the radical, in which cycloalkyl has the above meaning;

- the term "cycloalkenyl" means a monocyclic or bicyclic non-aromatic carbocyclic radical containing at least one double bond and which is a 3-10-membered ring, and means, in particular, cyclobutenyl, cyclopentenyl or cyclohexenyl;

- the term "cycloalkenyl" means the radical, in which cycloalkyl and alkyl choose among the above values: the radical, thus means, for example, radicals of cyclopropylmethyl, cyclopentylmethyl, cyclohexylmethyl and cycloheptylmethyl;

the term "acyl" or "r- -" means a linear or branched radical containing at most 12 carbon atoms, in which the radical r denotes the volume of hydrogen, alkyl, cycloalkyl, cycloalkenyl, heteroseksualci or aryl, and these radicals have the abovementioned meanings and can be substituted as indicated: should be called, for example, radicals formyl, acetyl, propionyl, butyryl or benzoyl or even valeryl, hexanoyl, acryloyl, crotonoyl or carbarnoyl;

- the term "alloctype" understand radicals acyl-O-, in which acyl has the above value: should be called, for example, acetoxy or propionyloxy;

- the term "alluminare" understand radicals acyl-NH-, in which acyl has the above meaning;

the term "aryl" means an unsaturated, monocyclic or educated condensed cycles, carbocyclic radicals. As examples of such aryl radical can be called radicals phenyl or naphthyl.

More preferably include phenyl;

- the term "arylalkyl" means the radical obtained by combination of the above, possibly substituted, alkyl radicals and also above, possibly substituted, aryl radicals: should be called, for example, benzyl radicals, phenylethenyl, 2-phenethyl, triphenylmethyl or naphthalenyl;

the term "heterocyclic radical" denotes a saturated (heterologously) or unsaturated (heteroaryl) carbocyclic radical, at most 6-member of the first, interrupted by one or more, same or different, heteroatoms selected from among oxygen atoms, nitrogen or sulfur.

As geterotsiklicheskikh radicals can be mentioned, in particular, dioxolane, dioxane, aitiology, DIOXOLANYL, Cooksey radicals, oxiranyl, oxolane, DIOXOLANYL, piperazinil, piperidinyl, pyrrolidinyl, imidazolidinyl, pyrazolidine, morpholinyl or more tetrahydrofuryl, tetrahydrothieno, bromanil, dihydrobenzofuranyl, indolinyl, piperidinyl, permitopen, pyridalyl, tetrahydroquinoline, tetrahydroisoquinoline or diazolidinyl, all these radicals can be substituted.

From geterotsiklicheskikh radicals can be mentioned, in particular, possibly substituted piperazinil, possibly substituted piperidinyl, possibly substituted pyrrolidinyl, imidazolidinyl, pyrazolidine, morpholinyl or diazolidinyl: still more preferably can be called possibly substituted radicals morpholinyl, pyrrolidinyl and piperazinil;

- the term "geterotsiklicheskikh" refers to radicals in which heterologously and alkyl residues have the above meanings;

from 5-membered heteroaryl radicals can be called furyl, such as 2-furyl, thienyl, such as 2-thienyl and 3-thienyl, pyrrolyl, thiazolyl, thiazolyl, thiadiazolyl, tetrazolyl from thiazolyl, oxazolyl, oxadiazolyl, 3 - or 4-isoxazolyl, imidazolyl, pyrazolyl, isoxazolyl.

6-membered heteroaryl radicals include, in particular, pyridyl, such as 2-pyridyl, 3-pyridyl and 4-pyridyl, pyrimidyl, pyrimidinyl, pyridazinyl, pyrazinyl and tetrazolyl.

As a condensed heteroaryl radicals containing at least one heteroatom chosen among the atoms of sulphur, nitrogen and oxygen, can be called, for example, benzothiazyl, such as 3-benzothiazol, benzofuran, benzofuranyl, benzopyranyl, benzimidazolyl, benzoxazolyl, Tinetti, indolyl, purinol, chinoline, ethenolysis and naphthyridine.

From a condensed heteroaryl radicals are more preferably can be called radicals sensational, benzofuranyl, indolyl or chinoline, benzimidazolyl, benzothiazolyl, furyl, imidazolyl, indolizinyl, isoxazolyl, ethenolysis, isothiazolin, oxadiazolyl, pyrazinyl, pyridazinyl, pyrazolyl, pyridyl, pyrimidinyl, pyrrolyl, hintline, 1,3,4-thiadiazolyl, thiazolyl, thienyl and triazolyl group, and these radicals can be substituted as indicated for the heteroaryl radicals;

the term "cyclic amine" means a 3-8-membered cycloalkyl radical in which one carbon atom is replaced by a nitrogen atom, and cycloalkenyl moiety has the above meaning and may contain t is the train one or more other heteroatoms, chosen among O, S, SO2N or NR7, where R7 as defined above; as examples of such cyclic amines include, for example, radicals: pyrrolidinyl, piperidinyl, morpholinyl, piperazinil, indolinyl, perindopril or tetrahydroquinolines.

The term "patient" refers to people, but also other mammals.

The term "prodrug" means a product that can be converted in vivo due to metabolic mechanisms (such as hydrolysis) into the product of formula (I). For example, ester product of formula (I)containing a hydroxyl group may be converted by hydrolysis in vivo in its molecule basis. Or else, ester product of formula (I)containing a carboxy group may be converted by hydrolysis in vivo in its molecule-based.

As examples of esters of the products of formula (I)containing a hydroxyl group include such as acetates, citrates, lactates, tartratami, malonate, oxalates, salicylates, propionate, succinate, fumarate, maleate, methylene-bis-b-hydroxynaphthoate, gentisate, isethionate, di-p-toluoyltartaric, methansulfonate, econsultancy, bansilalpet, p-toluensulfonate, cyclohexylsulfamate and hinata.

Particularly suitable esters of the products of formula (I)which contain a hydroxyl group can be obtained from the acid of Titkov, such as those described by Bundgaard, etc., J. Med. Chem.,32, 2503-2507 (1989): these esters include, in particular, substituted (aminomethyl)benzoate; dialkylaminomethyl, in which the two alkyl groups can be linked together or can be interrupted by an oxygen atom or a possibly substituted by a nitrogen atom or alkilirovanny the nitrogen atom; or else (morpholinomethyl)benzoate, for example 3 - or 4-(morpholinomethyl)benzoate, and (4-alkylpiperazine-1-yl)benzoate, for example 3 - or 4-(4-alkylpiperazine-1-yl)benzoate.

Carboxyl radical or carboxyl radicals of the products of formula (I) can be converted into a salt or tarifitsirovana using various groups known to the specialist, which can be called as not limiting the scope of protection of the invention examples, the following connections:

from salt-forming compounds: inorganic bases, such as, for example, one equivalent of sodium, potassium, lithium, calcium, magnesium or ammonium or organic bases, such as, for example, methylamine, Propylamine, trimethylamine, diethylamine, triethylamine, N,N-dimethylethanolamine, Tris(hydroxymethyl)amino methane, ethanolamine, pyridine, picoline, dicyclohexylamine, morpholine, benzylamine, procaine, lysine, arginine, histidine, N-methylglucamine;

compounds for the esterification of: alkyl radicals for education alkoxycarbonyl the groups, such as, for example, methoxycarbonyl, etoxycarbonyl, tert-butoxycarbonyl or benzyloxycarbonyl, and these alkyl radicals can be substituted by radicals selected among, for example, halogen atoms, hydroxyl, alkoxyl, acyl, alloctype, allylthiourea, amino or aryl, such as, for example, in chlormethine, hydroxypropyl, methoxymethyl, propionylthiocholine, methylthiomethyl, dimethylaminoethyl, benzyl or fenetylline groups.

The term "esterified carboxy" see, for example, radicals such as allyloxycarbonyl, such as methoxycarbonyl, etoxycarbonyl, propoxycarbonyl, butyl - or tert-butyloxycarbonyl, cyclobutanecarbonyl, cyclopentanecarbonyl or cyclohexyloxycarbonyl.

You can also call the radicals formed with easily atmasamyama ester residues such as methoxymethyl, ethoxymethyl; aryloxyalkyl radicals, such as pivaloyloxymethyl, pivaloyloxymethyl, acetoxymethyl or acetoxyethyl; allyloxycarbonyl radicals, such as methoxycarbonylmethyl or ethoxycarbonylmethyl, isopropoxycarbonyloxymethyl or isopropoxycarbonyloxymethyl.

The list of such ester radicals can be found, for example, in European patent 0034536.

The term "aminirovanie Carbo is strength" refers to radicals of the type-CONR5R6, such as specified above; also see radicals NCOR6R7, in which the radicals R6 and R7, identical or different, denote a hydrogen atom or alkyl with 1-4 carbon atoms, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl or tert-butyl, and especially as the amino group, alkylamino and dialkylamino.

The term "alkylamino" understand methylamino, ethylamino, propylamino or butylamino, linear or branched. Preferred alkyl radicals at most 4 carbon atoms; alkyl radicals can be selected from among the above alkyl radicals.

The term "dialkylamino" see, for example, dimethylamino, diethylamino, methylaminopropyl. As indicated above, the preferred alkyl radicals at most 4 carbon atoms, chosen from the above list.

Radicals NR5RR6 or NR6R7 can also represent a heterocycle, which may contain or not one additional heteroatom. Can be called radicals pyrrolyl, imidazolyl, indolyl, piperidinyl, morpholinyl and piperazinil. Preferred radicals piperidinyl, morpholinyl or piperazinil.

The term "transformed into a salt carboxyl" understand salts formed, for example, with one equivalent of sodium, potassium, lithium, calcium, magnesium or ammonium. You can also call Saul is, formed with organic bases such as methylamine, Propylamine, trimethylamine, diethylamine, triethylamine. The preferred sodium salt.

When the products of formula (I) include turn into salt with acid to the amino group, it goes without saying that these acid salts are also part of the invention. You can call the salts formed, for example, with hydrochloric acid or methansulfonate.

Additive salts of inorganic or organic acids of the products of formula (I) can be, for example, salts formed with hydrochloric, Hydrobromic, iodomethane, nitric, sulfuric, phosphoric, propionic, acetic, triperoxonane, formic, benzoic, maleic, fumaric, succinic, tartaric, citric, oxalic, Glyoxylic, aspartic, ascorbic acid; alkylphenolethoxylate, such as, for example, methanesulfonate, econsultation, propanesulfonate; alkylsulfonate, such as, for example, methanesulfonate, α,β-ethicalfashion; rimonabantcanadapy, such as benzosulfimide and ridiculousthe.

It should be recalled that stereoisomer can be defined in its broadest sense as the isomerism of compounds having the same structural formula but different groups are arranged differently in space, such as, the particular in monosubstituted cyclohexane, Deputy which may be in the axial or Equatorial position, and the various possible rotational conformations of ethane derivatives. However, there is another type of stereoisomerism arising from different spatial locations of the fixed Vice, or double bonds, or cycles, which is often called geometric isomerism or CIS-TRANS isomerism. The term stereoisomer use in the present application in its broadest sense, it refers, therefore, to the totality of the above compounds.

The object of the invention, in particular, are products of the formula (I), such as the above, which one of Y and Y1 denotes a hydrogen atom, and the other choose among S(O)nCF3, SO2CHF2and SO2CF2CF3and the other substituents of the above product of formula (I) is chosen among the above values

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms,

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the invention, in particular, are products of the formula (I), such as you specified is e, in which all the above alkyl, alkeline, alkyline, cycloalkyl, heterocytolysine, aryl or heteroaryl radical possibly substituted by one or more identical or different radicals selected from among halogen atom, ceanography, hydroxyl, alkoxyl, CF3, nitro, phenyl; free, turned into salt, esterified with an alkyl radical or liderando using radical NR11aR12a of carboxyl; -C(=O)-R9a, -NR11aR12a, -C(O)-NR11aR12a, -N(R10a)C(=O)-R9a, -N(R10a)C(=O)-R8a, -N(R10a)C(=O)-NR11aR12a, -N(R10a)S(O)n-R9a, -S(O)n-R9a, -N(R10a)S(O)n-NR11aR12a or-S(O)n-NR11aR12a,

moreover, the above-mentioned aryl and heteroaryl radicals still possible replaced by ethylenedioxythiophene;

R8a means a hydrogen atom, alkyl, alkenyl, phenyl, phenylalkyl, heteroaryl or heteroaromatic;

R9a means alkyl, cycloalkyl, cycloalkenyl, heteroseksualci, geterotsiklicheskikh, phenyl, phenylalkyl, heteroaryl or heteroaromatic;

R10a means a hydrogen atom or alkyl;

R11a and R12a, identical or different, denote a hydrogen atom, alkyl, cycloalkyl, cycloalkenyl, phenyl, phenylalkyl, possibly substituted by one or more, same or different substituents selected among halogen atom, hydroxyl, (C1-C4)-alkyl or (C1-C4)-alkoxyl; or R11a and R12a together is a nitrogen atom, to which they are attached, form a cyclic radical chosen among pyrrolidinyl, piperidinyl, piperazinil, morpholinyl, indolinyl, perindopril, tetrahydroquinoline, diazolidinyl and naphthyridine;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the invention, in particular, are products of the formula (I), such as the above, in which p denotes an integer of 0, and the other substituents of the above product of formula (I), each, have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which p denotes an integer of 1, and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which p denotes an integer of 2, and the other substituents of the above product of formula (I) are shown according to the present invention.

The object of the invention, in particular, are products of the formula (I), this ka is shown above in which R1 is 0, and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above in which R is 0, and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as shown above in which R2 and R3, identical or different, denote a hydrogen atom, alkyl, alkenyl, cycloalkyl, cycloalkenyl, phenyl, phenylalkyl, heteroseksualci, geterotsiklicheskikh, heteroaryl and heteroallyl, possibly substituted, or R2 and R3 together with the carbon atom to which they are attached, form a carbocyclic or heterocyclic radical, these radicals are 3-10-membered heterocyclic radical containing one or more heteroatoms chosen among O, S, N and NR7b with all these radical possibly substituted;

all the above radicals possibly substituted by one or more radicals chosen among a halogen atom, ceanography, hydroxyl, alkyl and alkoxyl containing 1-4 carbon atoms, CF3, nitro, phenyl; free, turned into salt, esterified with an alkyl radical or liderando using radical is NR11bR12b of carboxyl; -C(=O)-R9b, -NR11bR12b and-C(=O)-NR11bR12b;

R7b means hydrogen atom, alkyl or phenyl;

R9 denotes a hydrogen atom, alkyl, cycloalkyl, cycloalkenyl and phenyl;

R11b and R12b, identical or different, denote a hydrogen atom, alkyl, cycloalkyl and phenyl; or R11b and R12b together with the nitrogen atom to which they are bound, form a possibly substituted piperazinil;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as shown above in which R2 and R3, identical or different, chosen among hydrogen atom, alkyl, phenylalkyl, pyridylethyl, sensationalise and citibankonline, possibly substituted by one or more radicals, selected among halogen atoms and hydroxyl, alkyl and alkoxyl containing from 1 to 4 carbon atoms, or R2 and R3 together with the carbon atom to which they are bound, form a 3-6-membered cycloalkyl or heterologously radical containing a nitrogen atom;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as shown above in which R2 and R3, identical or different, chosen among hydrogen atom, alkyl, hydroxyalkyl, phenylalkyl, hydroxyp is nilacala, pyridylethyl, sensationalise and citibankonline; or R2 and R3 together with the carbon atom to which they are bound, form cycloalkyl radical comprising 3 to 6 carbon atoms, or azetidinol, pyrrolidinyl and piperidinyl;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as shown above in which R2 and R3, identical or different, chosen among hydrogen atom, alkyl, hydroxyalkyl, phenylalkyl and hydroxyphenylethyl, or R2 and R3 together with the carbon atom to which they are bound, form cycloalkyl radical comprising 3 to 6 carbon atoms.

The object of the invention, in particular, are products of the formula (I), such as the above in which one of R2 and R3 is chosen from among a hydrogen atom and alkyl and the other of R2 and R3 is chosen among all values of R2 and R3; or R2 and R3 together with the carbon atom to which they are bound, form cycloalkyl radical comprising 3 to 6 carbon atoms;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as shown above in which R2 and R3, identical or different, denote a hydrogen atom and alkyl, or R2 and R3 together with the carbon atom is, with which they are linked, form cycloalkyl radical comprising 3 to 6 carbon atoms;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as shown above in which R2 and R3, identical or different, denote a hydrogen atom and CH3or R2 and R3 together with the carbon atom to which they are bound, form cyclopropyl;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which A1 means a simple link, and A2 choose among simple relationship, linear or branched alkyl, containing at most 6 carbon atoms, and allyl, propenyl, C=O and SO2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which A1 means a simple link, and A2 choose among simple communication, alkyl, allyl, propenyl, C=O and SO2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are the products of the formula is (I), such as the above, in which A1 means a simple bond, and A2 is chosen among alkyl, allyl, propenyl, C=O and SO2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which A1 means a simple link, and A2 denotes alkyl or C=O;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which A1 means a simple link, and A2 indicates C=O, CH2-CH2- or-CH2-;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which A1 means a simple link, and A2 denotes-CH2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which Y and Y1 are such that one means a hydrogen atom, halogen atom or amino group, and the other choose among-OCF3, -O-CF2-CHF2, -O-CHF2, -O-CH2CF 3, SF5, -S(O)n-CF3, -S(O)n-Alk, -SO2CHF2, SO2CF2CF3, -SO2NH2, -S-CF2-CF2-CF3, -S-Alk-O-Alk, -S-Alk-OH, -S-Alk-CN, -S-Alk-morpholinopropan, -S-Alk-pyrrolidinyl and-S-Alk-piperazinil, and morpholinopropan, pyrrolidinyl and piperazinil possibly substituted with Alk, where Alk denotes alkyl with 1-4 carbon atoms;

and the other substituents of the above product of formula (I) are selected from the values specified in accordance with the present invention.

The object of the invention, in particular, are products of the formula (I), such as the above, in which Y represents a hydrogen atom, and Y1 is chosen among-OCF3, -S(O)n-CF3, -S(O)n-CH3, -SO2CHF2and-SO2NH2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which Y represents a hydrogen atom, and Y1 is chosen among-OCF3, -S(O)n-CF3and-SO2CHF2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which Y represents a hydrogen atom, and Y1 is chosen among-OCF3and-S(O)n-CF 3;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which Y represents a hydrogen atom, and Y1 is chosen among-OCF3S-CF3and-S(O)2-CF3;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, where B2 denotes monocyclic or bicyclic heteroaryl radical selected among pyridyl, pyrimidinyl, chinoline, isoindolyl, 1H-pyrrolo[2,3-b]pyridinyl, chinadoll, thiazolyl, imidazolyl, pyrazolyl, furazane, isoxazolyl, morpholinyl, pyrrolidinyl, furil, piperidyl, teinila, chromene, oxopropanal, indolyl, pyrrolyl, purinol, benzoxazine, benzimidazolyl, benzofuranyl, and these radicals possibly substituted by one or more radicals chosen among the values of Y2;

and the other substituents of the above product of formula (I) have the values specified for the products of formula (I).

The object of the invention, in particular, are products of the formula (I), such as the above, where B2 denotes heteroaryl radical selected among the 3 - or 4-pyridyl, 3 - and 4-chinoline, imidazolyl, thiazolyl, indolyl, pyrazolyl, pyrrolyl, pyrimidyl, purinol, benzoxazine, benzimidazolyl, benzofuranyl, and these radicals possibly substituted by one or more radicals selected from Y2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, where B2 denotes heteroaryl radical selected among 4-pyridyl, 4-chinoline, imidazolyl, thiazolyl, pyrazolyl, pyrrolyl, pyrimidyl and purine, and these radicals possibly substituted by one or more radicals selected from Y2;

and the other substituents of the above product of formula (I) have any of the above values.

In the products of formula (I), in particular, B2 means a heteroaryl radical chosen among the 3 - or 4-pyridyl, pyrimidinyl, 3 - or 4-chinoline, isoindolyl, chinadoll, thiazolyl, imidazolyl, pyrazolyl, furazane and isoxazolyl, and these radicals possibly substituted by one or more radicals selected from Y2;

and the other substituents of the above product of formula (I) are shown according to the present invention.

In the products of formula (I), in particular, B2 means ethereally radical, choose among 3 - or 4-pyridyl, pyrimidinyl, 3 - or 4-chinoline, azaindole and chinadoll, and these radicals possibly substituted by one or more radicals selected from Y2;

and the other substituents of the above product of formula (I) are shown according to the present invention.

The object of the present invention is the products of formula (I), such as the specified according to the present invention, in which B2 means 4-pyridyl and 4-chinolin, 1H-pyrrolo[2,3-b]pyridine-4-yl, possibly substituted by one or more radicals chosen among the values of Y2, listed according to the present invention;

and the other substituents of the above product of formula (I) are shown according to the present invention.

In the products of formula (I) according to the present invention, in particular, Y2 can mean 2-aminopyridine-4-yl in which the amino group possibly substituted as indicated for radical NR5R6, as described above or below in the experimental part;

and the other substituents of the above product of formula (I) can have values such as these in accordance with the present invention for the above-mentioned substituents.

The products of formula (I) according to the present invention in particular are such that Y2 denotes a hydrogen atom, the atom halog is on, hydroxyl, cyano, alkyl, alkoxyl, phenyl, COOH, COOAlk, CONR5R6, NR5R6, -NR10-COOR6, -NR10-CO-R6, -NR10-CS-NR5R6, -NR10-CO-NR5R6 or-NR10-SO2-R6, and these radicals possibly substituted;

R5 and R6, identical or different, chosen among hydrogen atom, alkyl, cycloalkyl, phenyl and heteroaryl radicals, which is a 5-6-membered ring containing 1-3 heteroatoms selected among O, N and S, all these radicals possibly substituted; or R5 and R6 together with the nitrogen atom to which they are bound, form a possibly substituted pyrrolidinyl, piperidyl, piperazinil, morpholinyl or hintline;

R10 denotes a hydrogen atom or alkyl;

all the above alkyl, CNS, cycloalkyl and phenyl radicals, as well as the loop formed by R5 and R6 with the atom to which they relate, possibly substituted by one or more identical or different radicals, selected among halogen atoms and ceanography, hydroxyl, alkyl, alkoxyl, OCF3, CF3, S(O)n-CF3, nitro, carbonyl group, tocography, OCOAlk; phenyl, which itself is possibly substituted by one or more radicals, selected among halogen atoms and alkyl and alkoxyl; NH2, NHAlk, N(Alk)2, N(alk)(phenylalkyl), N(Alk)(aminoalkyl), N(Alk)(acylaminoalkyl), N(Alk)(dialkylaminoalkyl), free or esterified by alkyl of carboxyl;

and

all of the above is phenyl radicals may be even replaced by alkylenedioxy;

all the abovementioned alkyl radicals may still be substituted by one or more saturated or partially unsaturated 4-7-membered heterocyclic radicals containing at least one nitrogen atom N and, in addition, 0-2 other heteroatoms chosen among O, N and S;

all of the above pyrrolidinyl and girasolereale radicals may have substituted oxo - or tocography;

all the above alkyl and CNS radicals are linear or branched and containing at most 6 carbon atoms;

all of the above cycloalkyl radicals contain at most 7 carbon atoms;

other substituents of the above product of formula (I) have the above values.

The radicals R5 and R6, in particular, can represent the following heteroaryl radicals: pyridinyl, pyrazinyl, pyrimidinyl, thienyl, thiazolyl and oxazolyl, all these radicals possibly substituted.

In the products of formula (I) according to the present invention, in particular, alkyl radicals can be substituted heterocyclic radicals, selected from the following radicals: thiomorpholine-4-yl, thiazolidin-3-yl, azetidin-1-yl, piperazinil, imidazolyl, morpholinyl, pyrrolidinyl, piperidyl and azepane, all these radicals possibly substituted as indicated above, and in particular one or not is how many radicals, selected among alkyl, hydroxyalkyl, carbonyl group, pyridyl and phenyl, possibly substituted by one or more radicals, selected among halogen atoms and alkyl, hydroxyl, alkoxyl, CN, carboxyl or amino groups, which are possibly substituted.

Can be called, for example, piperazinil, possibly substituted with Alk, Alk-OH, pyridyl or phenyl, which itself is possibly substituted by one or more radicals, selected among halogen atoms and alkyl, hydroxyl, alkoxyl, CN, carboxyl or amino groups, which are possibly substituted; piperidyl, possibly substituted by one or two groups Alk; azepane, possibly substituted by exography.

The object of the present invention is the products of formula (I), such as the above, where Y2 denotes a hydrogen atom, halogen atom, hydroxyl, cyano, alkyl, alkoxyl, phenyl, CONR5R6, NR5R6, -NR10-COOH, -NR10-COOAlk, -NR10-CO-R6, -NR10-CS-NR5R6, -NR10-CO-NR5R6 or-NR10-SO2-R6;

R5 and R6, identical or different, chosen among hydrogen atom, alkyl, cycloalkyl, phenyl, pyrimidinyl, teinila, pyridyl, chinoline; thiazolyl, possibly substituted by one or two halogen atoms; Piran, possibly substituted by one or more groups OCOAlk; phenyl substituted by one or more radicals, selected among halogen atoms and alkyl, alkoxyl, amino, alkyl is of aminogruppy, dialkylamino and free or esterified with an alkyl radical carboxyl; alkyl substituted by phenyl, which itself is possibly substituted by one or more radicals, selected among halogen atoms, alkyl, alkoxyl, amino, alkylamino, dialkylamino, free or esterified alkyl radical carboxyl; alkyl substituted by piperazinil, which itself is possibly substituted by one or more radicals selected among Alk, Alk-OH and pyridyl; alkyl substituted by imidazolyl; alkyl substituted by one or more radicals selected among NH2, NHAlk, N(Alk)2, N(alk)(phenylalkyl), N(Alk)(aminoalkyl), N(Alk)(acylaminoalkyl) and N(Alk)(dialkylaminoalkyl); alkyl substituted by morpholinyl, possibly substituted by one or two groups Alk; alkyl substituted by pyrrolidinyl; alkyl substituted by piperidyl, which itself is possibly substituted by one or two groups Alk; alkyl substituted by thiomorpholine; alkyl substituted by azetidinol; alkyl substituted by aseania, possibly substituted by oxopropoxy;

or R5 and R6 together with the nitrogen atom to which they are bound, form a radical pyrrolidinyl, piperidyl, piperazinil, morpholinyl or hintline, all these radicals possibly substituted by one or more, same or different radical and, selected among halogen atoms and alkyl, hydroxyl, alkoxyl and phenyl, which itself is possibly substituted by one or more radicals, selected among halogen atoms and alkyl and alkoxyl;

and

pyrrolidinyl and hintline perhaps even substituted by oxo or tocography;

piperazinil himself possibly substituted by one or more radicals selected among Alk, Alk-OH and pyridyl;

R10 denotes a hydrogen atom or alkyl;

and

all the above alkyl or Alk and CNS radicals are linear or branched and containing at most 6 carbon atoms;

all of the above cycloalkyl radicals contain at most 7 carbon atoms;

all the phenyl radicals may be even replaced by a radical chosen among CF3, -OCF3, nitro and alkylenedioxy;

other substituents of the above product of formula (I) have any of the above values.

Of the preferred structures according to the present invention can be called the products of formula (I), three structures of which are given below, in which the values NR14R15 choose among values NR5R6 and values radicals of alkyl, aryl and heteroaryl choose among the values of alkyl, aryl and heteroaryl radicals, such as those mentioned above, and possibly substituted, as indicated according to astasia invention.

The object of the invention, in particular, are products of the formula (I), such as the above, where B2 denotes 4-pyridyl and 4-chinolin, possibly substituted by one or more radicals selected from Y2;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, in which Y2 means V1, halogen atom, hydroxyl, -C(=NH)NH2, OV1, O-CO-V1, COOV1, COV1, CO-NV1V2, -NV1V2, -NH-CO-V1, -NH-COO-V1, -NH-NH-CO-V1, -NV1-CO-NV1V2, -NV1-CO-NHV1, -NH-CO-NHV1, -NH-SO2-NHV1 and-NH-SO2-V1, where V1 and V2 are identical or different, denote a hydrogen atom, alkyl, cycloalkyl or phenyl or heterocyclic radical, such as pyridinyl, pyrazolyl, imidazolyl, dihydroimidazole, tetrazolyl, morpholinyl, piperazinil, piperazinylmethyl, alkylpiperazine, phenylpiperazines, thienyl, furanyl, piperidinyl, methylpiperidine, pyridyl, pyrrolidinyl and pyrrolidinyloxyl;

and

all the alkyl, phenyl and heterocyclic radicals possibly substituted by one or more radicals, selected among halogen atoms, hydroxyl radicals, alkyl, alkoxyl, CF3, NH2, NHAlk, N(alk)2and phenyl, which itself is possibly substituted by one or more substituents, labiraakimised of halogen atoms, hydroxyl and alkoxyl;

all the above-mentioned phenyl and heterocyclic radicals may still be substituted by one or more alkyl radicals;

phenyl radicals may still be replaced by a radical NR5R6, where R5 and R6 are as above;

other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, where Y2 denotes a hydrogen atom, halogen atom, alkyl, cycloalkyl, hydroxyl, alkoxy, free or esterified by alkyl or phenyl, carboxyl, NH2, NHalk, N(alk)2and phenyl;

All alkyl, CNS and phenyl radicals possibly substituted by one or more radicals, selected among halogen atoms, hydroxyl, (C1-C4)-alkyl, (C1-C4)-alkoxyl, CF3, NH2, NHalk, N(alk)2and phenyl, which itself is possibly substituted by one or more substituents selected among halogen atoms, hydroxyl and alkoxyl;

All the phenyl radicals may still be substituted by one or more (C1-C4)-alkyl radicals and possibly substituted with NR5R6, where R5 and R6 are as above;

other substituents of the above product of formula (I) have any of shaukatullah values.

The object of the invention, in particular, are products of the formula (I), such as the above, where Y2 denotes a hydrogen atom, F, Cl, CH3CH2CH3, OH, OCH3, NH2, NHAlk and phenyl, possibly substituted with NR5R6, where R5 and R6 are as above;

and the other substituents of the above product of formula (I) have any of the above values.

The object of the invention, in particular, are products of the formula (I), such as the above, where B2 denotes 4-pyridyl and 4-chinolin substituted by one or two radicals, selected among F, Cl, OH and och3;

and the other substituents of the above product of formula (I) have any of the above values.

Some of the products of formula (I) according to the present invention the following group:

can mean, in particular, the following radicals:

Some of the products of formula (I) according to the present invention, the group-A2-B2-Y2 can mean, in particular, the following radicals:

In the products of formula (I) according to the present invention R2 and R3 together can form, in particular, cycloalkenyl or heterologously radical or, equal or different, can mean, in particular, a hydrogen atom and m is L.

The products of formula (I), such as above corresponding to the formula (IC):

in which

YC and Y1C are such that one means a hydrogen atom, halogen atom or amino group, and the other choose among-OCF3, -O-CF2-CHF2, -O-CHF2, -O-CH2-CF3, SF5, -S(O)n-CF3, -S(O)n-Alk, -SO2CHF2, SO2CF2CF3, -SO2NH2, -S-CF2-CF2-CF3, -S-Alk-O-Alk, -S-Alk-OH, -S-Alk-CN, -S-Alk-morpholinopropan, -S-Alk-pyrrolidinyl and-S-Alk-piperazinil, and morpholinopropan, pyrrolidinyl and piperazinil possibly substituted with Alk, where Alk denotes an alkyl radical containing from 1 to 4 carbon atoms;

or phenyl radical with his deputies YC and Y1C forms one of the following radicals:

R2C and R3C, identical or different, denote a hydrogen atom or a possibly substituted alkyl, or R2C and R3C, together with the carbon atom to which they are attached, form a (C3-C10-cycloalkyl or heteroseksualci;

AS means a simple link or CH2;

B2C means radicals pyridyl, pyrimidinyl, hinely, isoindolyl, chinadoll, thiazolyl, imidazolyl, pyrazolyl, furutani, isoxazolyl, morpholinyl, pyrrolidinyl, furyl, piperidyl, bromanil, oxopropanal, chinadoll, thienyl, indolyl, pyrrolyl, purinol benzoxazines, benzimidazolyl, benzofuranyl, possibly substituted by one or more radicals selected among values Y2A;

Y2CA means a hydrogen atom, halogen atom, hydroxyl, cyano, alkyl, alkoxyl, phenyl, COOH, COOAlk, CONR5R6, NR5R6, -NR10-COOH, -NR10-COOAlk, -NR10-CO-R6, -NR10-CS-NR5R6, -NR10-CO-NR5R6 or-NR10-SO2-R6, all these radicals possibly substituted;

R5 and R6, identical or different, chosen among hydrogen atom, alkyl, cycloalkyl, phenyl, pyrimidinyl, teinila, pyridyl, chinoline, thiazolyl and Piran, all these radicals possibly substituted; or R5 and R6 together with the nitrogen atom to which they are bound, form a possibly substituted pyrrolidinyl, piperidyl, piperazinil, morpholinyl or hintline;

R10 denotes a hydrogen atom or alkyl;

All the above alkyl, Alk or ALK, CNS, cycloalkyl and phenyl radicals, as well as the loop formed by R5 and R6 together with the atom to which they relate, possibly substituted by one or more identical or different radicals, selected among halogen atoms or ceanography, hydroxyl, alkyl, alkoxyl, OCF3, CF3, S(O)n-CF3, nitro, carbonyl group, tocography, OCOAlk; phenyl, which itself is possibly substituted by one or more radicals, selected among halogen atoms and alkyl and alkoxyl; NH2, NHAlk, N(Alk)2, N(alk)(phenylalkyl), N(Alk)(a is isoalkyl), N(Alk)(acylaminoalkyl), N(Alk)(dialkylaminoalkyl), free or esterified by alkyl of carboxyl;

All of the above-mentioned phenyl radicals may be even replaced by alkylenedioxy:

all the abovementioned alkyl radicals may still be substituted by one or more radicals selected among piperazinil, which may substituted with Alk, Alk-OH and pyridyl; imidazolyl; morpholinyl; pyrrolidinyl; piperidyl, which itself is possibly substituted by one or two groups alk; azepane, possibly substituted by oxopropoxy;

all of the above pyrrolidinyl and girasolereale radicals may have substituted oxo - or tocography;

all the above alkyl and CNS radicals are linear or branched and containing at most 6 carbon atoms;

all of the above cycloalkyl radicals contain at most 7 carbon atoms;

n means an integer from 0 to 2;

the above products of formula (IC) are in all possible racemic, enantiomeric and diastereoisomeric isomeric forms,

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (IC).

In the products of formula (I), in particular, following the radical, which may form a phenyl with vomi substituents Y and Y1:

can mean the following radical:

The object of the present invention, in particular, are products of the formula (I), such as above corresponding to the formula (IA):

in which:

Y1A means OCF3, S(O)n-CF3and SO2CHF2;

VA means radicals 4-chinolin and 4-pyridyl, possibly substituted by one or more radicals selected among values Y2A;

Y2A has the value shown above for Y2;

R2A and R3A, identical or different, denote a hydrogen atom or a possibly substituted alkyl, or R2A and R3A together with the carbon atom to which they are attached, form a (C3-C10-cycloalkyl or heteroseksualci;

all the alkyl and phenyl radicals possibly substituted by one or more radicals, selected among halogen atoms, HE, alk, Oalk, OCF3, S(O)n-CF3, CF3, NH2, NHAlk and N(alk)2;

n means an integer from 0 to 2;

with the above products of formula (IA) are all possible racemic, enantiomeric and diastereoisomeric isomeric forms,

as well as additive salts with inorganic and organic acids or with inorganic and organic bases of the above product of formula (IA).

The object of the crust is asego of the invention, in particular the products of formula (IA), such as the above, where Y1A, B2a, R2A and R3A have the above values and Y2A means a halogen atom, -OH, -alk, -Oalk, -Oall, -NR5AR6A, -CO2H, -CO2alk, -CO-NR5AR6A, -S(O)n-CF3, -NH-S(O)n-CF3or phenyl, and alk means a linear or branched alkyl radical containing at most 6 carbon atoms, all the alkyl, CNS and phenyl radicals possibly substituted;

R5A and R6A, identical or different, denote a hydrogen atom, alkyl, cycloalkyl, phenyl, and alkyl and phenyl radicals possibly substituted; or R5A and R6A together with the nitrogen atom to which they are attached, form a cyclic radical chosen among pyrrolidinyl, piperidinyl, piperazinil, morpholinyl, indolinyl, perindopril, tetrahydroquinoline and azetidine;

All alkyl, CNS and phenyl radicals possibly substituted by one or more radicals chosen among a halogen atom, HE, alk, Oalk, OCF3, S(O)n-CF3, CF3, NH2, NHAlk and N(alk)2;

n means an integer from 0 to 2;

the above products of formula (IA) are all possible racemic, enantiomeric and diastereoisomeric isomeric forms,

as well as additive salts of inorganic and organic acids or with inorganic and organic bases to enter the specified products of the formula (IA).

The object of the present invention, in particular, are products of the formula (IA), such as the above, in which:

Y1A means OCF3SCF3or S(O)2-CF3;

B2a means 4-chinolin or 4-pyridyl, possibly substituted by one or two radicals, selected among halogen atom, -HE, alk, -Oalk, -CO2H, -CO2alk, -NR5AR6A, -CF3, OCF3and possibly substituted phenyl;

R5A and R6A, identical or different, denote a hydrogen atom, alkyl, cycloalkyl, phenyl, and alkyl and phenyl radicals possibly substituted; or R5A and R6A together with the nitrogen atom to which they are attached, form a cyclic radical chosen among pyrrolidinyl, piperidinyl, piperazinil, morpholinyl and azetidine;

R2A and R3A, identical or different, denote a hydrogen atom or a possibly substituted alkyl; or R2A and R3A together with the carbon atom to which they are attached, form a (C3-C6)-cycloalkenyl or heterologously radical;

All the alkyl and phenyl radicals possibly substituted by one or more radicals chosen among a halogen atom, HE, alk, Oalk, OCF3, S(O)n-CF3, CF3, NH2, NHAlk and N(alk)2;

the above products of formula (IA) are all possible racemic, enantiomeric and diastereoisomeric isomeric forms,

as well as additive salt reorgani the definition and organic acids or with inorganic and organic bases of the above product of formula (IA).

The object of the present invention, in particular, are products of the formula (I), such as above corresponding to the formula (IA)in which:

Y1A means OCF3SCF3or S(O)2-CF3;

B2a means 4-chinolin or 4-pyridyl, possibly substituted by one or two radicals, selected among halogen atoms, -HE, alk and-Oalk;

R2A and R3A, identical or different, denote a hydrogen atom or a linear or branched alkyl at most four carbon atoms, possibly substituted by hydroxyl; or R2A and R3A together with the carbon atom to which they are attached, form a (C3-C6)-cycloalkenyl radical;

With the above products of formula (IA) are all possible racemic, enantiomeric and diastereoisomeric isomeric forms,

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (IA).

The object of the present invention, in particular, are products of the formula (I), such as above corresponding to the formula (IA)in which:

Y1A means OCF3SCF3or S(O)2-CF3; and

R2A and R3A, identical or different, denote a hydrogen atom and CH3; or R2A and R3A together with the carbon atom to which they are bound, form cyclopropyl;

And the other substituents have any one to enter the specified values;

the above products of formula (IA) are all possible racemic, enantiomeric and diastereoisomeric isomeric forms,

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (IA).

The object of the present invention are products of the formula (I), such as above corresponding to the formula (IB):

in which R2, R3, A1, Y, Y1, A2, B2, and Y2 have the above meanings;

with the above products of formula (IB) are in all possible racemic, enantiomeric and diastereoisomeric isomeric forms,

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (IB).

The object of the present invention are the products of formula (IB), such as the above, in which:

Y1 means OCF3SCF3or S(O)2CF3; and

R2 and R3, identical or different, denote a hydrogen atom and CH3; or R2 and R3 together with the carbon atom to which they are bound, form cyclopropyl;

And the other substituents have any of the above values;

the above products of formula (IB) are in all possible racemic, enantiomeric and diastereoisomeric isomer is ormah,

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (IB).

Of the preferred products according to the invention, more specifically, you can call the products of formula (I), such as the above, the names of which follow:

- triptorelin (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (S)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-4-methyl-3-quinoline-4-ylmethyl-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it;

- triptorelin (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triptime sulfanilyl)imidazolidin-2,4-dione;

- triptorelin (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-(4-hydroxybenzyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-(4-hydroxybenzyl)-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-(1-hydroxyethyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin (R)-1-(3-hydroxypyridine-4-ylmethyl)-5-methyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-(3-METI the pyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 4-quinoline-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-methylpyridin-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The preferred product is according to the invention in particular can be called the products of formula (I), such as the above, the names of which follow:

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide cyclopropanecarbonyl acids;

- triptorelin 5,5-dimethyl-1-[2-(pyridine-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-isobutyramide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

hydrochloride of 1-(2-aminopyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide pyridine-2-carboxylic acid;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-piperidine-1-ylpropionic;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-[4-(2-hydroxyethyl)piperazine-1-yl]propionamide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-morpholine-4-ylpropionic;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-t is attorneysalbanyny)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-pyrrolidin-1-ylpropionic;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-methylpiperazin-1-yl)propionamide;

- 1-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-phenylacetone;

- 1-[2-(6-ethylpyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(6-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4,6-dimethylpyridin-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(3,5-dichloropyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(pyridine-4-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(pyridine-3-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(2-oxazepan-1-yl)propionamide;

- 3-(benzylmethylamine)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

- 45-diacetoxy-6-acetoxymethyl-2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]-pyridine-2-yl}theoreticaly acid;

- 5,5-dimethyl-1-[2-(5-methylpyridin-2-ylamino)pyridine-4-yl-methyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl} - for 3,5-dimethoxybenzamide;

- triptorelin 5,5-dimethyl-1-[2-(pyrazin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3-methylpiperidin-1-yl)propionamide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3,5-dimethylpiperidin-1-yl)propionamide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-methoxybenzamide;

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide pyrazin-2-carboxylic acid;

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide thiophene-2-carboxylic acid;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-4-methylbenzamide;

- 1-isoquinoline-5-yl-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 3-(4-Aza reparacin-1-yl)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

- 3-[4-(2-diethylaminoethyl)piperazine-1-yl]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(2,6-dimethylmorpholine-4-yl)propionamide;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-pyrrolidin-1-reparacin-1-yl)propionamide;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-2-(4-pyrrolidin-1-reparacin-1-yl)ndimethylacetamide;

- 5,5-dimethyl-1-[2-(4-methylpyridin-3-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(6-morpholine-4-espiridion-3-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2,6-dimethylpyridin-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

methyl ester of 5-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-ylamino}pyridine-2-carboxylic acid;

- 1-[2-(2,6-dimethoxypyridine-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(6-herperidin-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(6-methoxypurine the-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the present invention is also a method of obtaining the products of General formula (I), such as specified above, characterized in that:

or the product of formula (II):

in which Y' and Y1' have the meanings indicated above, respectively for Y and Y1, in which the possible reactive functional groups may secure and R have the above significance,

in the presence of tertiary bases enter into interaction with the product of formula (III):

in which X means-A2'-B2'-Y2' or a hydrogen atom and A2', B2'and Y2', R2' and R3' have the meanings indicated above, respectively for A2', B2'and Y2', R2' and R3', in which the possible reactive functional groups may secure

to obtain the product of formula (IV):

in which Y', Y1', X, R, R2' and R3' have the above values,

which, if necessary or if desired, is subjected to any one or more of the following reactions, in any order:

a) implement the function of the possible elimination of the protective groups, which can carry Y', Y1', R, R2', R3' and X, when X is-A2'-B2'-Y2';

b) hydrolysis reaction of the group

before ketogroup;

(C) effect on the products of formula (IV)in which X means a hydrogen atom, and after a possible hydrolysis of the group

before ketogroup reagent of formula Hal-A2'-B2'-Y2'in which A2', B2' and Y2' have the above meanings and Hal denotes a halogen atom, to obtain products of formula (Ii):

in which Y', Y1', R2', R3', A2', B2' and Y2' have the above values,

then, if desirable, the impact on these products agent possible elimination of the protective groups, which can carry Y', Y1', R2', R3', A2', B2' and Y2', or, in the desirable case, the impact of agent esterification, amidation or salt formation;

either the product of the above formula (II) in the presence of tertiary bases enter into interaction with the product of formula (III'):

in which R2' and R3' have the above meanings and Q is either an atom of an alkali metal, e.g. sodium atom, or an alkyl radical with 1-6 carbon atoms, to obtain the product of formula (IVa):

in which Y', Y1', R, R2', R3' and X have the above meanings, which, if desired, is subjected to any one or not is how many of the following reactions, in any order:

a) reaction of the possible elimination of the protective groups, which can carry X;

b) impact on the products of formula (IVa), in which X means a hydrogen atom, a reagent of formula Hal-A2'-B2'-Y2'in which A2', B2' and Y2' have the above meanings and Hal denotes a halogen atom, to obtain products of formula (Iii):

in which Y', Y1', R, R1, R2', R3' and A2', B2' and Y2' have the above values,

then, if desirable, the impact on these products agent possible elimination of the protective groups, which can carry Y', Y1', R2', R3', A2', B2' and Y2', or, in the desirable case, the impact of agent esterification, amidation or salt formation;

or a reagent of formula Hal-A2'-B2'-Y2'in which A2', B2', Y2' and Hal have the above values, enter into interaction with the product of formula (IV'):

in which Y', Y1', R2'and R3' have the above meanings, to obtain the product of formula (IV"):

in which Y', Y1', R2', R3', A2', B2' and Y2' have the above values,

which, if necessary or if desired, is subjected to the reactions of elimination of possible protective groups, which can carry-A2'-B2'-Y2', then, in the desirable case, is exposed to agent esterification, amidation or salt formation.

You will notice that, depending on C is of acini Y', Y1', R2', R3', A2', B2' and Y2', the products of formulae (IV), (Ii), (IVa), (Iii) and (IV) may constitute the products of formula (I) and that, to get another or other products of formula (I), these products, if it is desired or if necessary, can be subjected to one or more of the following reactions reactions, in any order:

a) reaction of esterification of the acid functional groups;

b) reaction of saponification of ester groups to acid groups;

(C) the oxidation reaction of ancilliary to the corresponding sulfoxide or sulfone;

d) reaction of turning ketogroup in oximo group;

(e) the reduction of the free or esterified carboxyl group to an alcohol group;

f) reaction of turning CNS group in a hydroxyl group or more hydroxyl groups in the CNS group;

(g) the oxidation of the alcohol group to the aldehyde group, an acid group or catography;

h) reaction of turning ceanography in tetrazolyl group;

i) the reduction of nitro compounds to amino compounds;

(j) the elimination reaction of protective groups which may have a protected reactive functional group;

k) the reaction of the salt formation with an inorganic or organic acid or base to obtain the corresponding salt;

l) the reaction razdelnye.istorichesky forms for individual products;

and thus obtain the products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms.

You may notice that such reaction conversion of substituents into other substituents can also be implemented in case of initial products and intermediate products, such as those mentioned above, to continue the synthesis according to the reactions indicated in the above-described method.

Various reactive groups, which may bear some connection, in the case of the above reactions, if necessary, can be protected: we are talking about, for example, free hydroxyl, acyl, carboxyl groups or more of amino - and monoalkylamines that can be protected by protective groups.

May be represented by the following, but not exhaustive, list of examples of protection of reactive groups:

- hydroxyl group may be protected, for example, alkyl radicals such as tert-butyl, trimethylsilyl, tert-butyldimethylsilyl, methoxymethyl, tetrahydropyranyl, benzyl or acetyl;

the amino group may be protected, for example, acetyl, tritely, benzyl, tert-butoxycarbonyl, benzyloxycarbonyl radicals, phthalimidopropyl or other radicals known in the chemistry of peptides;

- acyl groups such as formyl group may be protected, for example, in the form of cyclic and acyclic ketals or tionately, such as dimethyl-or diethylacetal, or atlanticocean, or dietetical, or atlanticocean;

acid group of the above products, if desirable, can be lidirovali using primary or secondary amine, for example, in chloromethane in the presence of, for example, the hydrochloride of 1-ethyl-3-(dimethylaminopropyl)carbodiimide at room temperature;

acid group may be protected, for example, in the form of esters formed in the form of easily biodegradable esters, such as complex benzyl, or tert-butyl esters or esters known in the chemistry of peptides.

These reactions a) to (k)above, may be implemented, for example, as described below.

a) the Above products, if desired, can be subjected to esterification reactions on possible carboxyl groups, which can be carried out by conventional means known to the expert.

b) the Possible conversion of ester groups to the acid group of the above products can be, if desired, carried out in the usual, well-known specialist conditions, in particular by acid or alkaline hydrolysis, for example, by using a hydroxide on the model or potassium hydroxide in alcoholic medium, such as, for example, methanol, or even by using hydrochloric acid or sulphuric acid.

C) Possible ancilliary the above products in which the alkyl radical possibly substituted by one or more halogen atoms, in particular tortomasi may be, if desired, converted into the corresponding sulfoxide or sulfonic group in the usual, well-known specialist conditions such as, for example, using nagkalat, as, for example, over-acetic acid or metaglidasen acid, or else by means of ozone, oxone, periodate sodium in a solvent such as, for example, dichloromethane or dioxane, at room temperature.

Education sulfoxide group can be achieved by using equimolar mixtures containing allylthiourea product and reagent, such as, in particular, nagkalat.

Education sulfonic group can be achieved using a mixture containing allylthiourea product with an excess of reagent, such as, in particular, nagkalat.

d) Reaction of turning ketogroup in the reaction can be carried out in a conventional, well-known specialist conditions as, in particular, the impact in the presence of possible O-substituted hydroxylamine in an alcohol, such as, for example, ethanol, at room temperature or when heated.

e) Possible free or esterified carb is cselenyi group of the above products, if desirable, can be restored to alcohol groups by well-known specialist methods: the possible esterified carboxyl group, if desired, can be restored to an alcohol group known specialist methods, and in particular, using sociallyengaged in a solvent such as, for example, tetrahydrofuran or even dioxane or diethyl ether.

Possible free carboxyl group of the above products, if desirable, can be restored to an alcohol group, in particular, by using a boron hydride.

f) Possible CNS group, such as, in particular, metoxygroup, the above products, if desired, can be converted into a hydroxyl group in the usual, well-known specialist conditions, for example, using tribromide boron in a solvent such as, for example, dichloromethane, using a hydrobromide or hydrochloride of pyridine or even using a solution of bromovalerate in water or hydrochloric acid, or triperoxonane acid by boiling under reflux.

g) Possible alcohol group of the above products, if desired, can be converted into aldehyde or acid group by oxidation in a conventional, well-known specialist conditions such as, for example, by exposure to manganese oxide, to obtain the Alda is the Idov or Jones reagent to obtain the acid.

h) Possible ceanography the above products, if desirable, can be turned into tetrazolyl in the usual, well-known specialist conditions such as, for example, by reaction of azide cycloaddition of a metal, such as, for example, sodium azide or trialkylborane, cyano, as indicated in the method described in serving as a reference the following article: S. KOZIMA, etc., J. Organometallic Chemistry,33, 337 (1971).

You may notice that the reaction of the conversion of carbamate into urea, and in particular sulfonylamino in the sulfonylurea may be implemented, for example, at the boiling point under reflux of the solvent, such as toluene, in the presence of an appropriate amine.

It is clear that the above reaction can be carried out as specified, or else desirable in the case, according to other conventional methods known to the expert.

i) Elimination of the protective groups such as, for example, the above-mentioned protective group can be carried out in a conventional, well-known specialist conditions, in particular by acid hydrolysis carried out using acids such as hydrochloric acid, benzosulfimide or p-toluene-acid, formic acid or triperoxonane acid, or by catalytic hydrogenation.

Phthalimidopropyl can be removed with the aid of the completion of hydrazine.

The list used by the various protective groups can be found, for example, in French patent 2499995.

(j) the Above products, if desired, can be subjected to salt formation reactions, for example, when using inorganic or organic acids or with inorganic or organic bases, according to conventional, well-known specialist methods.

k) the Possible optically active forms of the above products can be obtained by separation of racemic mixtures of conventional, well-known specialist of ways.

The interaction of the products of formula (II) with the products of the formula (III) is carried out preferably in an organic solvent, such as tetrahydrofuran or dichloroethane, however, you can also use diethyl ether or diisopropyl ether.

Work, if necessary, in the presence of a tertiary base such as triethylamine or more pyridine or metiletilpiridin.

Possible reactive groups, which may be protected, in the product of formula (III), (IVa) or (IV) are hydroxyl groups or amino groups. To protect these groups use conventional protective group. As examples the following aminosidine groups: tert-butyl, tert-amyl, trichloroacetyl, chloroacetyl, benzhydryl, trityl, formyl, benzyloxycarbonyl the mud.

As a protective group for hydroxyl can be called radicals, such as formyl, chloroacetyl, tetrahydropyranyl, trimethylsilyl, tert-butyldimethylsilyl.

Needless to say that the above list is not exhaustive and there may be used other protective groups, for example, known in the chemistry of peptides. The list of such protective groups may be found, for example, in French patent 2499995, the contents of which are included in this context by reference.

Possible elimination reaction of the protective groups is carried out as shown in the above patent 2499995. The preferred method of elimination is acid hydrolysis using acids selected among hydrochloric acid, benzosulfimide or p-toluenesulfonic acid, formic acid or triperoxonane acid. The preferred hydrochloric acid.

The reaction of hydrolysis of the group

before ketogroup also preferably carried out using an acid such as hydrochloric acid, for example, by boiling under reflux.

The impact on the products of formula (IV), (IVa) or (IV') of the reagent of formula Hal-A2'-B2'-Y2' is carried out in the presence of a strong base such as sodium hydride or potassium. You can work through the implementation of the interfacial reaction in the presence of the Quaternary ammo yevich salts, such as tert-butylamine.

Example of elimination of tert-butyldimethylsilyloxy group with hydrochloric acid is given below in the examples.

Possible etherification of the free radical IT is carried out in classical terms. You can use, for example, an acid or a functional derivative, for example, anhydride, such as acetic anhydride, in the presence of a base, such as pyridine.

Possible esterification or salt formation can group COOH is carried out in classic conditions, known to the specialist.

Possible amidation radical COOH is carried out in classical terms. You can use the impact of primary or secondary amine functional derivative of the acid, as, for example, a symmetrical or mixed anhydride.

The object of the present invention is also a method of obtaining products of formula (I):

in which Y', Y1', A1, R, R1, R2' and R3' have the above meanings, wherein the product of formula (V):

in which A1, Y1' and Y2' have the above meanings and Hal denotes a halogen atom, enter into interaction with the product of formula (VI):

in which R, R1, R2', R3' and X have the above meanings, and the reaction is carried out in the presence rolled atora and if necessary, a solvent.

In regard to products of the formula (V), the term Hal preferably denotes chlorine atom, but can also mean a bromine atom, or iodine.

More specifically, an object of the invention is a method such as mentioned above, in which the catalyst is a metal in native or oxidized form or base.

The catalyst may be a metal in native form, in the form of a metal oxide or in the form of metal salts. The catalyst can also be the basis. When the catalyst is metal, this metal may be copper or Nickel.

The metal salts may be chloride or acetate.

You may notice that when A1 means a simple link, you can use the catalyst. When A1 denotes alkyl, then we are talking about the alkylation, which can be realized, in particular, in the presence of a reagent, such as a base.

When the catalyst is a base, this base can be, for example, sodium hydroxide or potassium, and, if desirable, can be added to the reaction medium dimethyl sulfoxide.

More specifically, an object of the invention is a method such as mentioned above, in which the catalyst is chosen among oxides of monovalent copper, divalent oxide of copper, copper in native form and Foundation, is such as sodium hydroxide or potassium.

Copper in native form, is used as the catalyst, is preferably in powder form.

The object of isbreene in particular is the way, such as specified above, in which the catalyst is an oxide of monovalent copper.

Used solvent is preferably chosen among the simple esters high boiling point, such as, for example, diphenyl ether, diglyme, trislim and dimethylsulfoxide, but can also be used, for example, oil with a high boiling point, such as paraffin or vaseline.

You may notice that, in particular, when A1 means a simple link, in case the reaction product of the formula (V) with the product of formula (VI), such as those mentioned above, as the catalyst can also use palladium or one of its salts, as described, for example, in the following articles, or salt of copper with the ligand, as a derivative of 1,2-diaminocyclohexane: S.L. Buchwald, J. Am. Chem. Soc., 6043 (2002); and S.L. Buchwald, J. Am. Chem. Soc., 7727 (2001).

The object of the invention features a method such as defined above, characterized in that the work in the presence of a solvent type, a simple ester, such as diphenyl ether, diglyme, trislim, dimethyl sulfoxide, toluene or dioxane.

The object of the invention features a method such as mentioned above, in the case of which the used solvent is diphenyl ether or trislim.

The method of obtaining the desired product, described above, can be carried out under pressure or at atmospheric pressure, preferably at an elevated temperature.

The object of the invention is also a method such as defined above, characterized in that the reaction is carried out at temperatures above 100°and preferably above 150°C.

More specifically, an object of the invention is a method such as defined above, characterized in that the reaction is carried out for more than 2 hours.

More specifically, an object of the invention is a method such as defined above, characterized in that the reaction is carried out in the presence of monovalent oxide of copper, triglyme at a temperature above or equal to 200°and for more than 3 hours.

The products that make up the object of the present invention, have an interest pharmacological properties: it is established that they have, in particular, any abscopal properties of protein kinases.

Of these kinases should be called, in particular, IGF1R.

It should also be called FAK.

It should also be called an ACT.

The tests listed below in the experimental part, explain the inhibitory activity of the products according to the present invention in relation to such protein kinases.

These properties, therefore, allow the use of roducti General formula (I) according to the present invention as a drug for the treatment of malignant tumors.

The products of formula (I) can also be used in the field of veterinary medicine.

The object of the invention therefore is the use as medicines pharmaceutically acceptable products of General formula (I).

The object of the invention in particular is used as a drug product, the names of which follow:

- triptorelin (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (S)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-4-methyl-3-quinoline-4-ylmethyl-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it;

- tripto the acetate (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-(4-hydroxybenzyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-(4-hydroxybenzyl)-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin (R)-5-(1-hydroxyethyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin (R)-1-(3-hydroxypyridine-4-ylmethyl)-5-methyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-(3-METI the pyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin 4-quinoline-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-methylpyridin-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

The object of the invention to persons whom nosti is used as medicinal products, the names of which follow:

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide cyclopropanecarbonyl acids;

- triptorelin 5,5-dimethyl-1-[2-(pyridine-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-isobutyramide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

hydrochloride of 1-(2-aminopyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide pyridine-2-carboxylic acid;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-piperidine-1-ylpropionic;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-[4-(2-hydroxyethyl)piperazine-1-yl]propionamide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-morpholine-4-ylpropionic;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov the l)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-pyrrolidin-1-ylpropionic;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-methylpiperazin-1-yl)propionamide;

- 1-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-phenylacetone;

- 1-[2-(6-ethylpyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(6-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4,6-dimethylpyridin-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(3,5-dichloropyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(pyridine-4-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(pyridine-3-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(2-oxazepan-1-yl)propionamide;

- 3-(benzylmethylamine)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-propionamide;

- ,5-diacetoxy-6-acetoxymethyl-2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]-pyridine-2-yl}theoreticaly acid;

- 5,5-dimethyl-1-[2-(5-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl} - for 3,5-dimethoxybenzamide;

- triptorelin 5,5-dimethyl-1-[2-(pyrazin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3-methylpiperidin-1-yl)propionamide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3,5-dimethylpiperidin-1-yl)propionamide;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-methoxybenzamide;

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide pyrazin-2-carboxylic acid;

- triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide thiophene-2-carboxylic acid;

- triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-4-methylbenzamide;

- 1-isoquinoline-5-yl-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 3-(4-Aza reparacin-1-yl)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

- 3-[4-(2-diethylaminoethyl)piperazine-1-yl]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(2,6-dimethylmorpholine-4-yl)propionamide;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-pyrrolidin-1-reparacin-1-yl)propionamide;

- N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-2-(4-pyrrolidin-1-reparacin-1-yl)ndimethylacetamide;

- 5,5-dimethyl-1-[2-(4-methylpyridin-3-ylamino)pyridine-4-yl-methyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(6-morpholine-4-espiridion-3-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2,6-dimethylpyridin-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

methyl ester of 5-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-ylamino}pyridine-2-carboxylic acid;

- 1-[2-(2,6-dimethoxypyridine-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(6-herperidin-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(6-methoxypurine the-3-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

with the above products of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as additive salts of inorganic and organic acids or with inorganic and organic bases of the above product of formula (I).

Products can be introduced parenterally, oral, perlingual, rectal, or local path.

The object of the invention are also pharmaceutical compositions characterized in that they comprise, as an active start, at least one of the drugs of General formula (I).

These compositions can be in the form of solutions or suspensions for injection, tablets, coated tablets, capsules, syrups, suppositories, creams, ointments and lotions. These pharmaceutical forms receive the usual ways. The active principle may be incorporated in excipients usually used in these compositions, such as aqueous or non-aqueous fillers, talc, gum Arabic, lactose, starch, magnesium stearate, cocoa butter, fatty substances of animal or vegetable origin, paraffin derivatives, glycols, various wetting, dispersing agents or emulsifying agents, preservatives.

The usual dose is variable depending on the exposed treatment of the subject and existing disease the ground state, may be, for example, from 10 mg to 500 mg per day for a man oral.

The present invention relates also to the use of products of formula (I), such as those mentioned above, or pharmaceutically acceptable salts of the above product of formula (I) to obtain drugs for inhibiting the activity of protein kinases and, in particular, one protein kinase.

The present invention relates also to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I), wherein the protein kinase is proteincontaining.

The present invention relates also to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I), in which the protein kinase is chosen from the following group: EGFR, Fak, FLK-1, FGFR1, FGFR2, FGFR3, FGFR4, FGFR5, flt-1, IGF-1R, KDR, DERIVED, tie2, VEGFR, AKT, Raf.

The present invention relates in particular to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I), wherein the protein kinase is IGF1R.

The present invention relates also to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above products is mswb formula (I), where the protein kinase is FAK.

The present invention relates also to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I), wherein the protein kinase is AKT.

The present invention relates also to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I), wherein the protein kinase is in a cell culture, and also to this application in the case of a mammal.

The present invention relates also to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I) for obtaining a medicinal product intended for the prevention or treatment of diseases characterized by the deregulation of the activity of protein kinases and, in particular, such diseases in a mammal.

The present invention relates to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I) for obtaining a medicinal product intended for the prevention or treatment of diseases related to the following group: disorders of proliferation of blood vessels, fibrations violations the Oia, violations proliferation mesangial cells, metabolic disorders, allergies, asthma, thrombosis, diseases of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, cancer, carcinoma.

The present invention relates in particular to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I) for obtaining a medicinal product intended for the treatment of cancer.

The present invention relates in particular to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I) for obtaining a medicinal product intended for the treatment of malignant tumors.

Of these malignant tumors of the present invention is of interest in particular in relation to the treatment of solid tumors and for the treatment of malignant tumors that are resistant to cytotoxic agents.

Of these malignant tumors of the present invention particularly relates to the treatment of cancer of the breast, stomach, colon, lung, ovaries, uterus, brain, kidney, larynx, lymphatic system, thyroid gland, urinary tract, enabling the th vesicles and the prostate tract, bone cancer, pancreatic cancer, melanoma.

The present invention is of interest in particular for the treatment of breast cancer, colon and lungs.

The present invention relates also to the use of products of formula (I), such as the above, or pharmaceutically acceptable salts of the above product of formula (I) for obtaining a medicinal product intended for chemotherapy of malignant tumors.

As medicines, according to the present invention, intended for chemotherapy zlokachestvennykh tumors, the products of formula (I) according to Angeles, the invention can be used individually or in combination with chemotherapy or radiation therapy or, alternatively, in combination with other therapeutic agents.

The present invention also relates in particular to pharmaceutical compositions, such as those described above, containing, in addition, effective the beginning of other chemotherapeutic drugs against cancer.

Such therapies can be commonly used antineoplastic agents.

As examples of known inhibitors of protein kinases include, in particular, butyrolactone, flavopiridol, 2-(2-hydroxyethylamino)-6-benzylamino-9-methylpurine, elemicin, Gleevec, and that the same iressa.

The products of formula (I) according to the present invention, thus, can also be advantageously used in combination with antiproliferative means: as examples of such antiproliferative agents but, however, without limiting the scope of protection of the invention this list can be called aromatase inhibitors, antiestrogens, inhibitors of topoisomerase I, topoisomerase II inhibitors, active against microcannulas agents, alkylating agents, inhibitors discontinuties inhibitors farnesyltransferase inhibitors SOH-2, MMP inhibitors, mTOR inhibitors, antineoplastic antimetabolites, platinum compounds that reduce the activity of protein kinases connection and also antiangiogenic compounds, agonists gonadorelin, antiandrogens, benhamadi, bisphosphonates and trastuzumab.

So, as examples, can be called antimicrobials agents, as taxaide, Vinca alkaloids, alkylating agents such as cyclophosphamide, intercalating DNA agents, such as CIS-platinum, interacting with topoisomerase agents, as camptothecin and derivatives, anthracyclines like adriamycin, antimetabolites, such as 5-fluorouracil and derivatives and analogs.

The present invention relates, therefore, to the products of formula (I) as inhibitors of protein kinases, and visheukazannogo formula (I) are all possible, racemic, enantiomeric and diastereoisomeric, isomeric forms, as well as additive salts of pharmaceutically acceptable inorganic and organic acids or with inorganic and organic bases of the above product of formula (I)and their proletarienne forms.

The present invention relates in particular to the products of formula (I), such as those described above, as inhibitors of IGF1R.

The present invention relates also to the products of formula (I), such as those described above, as inhibitors of FAK.

The present invention relates also to the products of formula (I), such as those described above, as inhibitors of the ACT.

The present invention relates in particular to the products of formula (IA), such as those described above, as inhibitors of IGF1R.

The products of formula (I) according to the present invention can be obtained by application or adaptation of known methods and, in particular, the methods described in the literature, such as those described R.C. Larock in the book "Comprehensive Organic Transformations", VCH publishers, 1989.

If these reactions may be necessary to protect reactive functional groups, such as, for example, hydroxyl group, amino group, aminogroup, tighrope or carboxyl when they desired in the final product, but when their participation is their undesirable reactions in the synthesis of products of formula (I). You can use the classic protective groups in accordance with the usual standard applications, such as those described, for example, by T.W. Greene and P.G. Wuts in the book "Protective Groups in Organic Chemistry", John Wiley and Sons, 1991.

Used first products of the formula (II) according to the invention can be obtained by exposure to phosgene, when X is an oxygen atom or thiophosgene, when X is a sulfur atom, the corresponding amine of formula (A) or aminoaniline derivative carrying the substituents Y and Y1', as above.

The product of this type is described in French patent 2329276.

The products of formula (III) or (III') are known or can be obtained from the corresponding cyanhydrin according to the method described in the publication: J. Am. Chem. Soc.,75, 4841 (1953).

The products of formula (III) can be obtained by exposure of the product of the formula Y2-B2-A2-Hal 2-cyano-2-aminopropan in the conditions specified above in the event of exposure Y2-B2-A2-Hal to the products of formula (IV). An example of obtaining this type is described in the link: Jilek, etc., Coll. Collect. Czech. Chem. Comm.,54(8), 2248 (1989).

The products of formula (IV') is described in the French patent 2329276.

The initial products of formulas (V) and (VI), is a process which is the object of the invention to obtain products of formula (I)are known and commercially available or can be obtained well-known specialist of ways.

Receive their products of the formula (VI) described, in particular, in the following publications:

- Zhur. Pröklad. Khim.,28, 969-975 (1955) [CA50, 4881a (1956)];

- Tetrahödron,43, 1753 (1987);

- J. Org. Chem.,52, 2407 (1987);

- Zh. Org. Khim.,21, 2006 (1985);

- J. Fluor. Chem.,17, 345 (1981);

or in patents: patent Germany 637318 (1935); European patent 0130875 and the Japan patent 81121524.

The products of formula (VI), which are derived as are widely used and cited in the literature as, for example, in the following articles:

- J. Pharm. Pharmacol., 67, including19(4), c. 209-216 (1967);

- Khim. Farm. Zh., 67, including1(5), S. 51-52;

the German patent 2217914;

European patent 0091596;

- J. Chem. Soc. Perkin Trans.,1, 219-221 (1974).

The products of formula (I) according to this application, such as the above, in which p denotes an integer of 0, and which, therefore, are derived as may be synthesized by the above method and, in particular, according to the following General scheme, in which case describes the synthesis on solid media. In the method, which follows the scheme given operating conditions such synthesis on solid media products of formula (I) according to the present application.

In the following experimental part contains a more specific explanation of such synthesis on a solid medium according to the above method in obtaining from the unity of the examples 1-56 according to the present application.

Such synthesis can be carried out according to the following General method.

From the resin Rinca, protected by a Fmoc group, removing the protective group using 20%solution of piperidine in dimethylformamide. The obtained amino bind with the amino acids protected by Fmoc group, in the presence of diisopropylcarbodiimide (DIC) and hydroxybenzotriazole (HOBt). From N-Fmoc-amino acid, deposited on a substrate, and then removing the protective group using 20%solution of piperidine in dimethylformamide. The free amine is injected into interaction with the aldehyde in the form of a solution in a mixture of tetrahydrofuran and triethylorthoformate (TEOF) in the ratio 50:50 with getting Schiff bases, which restores using cyanoborohydride sodium. The obtained amine condensed with an isocyanate or isothiocyanates with obtaining the corresponding urea or thiourea. When the isocyanate commercially available, it can be obtained from the corresponding amine by reaction 1/3 equivalent of triphosgene in the presence of 2 equivalents of pyridine. The product is then digested with a mixture of 95% triperoxonane acid and water. Thus freed urea cyclist with obtaining as expected. In some cases, the solution for splitting must be heated to a temperature of 80°for complete cyclization.

The products of formula (I) is according to this application, such as the above, in which p denotes an integer of 1, and which therefore represent derivatives dihydrouracil, can be synthesized by the above method and, in particular, according to the following General scheme, in which case describes the synthesis on solid media. In the method, which follows the scheme given operating conditions such synthesis on solid media products of formula (I) according to the present application.

In the following experimental part contains a more specific explanation of such synthesis on a solid medium according to the above method for obtaining the compound of example 5 of the present application.

For the synthesis of dihydrouracil on solid media, you can use the following method.

Use, for example, polystyrene Wang resin (1.7 mmol/g), which is treated with a mixture of β-amino acids, the acid chloride 2,6-dichlorobenzoyl acid and pyridine in dimethylformamide. After washing the resin is treated with 10%solution of piperidine in dimethylformamide. Obtained free amine enter into interaction with the aldehyde in a mixture of tetrahydrofuran and triethylorthoformate (TMOF). The resulting Schiff base restore using laborgerate sodium in a mixture of methanol, tetrahydrofuran and acetic acid. The resulting secondary is hydrated amine acelerou using phosgene and the resulting carbamoylated treated with a primary amine to obtain the corresponding urea. Cyclization to dihydrouracil, as well as cleavage of the final product is carried out by treatment with a strong base, such as databaseconnect (DBU).

The products of formula (I) according to the present application, therefore, can be synthesized on a solid medium as described above, or in the liquid phase according to the following method: in the experimental part of this application provides an explanation of such synthesis in the liquid phase in obtaining the compounds of examples 57-62.

In the case of this method of synthesis in the liquid phase can act according to two paths a and b, each of the two stages.

Path A:

Stage a:

Alkylation complex aminoether can be achieved by reductive amination using an aromatic or heterocyclic aldehyde according to the General method described in Advanced Organic Reaction, March, third edition, S. 798-800. In particular, the Schiff base (intermediate product) can be obtained from which, if necessary, in the form of a salt complex aminoether, aldehyde and, if necessary, desiccant (e.g., magnesium sulfate) in a solvent like dichloromethane or dichloroethane, at a temperature of from 0°C to the boiling temperature under reflux of the solvent. Formed Imin can be selected. Formed Imin restore with POM is using a metal hydride, as sodium borohydride in a solvent such as alcohol (e.g. ethanol or methanol)at a temperature of from 0°C to the boiling temperature under reflux of the solvent.

Stage b:

The obtained complex aminoether condense with the isocyanate in a solvent as tetrahydrofuran or dichloromethane, in the presence or not of a base (such as triethylamine) or acid (such as, for example, triperoxonane acid)at a temperature of from 0°C to the boiling temperature under reflux of the solvent. When isocyanates are commercially available, get them from the corresponding amines and triphosgene or diphosgene or phosgene in the presence of a base (e.g. pyridine or triethylamine) according to the General method described in Advanced Organic Reaction, March, third edition, S. 370.

The way In:

Stage a:

The isocyanate can be obtained by the condensation reaction of an aromatic or heterocyclic amine with diphosgene in the presence of activated vegetable carbon black in a solvent like toluene, at temperatures from -40°C to the boiling temperature under reflux of the solvent. The resulting isocyanate do not emit, and you can enter into interaction with complex aminoethanol or its salt in the same solvent in the presence of a base as triethylamine, at a temperature of from 0°C to the boiling point with bratim refrigerator solvent, obtaining the derived 3-ellimination-2,4-dione.

Stage b:

Condensation of this derivative with alkylhalogenide carried out in the presence of a base as tert-butyl potassium, or sodium hydride in a solvent like tetrahydrofuran (THF) or dimethylformamide (DMF), at temperatures from 0°C to the boiling temperature under reflux of the solvent.

The products of formula (I) according to the present application, which are products of examples No.201-207 according to the present application, receive, as described below in the experimental part, and as indicated in the following diagrams: these diagrams the Example I refers to example 201, Example II is an example 202, the Example III means the example 203, Example IV means the example 204, the Example V means example 205, Example VI means the example 206 and Example VII means the sample 207.

EXAMPLES I and II

EXAMPLES III and IV

EXAMPLES V, IV and VII

The synthesis of the products of formula (I) according to the present application, which are products of examples 208-243, carry out when using the way Century. Alkylhalogenide can be obtained from the corresponding carboxylic acids.

Ethylcarboxylates obtained by the esterification reaction of carboxylic KIS is from in ethanol in the presence of sulfuric acid, using the conditions described in Synthesis, 1138 (2000).

Recovery of ethylcarboxylates to alcohol is carried out in ethanol in the presence of sodium borohydride, using the conditions described in Synthesis, 1665 (2000).

Conversion of the thus obtained alcohol in alkylhalogenide exercise in the application of dibromothiophene as the halogenation agent, using the conditions described in J. Heterocyclic Chem.,30, 631 (1993).

Alkylhalogenide can also be obtained by radical synthesized corresponding metileno in the presence of N-bromosuccinimide and benzoyl peroxide in carbon tetrachloride, using the conditions described in J. Heterocyclic Chem.,30, 631 (1993).

So, for example, pyridine cycle in position 2 functionalitywith a bromine atom, fluorine or cyano.

This last connection, you can also get various carbonyl compounds.

Acid hydrolysis of the nitrile in the presence of sulfuric acid using the conditions described in J. Med. Chem.,34, 281-290 (1991), leads to carboxamide in the form of a dimer. Hydrolysis of the nitrile under more mild conditions allows to obtain the expected carboxamid.

Acid hydrolysis of the nitrile in the presence of 5 G. hydrochloric acid using the conditions described in J. Heterocyclic Chem.,30, 631 (1993), with the result to the corresponding carboxylic acid.

Amide can be obtained from carboxylic acids using the hydrochloride of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide as a binding agent when applying the conditions described in J. Am. Chem. Soc.,95, 875 (1973).

Various aminirovanie analogues obtained by nucleophilic substitution of the intermediate chlorinated product with amines under the action of irradiation in a microwave oven according to the conditions described in Tetrahedron,58, 1125 (2002).

Amino-similar get by removing protection from the p-methoxybenzylamine in the presence triperoxonane acid according to the conditions described in J. Chem. Soc., Perkin Trans.,1, 428-433 (2002).

This amino derivatives allows you to get other chemical functional group as an amide group, urethane group or even sulfonamidnuyu group.

Acetamide derivative is obtained by acylation of amine derivatives in the presence of acetic anhydride according to the conditions described in Tetrahedron Lett.,43, 3121 (2002). Methylcarbamate and tert-BUTYLCARBAMATE also receive according to the conditions described in J. Heterocyclic. Chem.,22, 313 (1985) and J. Org. Chem.,67, 4965 (2002). Derivatives also sulfonylureas using methylchloride according to the conditions described in J. Med. Chem.,8 , 824 (1985).

For the synthesis of compounds containing disubstituted phenyl group, were also used above conditions.

The as containing the pyridine cycle, disubstituted in position -2,6 a bromine atom, obtained using the above conditions, on the basis of 2,6-dibromo-4-(hydroxymethyl)pyridine described in Synthesis, 1665 (2000).

The products can be purified as follows.

Purification by liquid chromatography with mass spectrometry

The products can be purified by liquid chromatography with mass spectrometry (LC/MS) using Waters FractionsLynx consisting of a gradient pump, Waters model 600, the regenerative pump, Waters model 515 pump for dilute Waters Reagent Manager, autoinjector Waters model 2700, two valves Rheodyne, model LabPro, diode detector, a Waters model 996, mass spectrometer (Waters, model ZMD, and collection of fractions Gilson, model 204. The system is controlled by software, Waters FractionsLynx. The division carried out an alternate on two columns Waters Symmetry (C18, 5 microns, 19 mm x 50 mm, catalog number 186000210), and one column is in the regeneration process using a mixture of water/acetonitrile in the ratio of 95:5 (volume/volume)containing 0,07% (volume/volume) triperoxonane acid, while the other is column I is in the process of separation. Elution columns carried out using a linear gradient from 5% to 95% of acetonitrile containing 0.07 per cent (vol/vol) triperoxonane acid in water containing 0.07 per cent (vol/vol) triperoxonane acid, with a flow rate of 10 ml/min At the outlet of the separation column, a thousandth effluent separated using LC Packing Accurate, diluted with methyl alcohol with a flow rate of 0.5 ml/min and sent to the detectors in the proportion of 75% to the diode detector and the remaining 25% to the mass-spectrometer. The remainder effluent (999/1000) is directed to the collection of fractions, where the output stream until the mixture of the expected product are not determined using the software FractionsLynx. The molecular formula of the expected product are determined by the software FractionsLynx, which disables the collection of the product, when the signal is detectable mass corresponds to the ion [M+H]+and/or [M+Na]+. In some cases, depending on the results of the analytical LC/MS, when detected strong ion corresponding to [M+2H]++the value corresponding to half of the calculated molecular weight (MW/2), is determined by the FractionLynx software. Under these conditions, the collection is also turned off when the detected signal mass ion [M+2H]++and/or the signal mass ion [M+Na+H]++. The products collected in tared glass tubes. After collecting rest ritali is evaporated in a centrifugal evaporator Sovant AES 2000 or Genevac HT8 and mass of the products is determined by weighing the tubes after evaporation of the solvents.

Analysis by LC/MS carried out on the instrument Micromass model LCT associated with the apparatus of the HP 1100. The relative content of the products is determined using the diode detector HP G1315A in the range of wavelengths from 200 nm to 600 nm and the detector scattering Sedex 65. Registration of mass spectra Mass spectra is carried out in the range from 180 to 800. Data analyzed using software Micromass MassLynx. The separation is carried out on a column of Hypersil BDS C18, 3 μm (50 mm × 4.6 mm), elwira linear gradient from 5% to 90% acetonitrile containing 0.05% (volume/volume) triperoxonane acid (TFOC), in water containing 0.05% (volume/volume) TFUCK, within 3.5 minutes with a flow rate of 1 ml/min the total time of the analysis, including the period of re-equilibration of the column, is 7 minutes.

The products of examples 244-255 according to the present invention receives, as described in the experimental part and in accordance with the General route of synthesis according to the following scheme:

The products of examples 256-263 according to the present invention receive according to reaction schemes 1 and 2 below, where the numbers 1-8 correspond respectively to examples 256-263: products of examples 256-261 (or products 1-6) are obtained according to scheme 1, and the two compounds thiohydantoin examples 262 and 263 (or products 7 and 8) are obtained according to scheme 2.

SCHEME 1

Nitrosoaniline obtained by nitration of methyl ether 2-cryptomaterial acid with fuming nitric acid while controlling the temperature according to the conditions described in patent PCT Int. Appl. (2000), 564: WO 0069810.

The corresponding amine is obtained by nitrogroup reduction in the presence of SnCl2in ethanol, according to the same patent.

Isocyanate obtained by the reaction of diphosgene in the form of a solution in toluene at -20°in the usual known conditions. Isocyanate is injected into the interaction of with a quinoline derivative, obtained by known methods to obtain the desired as.

The acid is obtained by saponification using 2 n sodium hydroxide solution in tetrahydrofuran at a temperature of 60°C.

Amide produced by reaction of a combination of the desired amine, using EDCI as a binding agent (classical reaction conditions combination).

The alcohol obtained by reduction of complex ester in tetrahydrofuran in the presence of AlLiH4.

Halogenated derivatives, R = Cl and R = Br, obtained from commercially available anilines according to the same scheme of synthesis.

SCHEME 2

The following examples of the preparation explain the present invention but without limiting its scope.

Example 1

Getting trifenatate (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The syringe has a capacity of 50 ml, equipped with a Frit, suspended 2 g (1,02 mmol) of polystyrene AM RAM (Rink resin) (0.51 mmol/g) in 20 ml of dimethylformamide (DMF). After stirring for 10 minutes DMF is filtered off and replaced with 10 ml of 20%solution of piperidine in DMF. After stirring for one hour at room temperature the solution is filtered and the resin washed successively 3 times in 10 ml of DMF, 2 times 10 ml of methanol and 3 times with 10 ml DMF. To the resin add a solution of 0.94 g of Fmoc-Ala(OH) (3 mmol), 0,41 g HOBt (3 mmol) and of 0.48 ml of DIC (3 mmol) in 10 ml of DMF. The syringe is left under stirring overnight at room temperature, then the resin is washed successively 5 times with 10 ml DMF, 3 times with 10 ml of methanol and 5 times with 10 ml dichloromethane. Then in the syringe is injected 10 ml of 20%solution of piperidine in DMF. After stirring for 1 hour the solution is filtered and the resin is washed 5 times with 10 ml DMF, 2 times 10 ml of methanol, 3 times in 10 ml dichloromethane and 3 times 10 ml of tetrahydrofuran (THF). Then add to the resin solution of 0.79 g of the quinoline-4-carboxaldehyde (5.1 mmol) in 10 ml of a mixture of THF/TEOF in the ratio of 50:50. After stirring over night at room temperature the solution is filtered and the resin washed 10 times with 10 ml THF. To the resin is ATEM add 0,63 g cyanoborohydride sodium in a mixture of 1.5 ml of methanol, 3.5 ml of dichloromethane and 0.1 ml of acetic acid. The resin was incubated over night with stirring, and then, after filtration, is washed 10 times with 10 ml of dichloromethane, 3 times 10 ml of methanol and 5 times with 10 ml dichloromethane.

Parallel solution 0,563 g of 4-(trifloromethyl)-aniline (2.5 mmol) is treated with 0.25 g of triphosgene (0.83 mmol), then 0,23 ml of pyridine (2.5 mmol)at a temperature 0°and in nitrogen atmosphere. After the temperature will gradually rise to room temperature, the reaction mixture was kept under stirring for 2 hours, then again add to the mixture of 0.23 ml of pyridine in 1 ml of DMF. The resulting solution was transferred into a syringe, which is kept under stirring for 2 hours. The solution is then filtered and the resin is washed 5 times with 10 ml of dichloromethane, 3 times 10 ml of methanol and 5 times with 10 ml dichloromethane. Finally, the resin is treated with 5 ml of 95%aqueous solution triperoxonane acid in water. The mixture was incubated for 2 hours with stirring, then filtered. The resin is washed with 2 ml of methanol, then 2 ml of dichloromethane. The combined filtrates evaporated in vacuo. Thus obtain 280 mg of crude product. After purification preparative LC/MS emit 240 mg (total yield = 41%) of the desired product in the form of a solid white color.

MS(EI) mass spectrometry with ioniza what their electron impact) [M+H] +: 464.

Retention time (TR) = 3,12 min (column YMC S5 Basic; gradient acetonitrile/N2About 2-85% for 7 min).

1H-NMR (300 MHz; CDCl3) δ (ppm): to 1.59 (d, 3H), 4,11 (t, 1H), 5,01-5,55 (AB, 2H), of 7.70 (d, 1H), 7,89 (m, 1H), 7,99 (m, 3H), 8,15 (m, 2H), 8,30 (d, 1H), and 8.50 (d, 1H), which 9.22 (d, 1H).

Example 2

Getting trifenatate (S)-4-methyl-3-quinoline-4-ylmethyl-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it

Resin 3 (being 0.036 mmol), obtained according to example 1, is used for the connection.

33 mg (0.18 mmol) of Thiocarbonyldiimidazole added to a solution of 41 mg (0.18 mmol) of 4-(trifloromethyl)aniline in 3 ml of dichloromethane. The reaction mixture was incubated for 2 hours with stirring at room temperature, then added directly to the resin. After stirring for 2 hours the solution is filtered, and then the resin is washed 5 times with 2 ml of dichloromethane, 3 times 5 ml of methanol and 5 times in 2 ml of dichloromethane.

Finally, the resin is added 2 ml of 95%aqueous solution TFUK in the water. After stirring for 2 hours the mixture is filtered, the resin washed with 1 ml methanol and 1 ml of dichloromethane. The combined filtrate is heated at a temperature of 60°C for 2 hours, then concentrated in vacuo. After purification preparative LC-MS emit 1.8 mg of the target product.

MS(EI) [M+H]+: 480 pixels.

TR = 4,72 min (column YMC S5 Basic; gradient acetonitrile/N2 About 2-85% for 7 min).

Example 3

Getting trifenatate (S)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Connection get out of 0.025 mmol of resin, of 0.075 mmol of N-Fmoc-L-Ala(OH), 0.125 mmol of 4-pyridinecarboxamide and 0.0625 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 5.6 mg of the target product.

MS(EI) [M+H]+: 414; TR = 2,72 minutes

Example 4

Getting trifenatate (S)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Connection get out of 0.025 mmol of resin, of 0.075 mmol of N-Fmoc-L-Ala(OH), 0.125 mmol of 4-pyridinecarboxamide and 0.0625 mmol 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 1.3 mg of the target product.

MS(EI) [M+H]+: 382; TR = 2,83 minutes

Example 5

Getting trifenatate (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Connection get out of 0.025 mmol of resin, of 0.075 mmol of N-Fmoc-L-Ala(OH), 0.125 mmol of 4-chinainternational and 0.0625 mmol 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS receiving 0.6 mg of the target product.

MS(EI) [M+H]+: 432; TR = 3,14 minutes

Example 6

Getting trifenatate 1-quinoline-4-ylmethyl-3-(4-triptime unsulfonated)imidazolidin-2,4-dione

The compound is obtained from 4 mmol of resin, 12 mmol of N-Fmoc-Gly(OH), 20 mmol of 4-chinainternational and 10 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 1 g of the target product.

MS(EI) [M+H]+: 450; TR = 3,20 minutes

Example 7

Getting trifenatate 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.25 mmol of resin, 0.75 mmol of N-Fmoc-AIB-(OH), 1.25 mmol 4-chinainternational and of 0.625 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS obtain 22 mg of the target product.

MS(EI) [M+H]+: 478; TR = 4.26 deaths / min

Example 8

Getting trifenatate (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-D-Ala(OH), 0.20 mmol 4-chinainternational and 0.10 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 10 mg of the target product.

MS(EI) [M+H]+: 464; TR = 4,36 minutes

Example 9

Getting trifenatate (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-D-Ala(OH), 0.20 mmol 4-chinainternational is 0.10 mmol 4-(cryptomelane)aniline, in the same way, as in example 1. After purification preparative LC-MS obtain 11 mg of the target product.

MS(EI) [M+H]+: 432; TR = 4,50 minutes

Example 10

Getting trifenatate (R)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.28 mmol of resin, 0.84 mmol of N-Fmoc-D-Ala(OH), 1.4 mmol 4-pyridinecarboxamide and 0.70 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS obtain 105 mg of the target product.

MS(EI) [M+H]+: 414; TR = 2,40 minutes

Example 11

Getting trifenatate (R)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.28 mmol of resin, 0.84 mmol of N-Fmoc-D-Ala(OH), 1.4 mmol 4-pyridinecarboxamide and 0.70 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS obtain 91 mg of the target product.

MS(EI) [M+H]+: 382; TR = 2,52 minutes

Example 12

Getting trifenatate (S)-5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-L-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxamide and 0.10 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS obtain 17 mg of the target product.

MS(EI)[M+H] +: 396; TR = 4,20 minutes

Example 13

Getting trifenatate (S)-5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-L-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxamide and 0.10 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS obtain 16 mg of the target product.

MS(EI) [M+H]+: 428; TR = 4,07 minutes

Example 14

Getting trifenatate (S)-4-methyl-3-pyridin-4-ylmethyl-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-L-Ala(OH), 0.20 mmol 4-pyridinecarboxamide and 0.10 mmol of 4-(cryptomelane)aniline in the same manner as in example 2. After purification preparative LC-MS receive 1.7 mg of the target product.

MS(EI) [M+H]+: 398; TR = 4,51 minutes

Example 15

Getting trifenatate (S)-4-methyl-3-pyridin-4-ylmethyl-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-L-Ala(OH), 0.20 mmol 4-pyridinecarboxamide and 0.10 mmol of 4-(trifloromethyl)aniline in the same manner as in example 2. After purification preparative LC-MS receive 2.2 mg of the target product.

MS(EI) [M+H]+: 430; TR = 4,34 minutes

Example 16

Getting trifenatate (R)--methyl-3-(3-methylpyridin-4-ylmethyl)-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxamide and 0.10 mmol of 4-(cryptomelane)aniline in the same manner as in example 2. After purification preparative LC-MS receive 1.9 mg of the target product.

MS(EI) [M+H]+: 412; TR = 4,60 minutes

Example 17

Getting trifenatate (R)-4-methyl-3-(3-methylpyridin-4-ylmethyl)-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxamide and 0.10 mmol of 4-(trifloromethyl)aniline in the same manner as in example 2. After purification preparative LC-MS receive 4.5 mg of the target product.

MS(EI) [M+H]+: 444; TR = to 4.41 min

Example 18

Getting trifenatate (R)-5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxamide and 0.10 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS obtain 14 mg of the target product.

MS(EI) [M+H]+: 396; TR = 4,22 minutes

Example 19

Getting trifenatate (R)-5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.04 mmol of resin, 0.12 mmol NFmoc-D-Ala(OH), 0.20 mmol of 3-methyl-4-pyridinecarboxamide and 0.10 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 6.3 mg of the target product.

MS(EI) [M+H]+: 428; TR = 4,10 minutes

Example 20

Getting trifenatate (R)-4-methyl-3-quinoline-4-ylmethyl-5-thioxo-1-(4-triftormetilfullerenov)imidazolidin-2-it

The connection is obtained from 0.04 mmol of resin, 0.12 mmol of N-Fmoc-D-Ala(OH), 0.20 mmol 4-chinainternational and 0.10 mmol of 4-(cryptomelane)aniline in the same manner as in example 2. After purification preparative LC-MS receive 0.4 mg of the target product.

MS(EI) [M+H]+: 448; TR = 4,89 minutes

Example 21

Getting trifenatate (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Val(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 0.3 mg of the target product.

MS(EI) [M+H]+: 460; TR = 4,01 minutes

Example 22

Getting trifenatate (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Val(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline the mayor the same way as in example 1. After purification preparative LC-MS to receive 1 mg of the target product.

MS(EI) [M+H]+: 492; TR = 3,91 minutes

Example 23

Getting trifenatate (R)-5-benzyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Phe(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 8.9 mg of the target product.

MS(EI) [M+H]+: 508; TR = 4,11 minutes

Example 24

Getting trifenatate (R)-5-benzyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Phe(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receive 5.9 mg of the target product.

MS(EI) [M+H]+: 540; TR = 4,01 minutes

Example 25

Getting trifenatate (R)-5-benzyl-1-pyridine-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Phe(OH), 0.25 mmol of 4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 11.1 mg of the target product.

MS(EI) [+H] +: 490; TR = 3,76 minutes

Example 26

Getting trifenatate (R)-5-isobutyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Leu(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receive 5.9 mg of the target product.

MS(EI) [M+H]+: 506; TR = as 4.02 min

Example 27

Getting trifenatate (R)-5-(4-hydroxybenzyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Tyr(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS get 5.1 mg of the target product.

MS(EI) [M+H]+: 524; TR = 3,75 minutes

Example 28

Getting trifenatate (R)-5-(4-hydroxybenzyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Tyr(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receiving 1.8 mg of the target product.

MS(EI) [M+H]+: 556; TR = 3,66 minutes

Example 29

Getting trifurcata is a (R)-5-(4-hydroxybenzyl)-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Tyr(OH), 0.25 mmol of 4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receiving 0.7 mg of the target product.

MS(EI) [M+H]+: 506; TR = 3,48 minutes

Example 30

Getting trifenatate (R)-5-(1-hydroxyethyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Thr(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 4.2 mg of the target product.

MS(EI) [M+H]+: 462; TR = 3,52 minutes

Example 31

Getting trifenatate (R)-5-(1-hydroxyethyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Thr(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receive 3.4 mg of the target product.

MS(EI) [M+H]+: 494; TR = 3,43 minutes

Example 32

Getting trifenatate 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 4-hee is linkability and 0.125 mmol of 4-(cryptomelane)aniline, in the same way, as in example 1. After purification preparative LC-MS to receive 7.5 mg of the target product.

MS(EI) [M+H]+: 444; TR = 3,68 minutes

Example 33

Getting trifenatate 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS obtain 3.8 mg of the target product.

MS(EI) [M+H]+: 476; TR = 3,60 minutes

Example 34

Getting trifenatate 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 4-pyridinecarboxamide and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS receive 1.7 mg of the target product.

MS(EI) [M+H]+: 394; TR = 3,43 minutes

Example 35

Getting trifenatate 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS get 1.4 mg of the target product.

MS(EI) [M+H] : 426; TR = 3,35 minutes

Example 36

Getting trifenatate (R)-5-benzo[b]thiophene-3-ylmethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-benzothiazyl-Ala(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 5 mg of the target product.

MS(EI) [M+H]+: 596; TR = 4,12 minutes

Example 37

Getting trifenatate (R)-5-benzo[b]thiophene-3-ylmethyl-1-pyridine-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-benzothiazyl-Ala(OH), 0.25 mmol of 4-pyridinecarboxamide and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS get 1.4 mg of the target product.

MS(EI) [M+H]+: 514; TR = 3,35 minutes

Example 38

Getting trifenatate (R)-5-benzo[b]thiophene-3-ylmethyl-1-pyridine-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-benzothiazyl-Ala(OH), 0.25 mmol of 4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receive 8.5 mg of the target product.

MS(EI) [M+H]+: 546; T = 3,90 minutes

Example 39

Getting trifenatate (S)-5-pyridin-2-ylmethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-2-pyridine-Ala(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 7.5 mg of the target product.

MS(EI) [M+H]+: 509; TR = 3,47 minutes

Example 40

Getting trifenatate (S)-5-pyridin-2-ylmethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-2-pyridine-Ala(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receive 1.6 mg of the target product.

MS(EI) [M+H]+: 541; TR = 3,41 minutes

Example 41

Getting trifenatate (R)-1-(3-hydroxypyridine-4-ylmethyl)-5-methyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of N-Fmoc-D-Ala(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxamide and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 8.3 mg of the target product.

MS(EI) [M+H]+: 398; TR = 4.26 deaths / min

Example 42

Getting three is taratata 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(triptoreline)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 5.5 mg of the target product.

MS(EI) [M+H]+: 430; TR = 4,33 minutes

Example 43

Getting trifenatate 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 9.4 mg of the target product.

MS(EI) [M+H]+: 446; TR = 4,58 minutes

Example 44

Getting trifenatate 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxamide and 0.125 mmol of 4-(triptoreline)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 5.5 mg of the target product.

MS(EI) [M+H]+: 394; TR = 4,06 minutes

Example 45

Getting trifenatate 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxylic is degidi and 0.125 mmol of 4-(cryptomelane)aniline, in the same way, as in example 1. After purification preparative LC-MS gain of 13.1 mg of the target product.

MS(EI) [M+H]+: 410; TR = 4,30 minutes

Example 46

Getting trifenatate 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receive 9.6 mg of the target product.

MS(EI) [M+H]+: 442; TR = 4,18 minutes

Example 47

Getting trifenatate 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxamide and 0.125 mmol of 4-(triptoreline)aniline in the same manner as in example 1. After purification preparative LC-MS receive 6.9 mg of the target product.

MS(EI) [M+H]+: 394; TR = 4,15 minutes

Example 48

Getting trifenatate 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxamide and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS the floor is up to 9.7 mg of the target product.

MS(EI) [M+H]+: 412; TR = 4,39 minutes

Example 49

Getting trifenatate 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-AIB-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 15.2 mg of the target product.

MS(EI) [M+H]+: 444; TR = 4,30 minutes

Example 50

Getting trifenatate 4-quinoline-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 4-chinainternational and 0.125 mmol of 4-(triptoreline)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 4.1 mg of the target product.

MS(EI) [M+H]+: 428; TR = 4,24 minutes

Example 51

Getting trifenatate 4-(3-methylpyridin-4-ylmethyl)-6-(4-trifloromethyl)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 4-pyridinecarboxamide and 0.125 mmol of 4-(triptoreline)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 3 mg of the target product.

MS(EI) [M+H]+: 392; TR = 3,95 minutes

Example 52

Getting trifenatate 4-(3-methyl is iridin-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxamide and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 5 mg of the target product.

MS(EI) [M+H]+: 408; TR = 4,24 minutes

Example 53

Getting trifenatate 4-(3-methylpyridin-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 3-methyl-4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS receive 1.9 mg of the target product.

MS(EI) [M+H]+: 440; TR = 4,11 minutes

Example 54

Getting trifenatate 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-trifloromethyl)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxamide and 0.125 mmol of 4-(triptoreline)aniline in the same manner as in example 1. After purification preparative LC-MS gain of 5.5 mg of the target product.

MS(EI) [M+H]+: 394; TR = 4,04 minutes

Example 55

Getting trifenatate 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxamide and 0.125 mmol of 4-(cryptomelane)aniline in the same manner as in example 1. After purification preparative LC-MS receiving 0.7 mg of the target product.

MS(EI) [M+H]+: 410; TR = 4,34 minutes

Example 56

Getting trifenatate 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione

The connection is obtained from 0.05 mmol of resin, 0.15 mmol of Fmoc-ACPC-(OH), 0.25 mmol of 3-hydroxy-4-pyridinecarboxamide and 0.125 mmol of 4-(trifloromethyl)aniline in the same manner as in example 1. After purification preparative LC-MS to receive 2.5 mg of the target product.

MS(EI) [M+H]+: 442; TR = 4,17 minutes

Example 57

Getting 5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)dihydropyrimidine-2,4-dione

588 mg (1 mmol) of Polystyrene Wang resin (1.7 mmol/g) was washed with 2 times 5 ml of dimethylformamide, 1 times with 5 ml of dichloromethane, then treated with a solution of 0.49 g (1.5 mmol) of N-Fmoc-3-amino-2-(R,S)-methylpropionic acid, 0.24 g (3 mmol) of pyridine in 5 ml of dimethylformamide, and then immediately added 0.31 g of acid chloride 2,6-dichlorobenzoyl acid is added dropwise to control ectothermy). The reaction mixture was kept overnight under stirring at room temperature. The mixture is filtered, and then the resin is washed 1 time with 5 ml of di is malformed, 1 time with 5 ml dichloromethane and 2 times 5 ml of dimethylformamide and then treated with 5 ml of 10%solution of piperidine in dimethylformamide. The resin is then washed with 2 times 5 ml of dimethylformamide, 1 times with 5 ml of dichloromethane, 1 times using 5 ml of dimethylformamide, 4 times in 5 ml of dichloromethane, 4 times in 5 ml of methanol and dried in vacuum. 0,94 g (6 mol) of 4-Chinainternational in 16 ml of a mixture of tetrahydrofuran/TMOF in the ratio of 50:50 is added to the resin, which was incubated overnight with stirring. The resin is then washed with 3 times 5 ml of the same mixture of tetrahydrofuran/TMOF, then treated with 12 ml of 1 M solution of laborgerate sodium in tetrahydrofuran (12 mmol) in the presence of 1.2 ml of methanol and 0.12 ml of acetic acid. After stirring over night at room temperature the resin was washed 1 time with 5 ml of tetrahydrofuran (THF), 4 times in 5 ml of 30%aqueous solution of acetic acid in dimethylformamide (DMF), 1 time with 5 ml of methanol, 1 times using 5 ml of THF, 1 times using 5 ml of DMF, 1 times using 5 ml of THF, 1 times with 5 ml of methanol and dried in vacuum.

In parallel 0,121 g (0.41 mmol) of triphosgene in 1 ml of dichloromethane is added dropwise to a solution of 0,281 g (1.25 mmol) of 4-(trifloromethyl)aniline and 0.1 g (1.25 mmol) of pyridine in 2 ml of dichloromethane. After stirring for 15 minutes at room t is mperature add the same amount of pyridine, then videolooking resin. The mixture is stirred overnight, then filtered. The resin was washed 1 time with 5 ml of methanol, 1 times using 5 ml of THF, 1 times with 5 ml of methanol, 1 times using 5 ml of DMF, 1 times using 5 ml of THF, 1 times with 5 ml of methanol and 3 times with 5 ml THF and dried in vacuum. The resin is then treated with 154 mg (1 mmol) DBU in 5 ml of dichloromethane and incubated overnight with stirring. Finally, get dihydrouracil by treating the resin with 5 ml of 2%aqueous solution of acetic acid in THF. After purification preparative HPLC allocate 90 mg of the target product.

MS(EI) [M+H]+: 477;

TR = 1,83 min (gradient acetonitrile/H2O is from 20 to 100% for 5 minutes).

Example 58

(S)-5-Methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

This example describes another way of obtaining the compounds according to the above example 5.

A mixture of 0.71 g of ethyl ester of (S)-2-[(quinoline-4-ylmethyl)amino]propanoic acid and 1.42 g of 4-(triftormetilfullerenov)isocyanate in 15 ml of THF is stirred for 15 hours at room temperature in argon atmosphere. After evaporation of the solvent under reduced pressure, add 20 ml of dichloromethane. The precipitate is filtered off. The filtrate is concentrated under reduced pressure and the residue purified flash chromatography (SO 2CH2Cl2CH2Cl2/MeOH in a ratio of 95:5 by volume as the eluting means, Ar). Allocate 0,69 g (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of white powder.

[α]D= -33,1° ± 0,8° (methanol);

MS(EI) m/z = 431 M+, the peak of the molecular ion;

m/z = 143 [C10H9N]+;

1H-NMR (400 MHz, (CD3)2SO-d6) δ in ppm: to 1.42 (d, J=5.5 Hz, 3H), 4,35 (kV, J=5.5 Hz, 1H), 5,08 (d, J=17 Hz, 1H), 5.25-inch (d, J=17 Hz, 1H), 7,65 (d, J=5 Hz, 1H), the 7.65 to 7.75 (m, 1H), of 7.70 (d, J=8.5 Hz, 2H), 7,83 (t ush., J=8 Hz, 1H), 7,89 (d, J=8.5 Hz, 2H), 8,10 (l ush., J=8.5 Hz, 1H), 8,25 (l ush., J=8.5 Hz, 1H), 8,90 (d, J=5 Hz, 1H).

Ethyl ester of (S)-2-[(quinoline-4-ylmethyl)amino]propanoic acid (R-31397-073-1)

A mixture of 2 g of ethyl ester of L-alanine in the form of hydrochloride and 1.83 ml of triethylamine in 30 ml of dichloromethane is stirred at room temperature for 10 minutes. Then add 2,05 g quinoline-4-carbaldehyde. The reaction mixture was stirred at room temerature for 15 hours, then concentrated under reduced pressure. After that, add 35 ml of ethanol; the solution is cooled to a temperature of 0°then added in several portions of 0.49 g of sodium borohydride. Stirring is continued for 15 hours at room temperature. The precipitation is filtered off; the filtrate is concentrated under reduced pressure. The remainder eyes which indicate the column flash chromatography (SiO 2CH2Cl2CH2Cl2/MeOH in a ratio of 95:5 by volume as the eluting means, Ar). Obtain 0.71 g of ethyl ester of (S)-2-[(quinoline-4-ylmethyl)amino]propanoic acid as oil pink color.

MS(EI) m/z = 258 M+;

m/z = 185 [M-COOCH2CH3]+, the peak of the molecular ion;

m/z = 142 [C10H8N]+;

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,22 (t, J=7 Hz, 3H), of 1.28 (d, J=7 Hz, 3H), of 2.72 (m, 1H), 3,42 (m, 1H), 4,00-4,20 (m, 1H), 4,13 (kV, J=7 Hz, 2H), 4,27 (l ush., J=16 Hz, 1H), 7,55 (l ush., J=5 Hz, 1H), to 7.64 (DDD, J=8,5-7,5 and 1 Hz, 1H), to 7.77 (DDD, J=8,5-7,5 and 1 Hz, 1H), 8,04 (l ush., J=8.5 Hz, 1H), they were 8.22 (d ush., J=8.5 Hz, 1H), 8,86 (d, J=5 Hz, 1H).

Example 59

5,5-Dimethyl-1-quinoline-4-ylmethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione

This example describes another way of obtaining the compounds according to the above example 42.

The product is obtained according to the procedure described in example 58, using 600 mg of methyl ester of 2-methyl-2-[(quinoline-4-ylmethyl)amino]propanoic acid instead of the ethyl ester of (S)-2-[(quinoline-4-ylmethyl)amino]propanoic acid used according to example 58, and 1,114 g of 4-(trifloromethyl)isocyanate instead of 4-(triptorelin-sulfanilyl)isocyanate used according to example 58. After purification column flash chromatography (SiO2CH2Cl2as an eluting tools, Ar), the ATEM second purification column flash chromatography (SiO 2, cyclohexane/ethyl acetate in the ratio of 60:40 by volume as the eluting means, Ar) obtain 710 mg of the target product.

MS(EI) m/z = 429 M+, the peak of the molecular ion;

m/z = 414 [M-CH3]+;

m/z = 359 [M-C4H6O]+;

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,46 (C, 6N), 5,16 (s, 2H), 7,55 (l ush., J=8.5 Hz, 2H), 7,65 (d, J=5 Hz, 1H), 7,69 (d, J=8.5 Hz, 2H), of 7.70 (m, 1H), 7,83 (DDD, J=8 and 7.5 and 1.5 Hz, 1H), 8,09 (l ush., J=8.5 Hz, 1H), 8,27 (l ush., J=8.5 Hz, 1H), 8,88 (d, J=5 Hz, 1H).

Obtaining methyl ester-2-((quinoline-4-ylmethyl)amino)-propanoic acid

A mixture of 1.5 g of methyl ester hydrochloride α-aminoadamantane acid and 1.4 ml of triethylamine in 30 ml of dichloromethane is stirred at a temperature of 0°C for 20 minutes. Then add 1 g of magnesium sulfate and 1.5 g of the quinoline-4-carbaldehyde. Stirring is continued for 15 hours at room temperature, the mixture is then concentrated under reduced pressure. The residue is treated with 35 ml of methanol, the resulting solution is cooled to a temperature of 0°C. Portions add 0.4 g sodium borohydride and continue stirring for 15 hours at room temperature. The precipitation is filtered off, the filtrate is concentrated under reduced pressure. The resulting residue is purified by recrystallization from diisopropyl ether. Receive 600 mg of the target product in widebase pink color.

MS(DCI)(mass spectrometry with desorption-chemical ionization): m/z = 259 [M+H]+;

m/z = 199 [M+H-HCOOCH3]+;

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,36 (C, 6N), 2,68 (t ush., J=7 Hz, 1H), 3,69 (s, 3H), 4,11 (d, J=7 Hz, 2H), 7,60 (l ush., J=5 Hz, 1H), 7,63 (DDD, J=9-8,5 and 1 Hz, 1H), 7,76 (DDD, J=9-8,5 and 1 Hz, 1H), 8,03 (l ush., J=8.5 Hz, 1H), 8,20 (l ush., J=8.5 Hz, 1H), cent to 8.85 (d, J=5 Hz, 1H).

Example 60

5,5-Dimethyl-1-(3-chloro-6-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

The product is obtained according to the method described in example 59, from 180 mg of methyl ester of 2-methyl-2-[(3-chloro-6-methoxyquinoline-4-ylmethyl)amino]propanoic acid instead of methyl ester of 2-methyl-2-[(quinoline-4-ylmethyl)amino]propanoic acid used according to example 59, and 267 mg of 4-(trifloromethyl)isocyanate. After purification column flash chromatography (SiO2, cyclohexane/ethyl acetate in the ratio of 80:20 by volume as the eluting means, Ar) obtain 137 mg of the target product.

MS(EI) m/z = 493 M+, isotopic peak massif monochloropropane ion; m/z = 458 [M-Cl]+, the peak of the molecular ion;

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,27 (C, 6N), the 3.89 (s, 3H), at 5.27 (s, 2H), of 7.48 (DD, J=9 and 3 Hz, 1H), 7,56 (l ush., J=8.5 Hz, 2H), 7,68 (dt, J=8.5 and 2 Hz, 2H), 7,79 (d, J=3 Hz, 1H), 8,01 (d, J=9 Hz, 1H), 8,80 (s, 1H).

Obtain methyl ester of 2-methyl-2-[(3-chloro-6-metoxy the Olin-4-ylmethyl)amino]propanoic acid (R-31397-099-1)

The product is obtained according to the method described in example 59, based on 1 g of the methyl ester hydrochloride α-aminoadamantane acid, 1,25 g (3-chloro-6-methoxyquinoline)-4-carbaldehyde instead of quinoline-4-carbaldehyde used according to example 59, 0.66 g of triethylamine and 250 mg of sodium borohydride. After purification with flash chromatography (SiO2, cyclohexane/ethyl acetate in the ratio of 70:30 by volume as the eluting means, Ar) obtain 180 mg of the target product.

MS(EI) m/z = 322 M+, isotopic peak massif monochloropropane ion; m/z = 263 [M-COOCH3]+, the peak of the molecular ion, isotope peak massif monochloropropane ion; m/z = 206 [M-C5H10O2N]+, isotopic peak massif monochloropropane ion;

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1.39 in (C, 6N), 2,47 (t ush., J=7.5 Hz, 1H), 3,74 (s, 3H), 3,98 (s, 3H), Android 4.04 (d, J=7.5 Hz, 2H), 7,46 (DD, J=9 and 3 Hz, 1H), 7,66 (d, J=3 Hz, 1H), of 7.97 (d, J=9 Hz, 1H), 8,71 (s, 1H).

Receive (3-chloro-6-methoxyquinoline)-4-carbaldehyde (R-31397-097-1)

A solution of 2 g of 4-bromo-3-chloro-6-methoxyquinoline in 50 ml of THF cooled to a temperature of -78°C. Added 6.9 ml of 1.6 M solution of n-BuLi in dioxane. The solution is stirred for 2 hours at this temperature, then add 1.7 ml of DMF. The mixture is stirred at a temperature of -60°C for 2 hours and 30 minutes, and then leave the reaction medium to return to anatoy temperature. Then add 200 ml of water. The organic phase is extracted with 200 ml ethyl acetate, washed 5 times with 200 ml of water, dried over magnesium sulfate and concentrate under reduced pressure. The resulting residue is purified column flash chromatography (SiO2, cyclohexane/ethyl acetate in the ratio of 80:20 by volume as the eluting means, Ar). Obtain 1.2 g of the desired product as yellow powder.

MS(EI) m/z = 221 M+, the peak of the molecular ion, isotope peak massif monochloropropane ion;

m/z = 193 [M-CO]+, isotopic peak massif monochloropropane ion;

m/z = 150 [M-C3H3O2]+, isotopic peak massif monochloropropane ion;

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: of 3.96 (s, 3H), 7,56 (DD, J=9 and 3 Hz, 1H), 8,07 (d, J=9 Hz, 1H), they were 8.22 (d, J=3 Hz, 1H), 8,93 (s, 1H), 10,77 (s, 1H).

Getting 4-bromo-3-chloro-6-methoxyquinoline described in French patent 2816618 in example 1.

Example 61

5,5-Dimethyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution of 0,726 g of methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)amino]propanoic acid in 10 ml of tetrahydrofuran, add 0,764 g of 4-(triftormetilfullerenov)isocyanate. The reaction medium is stirred in an argon atmosphere for about 3 days at a temperature of about 20°C. the Reaction mixture formation is anywayt with ethyl acetate, washed successively with water, then saturated sodium chloride solution. The organic phase is dried over magnesium sulfate, and then concentrated under reduced pressure. Thus obtained residue is purified flash chromatography, using a column AIT, according to the standard FC-50SI filled with 50 g of silicon dioxide, and condition and elute with dichloromethane with a flow rate of 10 ml per minute. The fraction collected between 100 and 280 ml, concentrated under reduced pressure and the resulting residue treated with diethyl ether, the obtained insoluble part is filtered off. So get 700 mg of 5,5-dimethyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a white powder whose characteristics are the following:

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,43 (C, 6N), of 4.66 (s, 2H), 7,44 (l ush., J=6 Hz, 2H), 7,69 (d of t, J=8.5 and 2.5 Hz, 2H), 7,87 (l ush., J=8.5 Hz, 2H), 8,55 (DD, J=6 and 1.5 Hz, 2H).

MS(IE)(IE = EI) m/z = 395 M+, the peak of the molecular ion;

m/z = 380 (M-CH3)+;

m/z = 219 (C8H4NOSF3)+;

m/z = 92 (C6H6N)+.

Obtain methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)-amino]propanoic acid (R-31402-151-1)

To a solution of 0,945 g of methyl ester hydrochloride α-aminoadamantane acid in 28 ml of dichloroethane sequentially add the 1.04 ml of triethylamine, C is the 0,659 g of pyridine-4-carbaldehyde. The reaction mixture is stirred overnight at a temperature of about 20°C. the Mixture is purified by filtration through silica with grafted aminopropylene groups Merck Lichroprep. The filtrate is concentrated under reduced pressure and the thus obtained residue is treated with 25 ml of methanol, dobavlat 0,372 g of sodium borohydride. The reaction mixture is stirred for 48 hours at a temperature of about 20°C, then poured into a mixture of 1 n sodium hydroxide solution and ice. The resulting mixture was extracted three times with ethyl acetate. The organic phase is dried over magnesium sulfate, and then concentrated under reduced pressure. So get 0,726 g of methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)amino]propanoic acid in the form of oil, the characteristics of which are the following:

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,27 (C, 6N), 2,69 (t ush., J=5 Hz, 1H), to 3.64 (s, 3H), of 3.65 (d, J=5 Hz, 2H), 7,35 (l ush., J=6 Hz, 2H), of 8.47 (DD, J=6 and 1.5 Hz, 2H).

MS(IC)(IC = chemical ionization): m/z = 209 M+, the peak of the molecular ion;

m/z = 149 (M-C2H4O2)+.

Example 62

1-Pyridine-4-ylmethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione

To a solution 0,300 g of 3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in 6 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°, add auth 0,087 g of sodium hydride, stirring is continued at this temperature for 30 minutes, successively added 0,152 ml of triethylamine, 0,274 g of the hydrobromide of 4-(methyl bromide)of pyridine, and then, after 10 minutes, a mixture of water with ice. The reaction mixture contribute in a column with a diameter of 37 mm, filled with 50 g of silica with grafted octadecylsilyl groups Amicon, 50 μm, according to the standard, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution is performed with the mixture of water/acetonitrile (95:5, vol/vol) for 20 minutes, then linear gradient from 5% to 95% acetonitrile over 60 minutes, with a flow rate of 10 ml/min Fractions collected between 580 and 630 ml ml concentrate under reduced pressure. So get 0,220 g of 1-pyridine-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a white powder whose characteristics are the following:

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 4,16 (s, 2H)and 4.65 (s, 2H), 7,42 (l ush., J=6 Hz, 2H), to 7.64 (d ush., J=8.5 Hz, 2H), 7,87 (l ush., J=8.5 Hz, 2H), to 8.57 (d ush., J= 6 Hz, 2H).

MS(EI) m/z = 367 M+, the peak of the molecular ion;

m/z = 219 (C8H4NOSF3)+;

m/z = 92 (C6H6N)+.

The compound 3-(4-triftormetilfullerenov)imidazolidin-2,4-dione is described in U.S. patent 4496575.

Example 63

5,5-Dimethyl-1-pyridin-4-ylmethyl-3-(-trifloromethyl)-imidazolidin-2,4-dione

To a solution 0,150 g of 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione in 3 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0,042 g of sodium hydride, stirring is continued at this temperature for 30 minutes, successively added 0,094 ml of triethylamine, 0,132 g of the hydrobromide of 4-(methyl bromide)of pyridine, and then, after 10 minutes, a mixture of water with ice. The reaction mixture contribute in a column with a diameter of 27 mm, filled with 30 g of silica with grafted octadecylsilyl groups Amicon, 50 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution is performed with the mixture of water/acetonitrile (95:5, vol/vol) for 20 minutes, then linear gradient from 5% to 95% acetonitrile over 60 minutes, with a flow rate of 10 ml/min Fractions collected between 300 ml and 450 ml concentrate under reduced pressure. Thus, gain of 0.1 g of the mixture, which is again purified on a column with a diameter of 37 mm with 50 g of silica with grafted octadecylsilyl groups Amicon, 50 μm, according to the standard, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution is performed with the mixture of water/acetonitrile (95:5, vol/vol) for 20 minutes, then linear gradient from 5% to 95% acetonic the sludge for 60 minutes, with a flow rate of 10 ml/min Fractions collected between 550 ml and 750 ml concentrate under reduced pressure. So get to 0.060 g of 5,5-dimethyl-1-pyridin-4-ylmethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N)and 4.65 (s, 2H), 7,44 (l ush., J=6 Hz, 2H), 7,53 (l ush., J=8.5 Hz, 2H), to 7.64 (dt, J=8.5 and 2.5 Hz, 2H), 8,54 (l ush., J=6 Hz, 2H).

MS(EI) m/z = 379 M+, the peak of the molecular ion;

m/z = 364 (M-CH3)+;

m/z = 203 (C8H4NO2F3)+;

m/z = 92 (C6H6N)+.

Getting 5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a suspension of 8.7 g of diphosgene and 1 g of vegetable carbon black in 100 ml of toluene, at a temperature of about -20°With add, for 15 minutes, the solution was 7.08 g of 4-triphtalocyaninine in 50 ml of toluene. The mixture is stirred until it reaches a temperature of about 20°With, then refluxed for 3 hours. The mixture is cooled to a temperature of about 20°C, then filtered through celite, the filtrate add 5 g of methyl ester hydrochloride α-aminoadamantane acid, 50 ml of toluene and 10 ml of triethylamine. The thus obtained mixture is refluxed for 16 hours, then cooled to a temperature of about 20°C. the Precipitate is filtered off and the filtrate concentri the comfort under reduced pressure, the resulting residue is purified flash chromatography on a column of silica, and condition, then elute with a mixture of cyclohexane/ethyl acetate (50:50, vol/vol). The fraction containing the target product, concentrated under reduced pressure and thus obtained 3.4 g of 5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

MS(EI) m/z = 288 M+, the peak of the molecular ion;

m/z = 273 (M-CH3)+;

m/z = 203 (C8H4NO2F3)+.

1H-NMR (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), 7,49 (d, J=9 Hz, 2H), 7,55 (d, J=9 Hz, 2H), 8,63 (m, 1H).

Example 64

Getting trifenatate 3-[4-(pentaport)phenyl]-5,5-dimethyl-1-quinoline-4-immatrikulation-2,4-dione

The connection is obtained from 0.16 mmol of resin, 0.48 mmol Fmoc-AIB-(OH), 1.12 mmol 4-chinainternational and 0.4 mmol of 4-(pentaport)aniline in the same manner as in example 1. After purification by preparative chromatography LC-MS receive 5 mg of the target product.

MS(EI) [M+H]+: 472.

Example 65

Getting trifenatate 3-[4-(pentaport)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

The connection is obtained from 0.16 mmol of resin, 0.48 mmol Fmoc-AIB-(OH), 1.12 mmol 4-pyridinecarboxamide and 0.4 mmol of 4-(pentaport)aniline in the same manner as in example 1. After cleaning, the preparation is effective chromatography LC-MS receive 13.2 mg of the target product.

MS(EI) [M+H]+: 422.

Example 66

Getting trifenatate 3-[4-(pentaport)phenyl]-1-quinoline-4-immatrikulation-2,4-dione

The connection is obtained from 0.1 mmol of resin, 0.3 mmol of N-Fmoc-Gly-(OH), 0.5 mmol of 4-chinainternational and 0.25 mmol of 4-(pentaport)aniline in the same manner as in example 1. After purification by preparative chromatography LC-MS obtain 18 mg of the target product.

MS(EI) [M+H]+: 444.

Example 67

Getting trifenatate 3-[4-(pentaport)phenyl]-1-pyridin-4-immatrikulation-2,4-dione

The connection is obtained from 0.1 mmol of resin, 0.3 mmol of N-Fmoc-Gly-(OH), 0.5 mmol of 4-chinainternational and 0.25 mmol of 4-(pentaport)aniline in the same manner as in example 1. After purification by preparative chromatography LC-MS obtain 18 mg of the target product.

MS(EI) [M+H]+: 394.

Example 68

Getting trifenatate 3-[4-(pentaport)phenyl]-1-pyridin-2-immatrikulation-2,4-dione

The connection is obtained from 0.1 mmol of resin, 0.3 mmol of N-Fmoc-Gly-(OH), 0.5 mmol of 4-chinainternational and 0.25 mmol of 4-(pentaport)aniline in the same manner as in example 1. After purification by preparative chromatography LC-MS receive 9 mg of the target product.

MS(EI) [M+H]+: 394.

Example 69

Getting trifenatate 3-[4-(pentaport)phenyl]-1-pyridin-3-immatrikulation-2,4-dione

Connection receive is from 0.2 mmol of resin, 0.6 mmol of N-Fmoc-Gly-(OH), 1 mmol of 4-chinainternational and 0.5 mmol of 4-(pentaport)aniline in the same manner as in example 1. After purification by preparative chromatography LC-MS obtain 42 mg of the target product.

MS(EI) [M+H]+: 394.

6 following reaction schemes described the receipt of the products of formula (I) according to the present invention, in particular products of the following examples 70-178.

Scheme 1 describes the preparation of derivatives as with aminosalicylate in two provisions of the pyridine cycle (B2).

Scheme 1

Methods according to the scheme 1

Stage 1:

(Synthesis described for X = S, the scheme is similar to that for X = O).

1-Isocyanato-4-triftormetilfullerenov (14,27 g, 65 mmol) is dissolved in 30 ml anhydrous CH2Cl2and cooled down to a temperature of 0°C. Add 7.5 g (65 mmol) of N-ethylmorpholine and then 10 g (65 mmol) of methyl ester of 2-amino-2-methylpropionic acid. The reaction mixture is incubated for a time period of 6 hours at a temperature of 25°, washed with water and after removal of the solvent allocate 21.8 g of methyl ester of 2-methyl-2-[3-(4-triftormetilfullerenov)-ureido]propionic acid 3.

Stage 2:

30 g of methyl ester of 2-methyl-2-[3-(4-triftormetilfullerenov)ureido]propionic KIS is the notes 3 dissolved in a mixture of 225 ml of 3 N. HCl and 230 ml of dioxane and refluxed for 6 hours and after cooling to a temperature of 4°allocate product 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione as white crystals (24,14 g).

Stage 3:

5,5-Dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione 3 (1 g, 3,29 mmol) dissolved in 10 ml of DMF, add 1,36 g (3 EQ., 9,87 mmol) To a2CO3and 909 mg (3.95 mmol, 1.2 EQ.) 2-chloro-4-chloromethylpyridine and the mixture is refluxed for 20 hours. The solvent is removed in vacuum, the residue is dissolved in CH2Cl2and treated three times with activated charcoal. After removal of the solvent to obtain 1-(2-chloropyridin-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione (3.2 g; 56%).

Analytical data:

MS (LC-MS): 429,05; retention time: 2,49 minutes

NMR: 1,4 (C, 6N), 4,7 (s, 2H), 7,45 (m, 1H), and 7.6 (s, 1H), 7.7 (d, 2H), 7,9 (d, 2H), and 8.4 (m, 1H).

Getting 2-chloro-4-chloromethylpyridine

10 g of 2-Chloro-4-methylpyridine are dissolved in 30 ml of CH3CN and add a mixture of 2,2'-azobisisobutyronitrile (AIBN) (3 g) and NCS (30 g). The resulting mixture was refluxed for 4 hours. After removal of solvent the crude product is further purified by distillation (boiling point: 70°C, 20 mtorr).

Stage 4:

A General method palladium catalyzed the amination of cyclic pyridine system 1-(2-chloropyridin-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-Dion

100 mg (0.23 mmol) of 1-(2-chloropyridin-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 20 mg of Pd(OAc)2, 60 mg XANTPHOS and 300 mg Cs2CO3contribute to the reaction tube with a threaded tube which is provided with a rubber gasket, and in vitro create an atmosphere of argon. 1.5 Equivalent (0.35 mmol) of the corresponding amine or the corresponding amide is dissolved in 10 ml of toluene, the solution is transferred into the above reaction tube and the mixture is heated at a temperature of 95°C for 6-10 hours depending on the reaction-controlled LC-MS.

After filtration the solvent is removed in vacuum and the crude product is purified further by chromatography using HPLC system.

Scheme 2 describes the preparation of derivatives of urea and thiourea.

Scheme 2

Methods according to the scheme 2

Stage 1:

This stage is identical to stage 4 of scheme 1, ndimethylacetamide as a reagent in the catalytic reaction.

Analytical data for N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}ndimethylacetamide:

MS (LC-MS): 452,11; retention time: 1,82 minutes

NMR: 1,4 (C, 6N), was 2.05 (s, 3H)and 4.65 (s, 2H), and 7.1 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (m, 1H), 8,25 (m, 1H).

Stage 2:

500 mg (1.11 mmol) of N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-tripto methylsulfinylphenyl)imidazolidin-1-ylmethyl]pyridine-2-yl}ndimethylacetamide dissolved in methanol, add 1.5 mmol of sodium methylate and the mixture was refluxed for 4 hours. The solvent is removed, the residue is treated with CH2Cl2, washed with twice 10%solution of NaHCO3and water and the organic phase is evaporated. Thus emit 340 mg (75%) of 1-(2-aminopyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione.

MS (LC-MS): 410,10; retention time: 1.57 in minutes

NMR: 1,4 (C, 6N), and 4.4 (s, 2H), 6.35mm (s, 2H), 6.4 (m, 1H), 6,5 (m, 1H), 7,65 (d, 2H), 7,9 (m, 3H).

Stage 3:

General methods; all derivatives of urea and thiourea get so

100 mg of 1-(2-Aminopyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione are dissolved in 5 ml of dioxane and added 1.5 equivalent of the corresponding isocyanate or thioisocyanate. The reaction mixture is stirred at a slightly elevated temperature until the termination of the reaction, which is controlled by LC-MS. The solvent is removed, additional cleaning is performed by chromatography using HPLC system.

Scheme 3

Stage 1:

(Synthesis described for X = S scheme, similar to X = O)

5,5-Dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione (1000 mg/3,29 mmol) was dissolved in 20 ml of DMF, add Cs2CO3(3,21 g/,9 mmol) and 2,6-dichloro-4-chloromethylpyridine (774 g/3.9 mmol) and the resulting mixture is heated at a temperature of 80° C for 6 hours. The solvent is removed, the residue is dissolved in CH2Cl2and washed three times with water. After evaporation of the solvent the crude substance is purified further by chromatography using HPLC system.

Stage 2:

A General method catalyzed by palladium monolinuron 1-(2,6-dichloropyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

This stage is identical to stage 4 of scheme 1, but use only 1 equivalent of the appropriate amine or amide.

Stage 3:

A General method catalyzed by palladium bikiniready 1-(2,6-dichloropyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

This stage is identical to stage 4 of scheme 1, but in this stage using 2.2 equivalents of the corresponding amine or amide.

Scheme 4

The General procedure of alkylation of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione with aromatic or aliphatic heterocycles bearing CHLOROTHALONIL or brometalia Deputy

5,5-Dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione (100 mg/0.33 mmol) dissolved in 10 ml of DMF, add Cs2CO3(321 mg/0,99 mmol) and 0.49 mmol (1.5 equivalent) aromatic or aliphatische heterocycle, substituted soo is relevant chloromethylene or bromatology group, and the resulting mixture is heated at a temperature of 80°C for 6 hours. The solvent is removed and the resulting crude substance is purified further by chromatography using HPLC system.

Scheme 5

The syntheses of the compounds according to examples 175, 176 and 177

100 mg (0.23 mmol) of 1-(2-chloropyridin-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 20 mg of Pd(OAc)2, 60 mg XANTPHOS, 300 mg Cs2CO3, 124 mg (2 EQ.) Mo(CO)6contribute to the reaction tube with a threaded tube which is provided with a rubber gasket, and in vitro create an atmosphere of argon.

1.5 Equivalent (0.35 mmol) of the corresponding amine and 212 mg of DBU dissolved in 10 ml of toluene, the solution is transferred into the above reaction tube and the mixture is heated at a temperature of 95°C for 6-10 hours depending on the reaction controlled by using LC-MS.

After filtration the solvent is removed in vacuum and the crude product is purified further by chromatography using HPLC system.

Scheme 6

The synthesis of the compound of example 178

30 mg (0.05 mmol) of the Methyl ester of 2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}touraid)benzoic acid dissolved in 2 ml of methanol, add 01 mmol of sodium methylate and the reaction mixture stirred at room temperature overnight. After evaporation of the solvent the crude substance 5,5-dimethyl-1-[2-(4-oxo-2-thioxo-1,4-dihydro-2H-hinzelin-3-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione purified further by chromatography using HPLC system.

Example 70

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide; triptorelin

MS (LC-MS): 466,13; retention time: 1,83 minutes

NMR: of 1.05 (t, 3H), 1,40 (C, 6N), 2,35 (kV, 2H)and 4.65 (s, 2H), and 7.1 (d, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), of 8.25 (d, 1H).

The synthesis described in scheme 1.

Example 71

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)-imidazolidin-1-ylmethyl]pyridine-2-yl}isobutyramide; triptorelin

MS (LC-MS): 480,14; retention time: 1,93 minutes

NMR: 1,10 (d, 6N), 1,40 (C, 6N), a 2.75 (s, 1H)and 4.65 (s, 2H), 7,15 (d, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), of 8.25 (d, 1H).

The synthesis described in scheme 1.

Example 72

N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)-imidazolidin-1-ylmethyl]pyridine-2-yl}-3-morpholine-4-yl-propionamide; triptorelin

MS (LC-MS): 551,18; retention time: 1,54 minutes

NMR: 1,40 (C, 6N), 2,85 (m, 2H), 3,1 (m, 2H), 3,4 (m, 2H), 3,95 (m, 2H)and 4.65 (s, 2H), 7,15 (d, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), of 8.25 (d, 1H).

The synthesis described in scheme 1.

P the emer 73

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-[4-(2-hydroxyethyl)piperazine-1-yl]propionamide

MC (LC-MS): 594,22; retention time: 1,40 minutes

NMR: 1,40 (C, 6N), 2,55-3,50 (m, N)and 4.65 (s, 2H), 7,15 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), of 8.25 (d, 1H).

The synthesis described in scheme 1.

Example 74

N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-methylpiperazin-1-yl)propionamide

MC (LC-MS): 564,21; retention time: 1,41 minutes

NMR: 1,40 (C, 6N), 2,55-3,50 (m, N), a 2.75 (s, 3H)and 4.65 (s, 2H), 7,15 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), of 8.25 (d, 1H).

The synthesis described in scheme 1.

Example 75

{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)-imidazolidin-1-ylmethyl]pyridine-2-yl}amide cyclopropanecarbonyl acid

MS (LC-MS): 478,13; retention time: 1,99 minutes

NMR: 0,80 (m, 4H)and 1.15 (t, 1H), 1,40 (C, 6N)and 4.65 (s, 2H), 7,15 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), of 8.25 (d, 1H).

The synthesis described in scheme 1.

Example 76

5,5-Dimethyl-1-[2-(pyridine-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 487,13; retention time: 1,85 minutes

NMR: 1,40 (C, 6N)and 4.65 (s, 2H), and 7.3 (m, 4H), of 7.65 (d, 2H), a 7.85 (d, 2H), with 8.05 (s, 1H), 8,35 (m, 1H)

The synthesis described in scheme 1.

Example 77

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-pyrrolidin-1-ylpropionic

MS (LC-MS): 535,19; retention time: 1,52 minutes

NMR: 1,40 (C, 6N), and 1.8 (m, 2H), 2.0 (m, 2H), 2,85 (m, 2H), 3.0 a (m, 2H), 3,4 (m, 2H), 3,5 (m, 2H)and 4.65 (s, 2H), 7,2 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), 8,40 (m, 1H).

The synthesis described in scheme 1.

Example 78

5,5-Dimethyl-1-{2-[3-(4-methylpiperazin-1-yl)propylamino]pyridine-4-ylmethyl}-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 550,23; retention time: 1,52 minutes

NMR: 1,40 (C, 6N), 2,6-3,5 (m, 14N), a 2.75 (s, 3H)and 4.65 (s, 2H), 6,85 (m, 1H), 6,95 (m, 1H), 7,65 (d, 2H), 7,9 (m, 3H).

The synthesis described in scheme 1.

Example 79

5,5-Dimethyl-1-{2-[3-(4-ethylpiperazin-1-yl)propylamino]pyridine-4-ylmethyl}-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The synthesis described in scheme 1.

Example 80

1-[2-(3-Methoxybenzylamine)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 516,14; retention time: 1,90 minutes

NMR: 1,40 (C, 6N), and 3.7 (s, 3H)and 4.65 (s, 2H), and 6.6 (m, 1H), 6,9 (m, 2H), 7,15 (m, 1H), 7,2 (m, 1H), 7,25 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), with 8.05 (s, 1H).

The synthesis described in scheme 1./p>

Example 81

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-ethylpiperazin-1-yl)-propionamide

MS (LC-MS): 516,14; retention time: 1,90 minutes

NMR: to 1.15 (t, 3H), 1,40 (C, 6N), 2,5-3,7 (m, 14N)and 4.65 (s, 2H), 7,15 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), 8,25 (m, 1H).

The synthesis described in scheme 1.

Example 82

5,5-Dimethyl-1-[2-(3-methyl-2-oxopyrrolidin-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 492,14; retention time: 2,23 minutes

NMR: to 1.15 (d, 3H), 1,40 (C, 6N), to 1.60 (m, 1H), 2,30 (m, 1H), 2,70 (m, 1H), 3,80 (m, 1H), 4,0 (m, 1H)and 4.65 (s, 2H), 7,15 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,35 (m, 2H).

The synthesis described in scheme 1.

Example 83

MS (LC-MS): 495,19; retention time: 1,43 minutes

The synthesis described in scheme 1.

Example 84

5,5-Dimethyl-1-[2-(4-pyridine-2-reparation-1-yl)-pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 556,19; retention time: 1,56 minutes

The synthesis described in scheme 1.

Example 85

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)-imidazolidin-1-ylmethyl]pyridine-2-yl}-3-piperidine-1-yl-propionamide; triptorelin

MS (LC-MS): 549,22; retention time: 1,62 minutes

NMR: 1,45 (s, 6N), of 1.55 (m, 3H), of 1.80 (m, 2H), 2,80 (m, 4H), 3,3-3,5 (m, 7H)and 4.65 (s, 2H), 7,15 (m, 1H), 7,65 (d, 2H), a 7.85 (m, 2H), 8,15 (m, 1H), 8,3 (m, 1H), and 9.0 (m, 1H).

The synthesis described in scheme 1.

Example 86

1-[2-(3-Imidazol-1-ylpropionic)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 518,17; retention time: 1.57 in minutes

The synthesis described in scheme 1.

Example 87

1-[2-(4-Ethylpyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 515,16; retention time: 1,85 minutes

NMR: to 1.15 (t, 3H), 1,45 (s, 6N), and 2.7 (q, 2H), and 4.75 (s, 2H), 7,1 (ush., 2H), and 7.3 (ush., 2NM), the 7.65 (d, 2H), a 7.85 (d, 2H), of 8.25 (s, 1H), 8,45 (s, 1H).

The synthesis described in scheme 1.

Example 88

1-[2-(6-Ethylpyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 515,16; retention time: 1,95 minutes

NMR: to 1.15 (t, 3H), 1,45 (s, 6N), and 2.7 (q, 2H), and 4.75 (s, 2H), 7,1 (ush., 2H), and 7.3 (ush., 2NM). the 7.65 (d, 2H), a 7.85 (d, 2H), of 8.25 (s, 1H), 8,45 (s, 1H).

The synthesis described in scheme 1.

Example 89

5,5-Dimethyl-1-[2-(quinoline-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 537,14; retention time: 1,95 minutes

NMR: 1,45 (s, 6N), and 4.75 (s, 2H), 7,4-7,6 (m, 6N), the 7.65 (d, 2H), a 7.85 (d, 2H), 8,00 (ush., 1H), and 8.50 (ush., 2H).

The synthesis described in scheme 1.

Example 90

5,5-Dimethyl-1-[2-(4-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 501,14; retention time: 1,80 minutes

NMR: 1,45 (s, 6N), and 2.4 (s, 3H), and 4.75 (s, 2H), and 7.1 (m, 2H), 7,25 (m, 2H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,20 (ush., 1H), 8,45 (ush., 1H).

The synthesis described in scheme 1.

Example 91

5,5-Dimethyl-1-[2-(6-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 501,14; retention time: 1,85 minutes

NMR: 1,45 (s, 6N), to 2.55 (s, 3H), and 4.75 (s, 2H), and 7.1 (m, 1H), 7,25 (m, 2H), and 7.4 (s, 1H), 7,65 (d, 2H), a 7.85 (m, 3H), 8,45 (ush., 1H).

The synthesis described in scheme 1.

Example 92

1-[2-(3,5-Dichloropyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 555,05; retention time: 1,96 minutes

NMR: 1,45 (s, 6N), 4,70 (s, 2H), and 7.1 (m, 1H), 7,20 (m, 1H), 7,65 (d, 2H), a 7.85 (m, 3H), 8,30 (m, 3H).

The synthesis described in scheme 1.

Example 93

1-[2-(4,6-Dimethylpyridin-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 515,16; retention time: 2.00 in minutes

NMR: 1,45 (s)to 2.35 (s, 3H), and 2.6 (s, 3H, 6N), and 4.75 (s, 2H), 7,0 (m, 2H), 7,35 (m, 2H), of 7.70 (d, 2H), 7,9 (d, 2H), 8,40 (ush., 1H).

The synthesis described in scheme 1.

Example 94

5,5-Dimethyl-1-[2-(methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 501,14; retention time: 1,74 minutes

The synthesis described in scheme 1.

Example 95

5,5-Dimethyl-1-[2-(pyridine-4-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 487,13; retention time: 1,69 minutes

NMR: 1,45 (s), 4,70 (s, 2H), 7,15 (m, 1H), 7,25 (m, 1H), 7,65 (d, 2H), 7,9 (d, 2H), 8,10 (ush., 2H), 8,40 (s, 1H), and 8.50 (m, 2H).

The synthesis described in scheme 1.

Example 96

5,5-Dimethyl-1-[2-(pyridine-3-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 487,13; retention time: 1,69 minutes

NMR: 1,45 (s)4,60 (s, 2H), 6,95 (s, 1H), 7,05 (s, 1H), 7.7 (d, 2H), and 7.8 (m, 1H), a 7.85 (d, 2H), of 8.25 (s, 1H), 8,35 (s, 1H), 8,45 (m, 1H), and 9.4 (s, 1H).

The synthesis described in scheme 1.

Example 97

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(2-oxazepan-1-yl)propionamide

MS (LC-MS): 577,20; retention time: 2.00 m is N.

NMR: 1,45 (s, 6N), and 1.5 (m, 4H), of 1.55 (m, 2H), 2,35 (m, 2H), and 2.6 (m, 4H), 3,3 (m, 2H)and 4.65 (s, 2H), 7,15 (s, 1H), 7,65 (d, 2H), a 7.85 (d, 2H)and 8.1 (s, 1H), 8,35 (s, 1H).

The synthesis described in scheme 1.

Example 98

3-(Benzylmethylamine)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide

MS (LC-MS): 585,20; retention time: 1,73 minutes

NMR: 1,45 (s, 6N), 2,2 (s, 3H), 2.95 and (m, 2H), 3,3 (m, 1H), 4,3 (m, 1H), 4,4 (m, 1H)and 4.65 (s, 2H), 7,2 (s, 1H), 7,45 (m, 2H), 7,50 (m, 2H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,1 (m, 1H), 8,3 (m, 1H).

The synthesis described in scheme 1.

Example 99

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-2-pyrrolidin-1-ylacetamide

MS (LC-MS): 521,17; retention time: 1,68 minutes

NMR: 1,45 (s, 6N), of 1.85 (m, 2H), 2,00 (m, 2H), 3,1 (m, 2H), 4,25 (m, 2H), 4,7 (s, 2H), 7,25 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,1 (ush., 1H), and 8.3 (s, 1H)

The synthesis described in scheme 1.

Example 100

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-2-(4-pyridine-2-reparation-1-yl)ndimethylacetamide

MS (LC-MS): 613,21; retention time: 1,60 minutes

NMR: 1,45 (s, 6N), 3,3 (m ush., 4H), 4,35 (m ush., 4H)and 4.65 (s, 2H), 6,7 (m, 1H), 6,9 (m, 1H), 7,25 (s, 1H), 7,65 (m + d, 3H), a 7.85 (d, 2H), 8,15 (m, 2H), 8,35 (s, 1H).

The synthesis described in scheme 1.

Example 101

2-[(2-Dimethyl shall aminoethyl)methylamino]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}ndimethylacetamide

MS (LC-MS): 552,21; retention time: 1,52 minutes

NMR: 1,45 (s, 6N), 2,75 (C, 6N)and 4.65 (s, 2H), 7,20 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), 8.30 to (m, 1H).

The synthesis described in scheme 1.

Example 102

3-[(2-Dimethylaminoethyl)methylamino]-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide

MS (LC-MS): 566,23; retention time: 1,37 minutes

NMR: 1,45 (s, 6N), 2,75 (C, 6N), 2,8-3,4 (m ush., 8H), 7,20 (m, 1H), 7,65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), 8.30 to (m, 1H).

The synthesis described in scheme 1.

Example 103

5,5-Dimethyl-1-[2-(5-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 501,14; retention time: 1,83 minutes

NMR: 1,45 (s, 6N), and 2.3 (s, 3H), 4,7 (s, 2H), and 7.3 (m, 3H), 7.7 (d, 2H), 7,9 (d, 2H), and 8.2 (m, 1H), 8,35 (m, 1H).

The synthesis described in scheme 1.

Example 104

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl} - for 3,5-dimethoxybenzamide; triptorelin

MS (LC-MS): 574,78; retention time: 2,34 minutes

NMR: 1,45 (s, 6N), and 2.3 (s, 3H), 4,7 (s, 2H), 6,7 (s, 2H), 7,2 (m, 2H), 7,25 (m, 1H), 7.7 (d, 2H), 7,9 (d, 2H), and 8.2 (m, 1H), 8,3 (m, 1H).

The synthesis described in scheme 1.

Example 105

2-(Benzylmethylamine)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-trift methylsulfinylphenyl)imidazolidin-1-ylmethyl]pyridine-2-yl}ndimethylacetamide; triptorelin

MS (LC-MS): 574,78; retention time: 2,34 minutes

NMR: 1,45 (s, 6N), and 2.8 (C), of 4.0-4.4 (m, 4H), 4,7 (s, 2H), 7,2 (m, 1H), and 7.4 (m, 2H), 7.5 (m, 2H), 7.7 (d, 2H), 7,9 (d, 2H), 8,1 (m, 1H), 8.30 to (m, 1H).

The synthesis described in scheme 1.

Example 106

5,5-Dimethyl-1-[2-(pyrazin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 488,12; retention time: 1,63 minutes

NMR: 1,45 (s, 6N), 4,7 (s, 2H), and 7.1 (m, 1H), 7,6 (m, 1H), 7,65 (d, 2H), 7,9 (d, 2H), and 8.2 (s, 1H), 8,3 (m, 2H), and 9.0 (s, 1H).

The synthesis described in scheme 1.

Example 107

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-2-phenylbutyramide; triptorelin

MS (LC-MS): 566,18; retention time: 2,43 minutes

NMR: 0,7 (t, 3H), 1,4 (C, 6N), and 1.7 (m, 1H), 2.05 is (m, 1H), 4,6 (s, 2H), and 7.1 (s, 1H), 7,25 (m, 1H), and 7.3 (m, 1H), and 7.4 (m, 2H), 7,65 (d, 2H), a 7.85 (d,2H), 8,15 (s, 1H), 8,25 (m, 1H).

The synthesis described in scheme 1.

Example 108

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3-methylpiperidin-1-yl)propionamide; triptorelin

MS (LC-MS): 563,22; retention time: 1,62 minutes

The synthesis described in scheme 1.

Example 109

1-[2-(4-Methoxybenzylamine)pyridine-4-ylmethyl]-5,5-dimethyl-3-(-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 517,1; retention time: 1,74 minutes

NMR: 1,4 (C, 6N), and 4.6 (s, 2H), 6,85 (ush., 1H), 7,0 (m, 1H), and 7.4 (m, 2H), and 7.6 (d, 2H), 7,9 (d, 2H), of 8.95 (s, 1H).

The synthesis described in scheme 1.

Example 110

5,5-Dimethyl-1-[2-(2-oxopyrrolidin-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 478,13; retention time: 1,83 minutes

The synthesis described in scheme 1.

Example 111

{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)-imidazolidin-1-ylmethyl]pyridine-2-yl}amide pyrazin-2-carboxylic acid; triptorelin

MS (LC-MS): 516,12; retention time: 2,42 minutes

NMR: 1,4 (C, 6N), 4,7 (s, 2H), and 7.3 (m, 1H), 7,65 (d, 2H), 7,95 (d, 2H), and 8.3 (s, 1H), and 8.4 (s, 1H), and 8.7 (s, 1H), and 9.0 (s, 1H), and 9.4 (s, 1H).

The synthesis described in scheme 1.

Example 112

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-2,2-dimethylpropanamide; triptorelin

MS (LC-MS): 494,16; retention time: 2,48 minutes

NMR: 1,2 (s, N), 1,4 (C, 6N), 4,7 (s, 2H), 7,2 (m, 1H), 7,65 (d, 2H), of 7.90 (d, 2H)and 8.1 (s, 1H), and 8.3 (s, 1H).

The synthesis described in scheme 1.

Example 113

{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)-imidazolidin-1-ylmethyl]pyridine-2-yl}amide thiophene-2-carboxylic acid; trifurcata the

MS (LC-MS): 520,09; retention time: 2,14 minutes

NMR: 1,4 (C, 6N), 4,7 (s, 2H), 7,2 (m, 2H), 7,65 (d, 2H), and 7.8 (m, 3H), and 8.2 (s, 1H), of 8.25 (s, 1H), and 8.4 (m, 1H).

The synthesis described in scheme 1.

Example 114

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-4-methylbenzamide; triptorelin

MS (LC-MS): 528,16; retention time: 2,23 minutes

NMR: 1,4 (C, 6N), 4,7 (s, 2H), 7,2 (m, 1H), and 7.3 (d, 2H), 7.7 (d, 2H), a 7.85 (d, 2H), 7,95 (d, 2H), and 8.2 (s, 1H), and 8.3 (s, 1H).

The synthesis described in scheme 1.

Example 115

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3,5-dimethylpiperidin-1-yl)propionamide; triptorelin

MS (LC-MS): 577,23; retention time: 1,72 minutes

The synthesis described in scheme 1.

Example 116

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-pyridine-2-reparation-1-yl)propionamide; triptorelin

MS (LC-MS): 627,22; retention time: 1.50 in minutes

NMR: 1,4 (C, 6N), 2,9 (m, 2H), 3,1 (m, 2H), 3,4 (m, 2H), 3,6 (m, 2H), 4,4 (m, 2H)and 4.65 (s, 2H), 6,7 (m, 1H), 6,95 (d, 1H), 7,2 (m, 1H), 7.7 (d, 2H), 7,9 (d, 2H), 8,15 (m, 2H), 8,3 (m, 1H).

The synthesis described in scheme 1.

Example 117

5,5-Dimethyl-1-[2-(5-triptorelin-2-ylamino)pyridine-4-and the methyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 555,51; retention time: 1,78 minutes

The synthesis described in scheme 1.

Example 118

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-methoxybenzamide; triptorelin

MS (LC-MS): 544,14; retention time: 2,15 minutes

The synthesis described in scheme 1.

Example 119

1-(3,5-Dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}urea

MS (LC-MS): 597,06; retention time: 2,15 minutes

The synthesis described in scheme 2.

Example 120

Methyl ester 3-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}touraid)benzoic acid

MS (LC-MS): 603,12; retention time: 2,81 minutes

The synthesis described in scheme 2.

Example 121

1-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-prilocaine

MS (LC-MS): 529,14; retention time: 2,33 minutes

NMR: 1,50 (C, 6N)and 4.65 (s, 1H), 7,0 (m, 2H), 7,30 (m, 2H), 7.5 (m, 3H), of 7.65 (d, 2H), a 7.85 (d, 2H), of 8.25 (d, 1H), and 9.4 (s, 1H).

The synthesis described in scheme 2.

Example 122

1-(2,4-Dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-Tr is formatterconverter)imidazolidin-1-ylmethyl]pyridine-2-yl}urea

MS (LC-MS): 597,06; retention time: 3,00 minutes

The synthesis described in scheme 2.

Example 123

1-(3-Chlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}thiourea

MS (LC-MS): 579,08; retention time: 3,05 minutes

The synthesis described in scheme 2.

Example 124

Methyl ester of 2-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}touraid)benzoic acid

MS (LC-MS): 603,12; retention time: 2,85 minutes

The synthesis described in scheme 2.

Example 125

3,5-Diacetoxy-2-acetoxymethyl-6-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}touraid)tetrahydropyran-4-silt ether acetic acid

MS (LC-MS): 799,18; retention time: 2,60 minutes

The synthesis described in scheme 2.

Example 126

1-(4-Dimethylaminophenyl)-3-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}thiourea

MS (LC-MS): 588,16; retention time: 1,99 minutes

NMR: 1,4 (C, 6N), 2,9 (C, 6N), 4,7 (s, 2H), 6,7 (d, 2H), and 7.1 (m, 1H), 7,25 (s, 1H), and 7.4 (d, 2H), 7.7 (d, 2H), 7,9 (d, 2H), 8,25 (m, 1H).

The synthesis describes the scheme and 2

Example 127

1-(2,4-Acid)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}urea

MS (LC-MS): 589,60; retention time: 1,98 minutes

The synthesis described in scheme 2.

Example 128

3-(3-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}touraid)benzoic acid

MS (LC-MS): 589,11; retention time: 2,30 minutes

The synthesis described in scheme 2.

Example 129

1-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)-imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(2-methoxyphenyl)urea

MS (LC-MS): 559,15; retention time: 1,88 minutes

The synthesis described in scheme 2.

Example 130

1-(2-Aminopyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolin-2,4-dione

MS (LC-MS): 410,10; retention time: 1.57 in minutes

NMR: 1,4 (C, 6N), and 4.6 (s, 2H), 6,9 (d, 1H), 7,0 (s, 1H), 7.7 (d, 2H), a 7.85 (d, 2H), 7,95 (d, 1H), 8.0 a (ush., 1H).

The synthesis described in scheme 2.

Example 131

1-(2,6-Dichloropyridine-4-yl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}urea

MS (LC-MS): 599,42; retention time: 2,73 minutes

NMR: 1,4 (C, 6N)and 4.65 (s, 2H), 7.5 (m, 1H), the 7.65 (d, 2H), a 7.85 (d, 2H), 8,15 (s, 1H), 8,25 (m, 1H).

The synthesis described in scheme 2.

Example 132

1-(2,6-Dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}urea

MS (LC-MS): 597,06; retention time: 2,44 minutes

The synthesis described in scheme 2.

Example 133

1-(2,3-Dichlorophenyl)-3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-urea

MS (LC-MS): 597,06; retention time: 2,08 minutes

The synthesis described in scheme 2.

Example 134

1-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-pyridin-3-ultimatemenu

MS (LC-MS): 546,11; retention time: 1,89 minutes

The synthesis described in scheme 2.

Example 135

1-[2-Chloro-6-(4-methylthiazole-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 541,06; retention time: 2,49 minutes

The synthesis is described in scheme 3.

Example 136

N-{6-Chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-2-phenylbutyramide

MS (LC-MS): 541,06; retention time: 2,49 m is N.

The synthesis is described in scheme 3.

Example 137

N-{6-Acetylamino-4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}ndimethylacetamide

MS (LC-MS): 509,13; retention time: 1,73 minutes

The synthesis is described in scheme 3.

Example 138

1-[2-Chloro-6-(4-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 535,11; retention time: 1,90 minutes

The synthesis is described in scheme 3.

Example 139

1-[2,6-bis(3-methoxybenzylamine)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 621,22; retention time: 1,95 minutes

The synthesis is described in scheme 3.

Example 140

1-[2,6-bis(2,4-Dimethoxyaniline)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 681,24; retention time: 1,83 minutes

The synthesis is described in scheme 3.

Example 141

1-[2,6-bis(4-methoxybenzylamine)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 621,22; retention time: 1,63 minutes

The synthesis described in schemes is 3.

Example 142

N-{4-[5,5-Dimethyl-2,4-dioxo-3-(4-trifloromethyl)-imidazolidin-1-ylmethyl]-6-astroteilchenphysik-2-yl}-isobutyramide; triptorelin

MS (LC-MS): 549,22; retention time: 1,83 minutes

The synthesis is described in scheme 3.

Example 143

1-[2-Chloro-6-(pyridine-4-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 563,19; retention time: 2,61 minutes

The synthesis is described in scheme 3.

Example 144

1-[2-Chloro-6-(pyridine-4-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 521,09; retention time: 1,91 minutes

The synthesis is described in scheme 3.

Example 145

N-{6-Chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide

MS (LC-MS): 500,09; retention time: 2,46 minutes

The synthesis is described in scheme 3.

Example 146

N-{6-Chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}ndimethylacetamide

MS (LC-MS): 486,90; retention time: 2,15 minutes

The synthesis is described in scheme 3.

Example 147

1-[2-Chloro-6-(pyridine-3-the laminitis)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 505,11; retention time: 2,27 minutes

The synthesis is described in scheme 3.

Example 148

{6-Chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide cyclopropanecarbonyl acid

MS (LC-MS): 512,09; retention time: 2,32 minutes

The synthesis is described in scheme 3.

Example 149

N-{6-Chloro-4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}isobutyramide

MS (LC-MS): 514,11; retention time: 1,63 minutes

The synthesis is described in scheme 3.

Example 150

1-[2,6-bis(pyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione; triptorelin

MS (LC-MS): 563,15; retention time: 1,70 minutes

The synthesis is described in scheme 3.

Example 151

1-[2-Chloro-6-(pyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 521,09; retention time: 1,78 minutes

The synthesis is described in scheme 3.

Example 152

5,5-Dimethyl-1-(5-phenyl-[1,2,4]oxadiazol-3-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 462,10; retention time: 2,77 minutes

The synthesis is described in scheme 4.

Example 153

1-(2-Imidazol-1-retil)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 398,10; retention time: 1,49 minutes

The synthesis is described in scheme 4.

Example 154

1-[2-(4-Chlorophenyl)oxazol-5-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 495,06; retention time: 2,99 minutes

The synthesis is described in scheme 4.

Example 155

Getting a 1-isoquinoline-5-yl-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

500 mg (2.4 mmol) of 2-(isoquinoline-5-ylamino)-2-methylpropionitrile, 1.6 mg (0,013 mmol) of benzoic acid and 526 mg (2.4 mmol) of 4-(triptoreline)phenylisocyanate in 4 ml of chlorobenzene is refluxed for 2 days. The resulting mixture was filtered and the filtrate is evaporated to dryness. The intermediate amine is separated by preparative chromatography HPLC (RP 18, acetonitrile, water, 0.01% TFUC). 60 mg of the obtained product was stirred with 1 N. hydrochloric acid for 1 hour at a temperature of 40°C. the Solvent is evaporated and the residue treated with sodium hydrogen carbonate solution and extracted with ethyl acetate. The combined organic phases are dried and the remaining after viparivartate purified flash chromatography (SiO 2, dichloromethane:methanol = 98:2)to give 38 mg of the target product.

(M+N)+= 432; LC-MS: retention time: 1,245 minutes

Example 156

5,5-Dimethyl-1-(5-phenyloxazol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 461,10; retention time: 2,63 minutes

The synthesis is described in scheme 4.

Example 157

5,5-Dimethyl-1-(1-methylpiperidin-3-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 415,15; retention time: 1,63 minutes

The synthesis is described in scheme 4.

Example 158

5,5-Dimethyl-1-(1-methylpiperidin-3-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

MS (LC-MS): 499,18; retention time: 1.39 in minutes

The synthesis is described in scheme 4.

Example 159

1-[2-(4-Chlorophenyl)thiazol-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 511,04; retention time: 3,12 minutes

The synthesis is described in scheme 4.

Example 160

5,5-Dimethyl-1-(1-methyl-1H-imidazol-2-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 398,10; retention time: 1,53 minutes

The synthesis is described in scheme 4.

Example 161

1-(7-Methoxy-2-oxo-2H-who Romaine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 492,48; retention time: 1,84 minutes

The synthesis is described in scheme 4.

Example 162

5,5-Dimethyl-1-(5-methylisoxazol-3-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 500,09; retention time: 2,52 minutes

The synthesis is described in scheme 4.

Example 163

1-[5-(4-Methoxyphenyl)-[1,2,4]oxadiazol-3-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 492,11; retention time: 1,87 minutes

The synthesis is described in scheme 4.

Example 164

1-[5-(4-Methoxyphenyl)-[1,2,4]oxadiazol-3-ylmethyl]-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione

MS (LC-MS): 476,13; retention time: 2,03 minutes

The synthesis is described in scheme 4.

Example 165

Methyl ester 5-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]furan-2-carboxylic acid

MS (LC-MS): 442,42; retention time: 1,74 minutes

The synthesis is described in scheme 4.

Example 166

1-(1-Benzyl-1H-imidazol-2-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 474,13; retention time: 2,02 minutes

Synthesis of opisyvaet is camping in figure 4.

Example 167

1-(4-Dimethylaminopyridine-2-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 439,46; retention time: 1,91 minutes

The synthesis is described in scheme 4.

Example 168

1-[1-(4-Methoxybenzyl)-1H-imidazol-2-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 504,14; retention time: 2,24 minutes

The synthesis is described in scheme 4.

Example 169

5,5-Dimethyl-1-[2-(1-methylpyrrolidine-2-yl)ethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 415,15; retention time: 1,66 minutes

The synthesis is described in scheme 4.

Example 170

5,5-Dimethyl-1-(2-morpholine-4-retil)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 417,13; retention time: 1,62 minutes

The synthesis is described in scheme 4.

Example 171

1-[5-(2-Methoxyphenyl)-[1,2,4]oxadiazol-3-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 492,11; retention time: 2,67 minutes

The synthesis is described in scheme 4.

Example 172

5,5-Dimethyl-1-(5-methylisoxazol-3-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

MS (LC-MS): 383,33; retention time: 1,95 minutes

The synthesis is described in scheme 4.

Example 173

1-(5-tert-Butyl-[1,2,4]oxadiazol-3-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

MS (LC-MS): 442,16; retention time: 2,64 minutes

The synthesis is described in scheme 4.

Example 174

4-Methylbenzylamine 4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-carboxylic acid; triptorelin

MS (LC-MS): 542,16; retention time: 2,80 minutes

The synthesis is described in scheme 5.

Example 175

(2-p-Triletal)amide 4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-carboxylic acid

MS (LC-MS): 556,18; retention time: 2,31 minutes

The synthesis is described in scheme 5.

Example 176

3,4-Dimethoxybenzene 4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-carboxylic acid

MC (LC-MS): 588,16; retention time: 1,58 minutes

The synthesis is described in scheme 5.

Example 177

Benzylamine 4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-carboxylic acid

<> MC (LC-MS): 528,14; retention time: 1.77 in minutes

The synthesis is described in scheme 5.

Example 178

5,5-Dimethyl-1-[2-(4-oxo-2-thioxo-1,4-dihydro-2H-hinzelin-3-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione

MS (LC-MS): 571,10; retention time: 2,3 minutes

The synthesis is described in scheme 6.

On the following two reaction schemes described the synthesis of products of formula (I) according to the present invention, in particular of products below examples 179-200.

Bis-(4-Amino-2-chlorophenyl)disulfide

with 76.8 g (0.4 mol) of 1,2-Dichloro-4-nitrobenzene, suspended in 120 ml of water, heated to a temperature of 90°and treated With a solution of 62.4 g (0.8 mol) of sodium sulfide and 12.8 g (0.4 mol) of sulfur in 200 ml of water.

After boiling under reflux the mixture for 5 hours bubbled through a solution of 6 g of carbon dioxide, then uniform air flow. The pH value was adjusted to 5.5, the mixture is cooled to room temperature and precipitated precipitate was separated by filtration.

The crude material is recrystallized from isopropanol, obtaining 45 g (71%) of the target product.

(M+N)+= 318

LC-MS: retention time = 1,526 minutes

Bis[(2-Chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyridin-4-immatrikulation-1-yl)]phenoldisulfonic

A solution of 13.7 g (69,5 mmol of diphosgene in 100 ml of toluene cooled to a temperature of -20° C and treated with a solution of 5.0 g (15.8 mmol) of bis(4-amino-2-chlorophenyl)disulfide. The resulting mixture was stirred for 30 minutes at room temperature, refluxed for 1 hour and then evaporated to dryness.

2,53 g (approximately 6,86 mmol) of the substance is dissolved in THF and treated with 2.0 g (9.5 mmol) of the methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)amino]propionic acid. The mixture is stirred for 3 hours at room temperature, evaporated to dryness and the remaining solid is purified flash chromatography (SiO2, dichloromethane:methanol = 97:3)to give 1.8 g (37%) of the target product.

(M+N)+= 722.

LC-MS: retention time = 1,176 minutes

Example 179

Obtaining 3-(4-tert-butylsulfonyl-3-chlorophenyl)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione of triptoreline

200 mg (0.28 mol) of bis[(2-Chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyridin-4-immatrikulation-1-yl)]phenoldisulfonic dissolved in 10 ml of methanol and treated with 22 mg (0,56 mmol) sodium borohydride. After stirring for 30 minutes at room temperature the mixture is evaporated to dryness. The residue is dissolved in 10 ml of 75%sulfuric acid and added to 20 ml of 75%sulfuric acid, which is saturated with isobutylene. The mixture is stirred for 20 minutes at room temperature and then gently add to the chilled R is the target of sodium hydroxide in water. The aqueous alkaline phase is extracted three times with ethyl acetate, the combined organic phases are dried over sodium sulfate and remaining after evaporation of the substance is filtered through silica gel (dichloromethane:methanol = 95:5). The resulting crude product is purified by chromatography HPLC (RP 18, acetonitrile, water, 0.01% TFUC)to give 120 mg (81%) of the target product.

(M+N)+= 418.

LC-MS: retention time = 1,249 minutes

A General method 1A

Obtaining 3-(3-chloro-4-alkylsulfanyl)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-diones

445 mg (of 0.62 mol) of bis[(2-Chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyridin-4-immatrikulation-1-yl)]phenoldisulfonic dissolved in 15 ml of methanol and treated with 49 mg (1,24 mmol) sodium borohydride. After stirring for 30 minutes at room temperature add to 1.24 mmol of the corresponding alkylhalogenide and the resulting mixture is refluxed for 1 hour. The solvent is removed by evaporation and the remaining crude substance is purified by preparative chromatography HPLC (RP 18, acetonitrile, water, 0.01% TFUC).

Example 180

Obtaining 3-(3-chloro-4-isopropylaniline)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Synthesized according to the General method 1A.

M+N+= 404.

LC-MS: retention time = 1,196 minutes

Example 181

Obtaining 3-(3-chloro-4-image is tranformer)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione of triptoreline

Receive according to the General method 1A.

M+N+= 418.

LC-MS: retention time = 1,272 minutes

Example 182

Obtaining 3-(3-chloro-4-methylsulfinylphenyl)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 1A.

M+N+= 376.

LC-MS: retention time = 1,054 minutes

Example 183

Getting trifenatate 3-[3-chloro-4-(3-methoxypropionitrile)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 1A.

M+N+= 434.

LC-MS: retention time = 1,096 minutes

Example 184

Getting trifenatate 3-[3-chloro-4-(2-morpholine-4-reticular)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 1A.

M+N+= 475.

LC-MS: retention time = 0,792 minutes

Example 185

Getting trifenatate 3-{3-chloro-4-[2-(1-methylpyrrolidine-2-yl)ethylsulfanyl]phenyl}-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 1A.

M+N+= 473.

LC-MS: retention time = 0,865 minutes

Example 186

Getting trifenatate 3-{3-chloro-4-[3-(4-methylpiperazin-1-yl)propylsulfonyl]phenyl}-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 1A.

M+N+= 502.

LC-MS: retention time = 0,795 minutes

Getting trifenatate 3-[3-chloro-4-(3-hydroxypropanesulfonic)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 1A.

M+N+= 420.

LC-MS: retention time = 0,968 minutes

Example 188

Getting trifenatate 3-[3-chloro-4-(2-hydroxyarylalkyl)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 1A.

M+N+= 406.

LC-MS: retention time = 0,921 minutes

Example 189

Getting trifenatate [2-chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyridin-4-immatrikulation-1-yl)phenylsulfanyl]acetonitrile

Receive according to the General method 1A.

M+N+= 401.

LC-MS: retention time = 0,999 minutes

3-Nitro-4-cryptomaterial

20 g (112,9 mmol) 4-Triphtalocyaninine dissolved in 50 ml of concentrated sulfuric acid at a temperature of 0-5°C, treated with 30 ml of a mixture of sulfuric acid and nitric acid in the ratio of 4:1. The mixture is stirred for 5 hours at a temperature of 0°and then poured into a mixture of ice water and alkalinized with 200 ml of concentrated ammonium hydroxide solution. Extraction with ethyl acetate, drying over sodium sulfate, evaporation to dryness and recrystallization from a mixture of ethyl acetate and heptane yield 15.5 g (63%) of the target product.

M+N+= 223.

LC-MS: retention time = 1,378 minutes

Example 190

Getting trifenatate 5,5-dimethyl-3-(3-nitro-4-trifloromethyl)-1-pyridin-4-immatrikulation-2,4-dione

of 2.27 g (11.5 mmol) of diphosgene in 1,2-dichloroethane at a temperature of -20°added to a solution of 1.0 g (4.5 mmol) of 3-nitro-4-triphtalocyaninine in 20 ml of 1,2-dichloroethane. The mixture is stirred for 1 hour allowing the temperature to return to room temperature and then heated at a temperature of 50°C for 2 hours. After standing overnight the solvent is evaporated, the residue is treated with anhydrous tetrahydrofuran and then treated with 937 mg (4.5 mmol) of methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)amino]propionic acid. The mixture is stirred for 2 hours at room temperature and for 1 hour at a temperature of 40°With, then is evaporated to dryness and the remaining residue purified (RP 18, acetonitrile, water, 0.01% TFOC), getting to 1.15 g (61%) of the target product.

M+N+= 425.

LC-MS: retention time = 1,324 minutes

Example 191

Obtaining 3-(3-amino-4-trifloromethyl)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

9,63 g (22.7 mmol) of Triptoreline 5,5-dimethyl-3-(3-nitro-4-trifloromethyl)-1-pyridin-4-immatrikulation-2,4-dione is dissolved in policecontributing hydrochloric acid, heated to temperature is ture boiling under reflux and treated with 30 g of zinc powder. After 1.5 hours the mixture is cooled, filtered and extracted two times with methyl tert-butyl ether. The aqueous phase is alkalinized with 6 n sodium hydroxide solution, extracted with methyl tert-butyl ether and the combined organic phases are dried over sodium sulfate. Evaporation of the solvent leads to obtain 5.0 g (56%) of the target product.

M+N+= 395.

LC-MS: retention time = 0,948 minutes

Example 192

Getting 5,5-dimethyl-1-pyridin-4-ylmethyl-3-[4-(2,2,2-triptoreline)phenyl]imidazolidin-2,4-dione

To 688 mg (3.6 mmol) of 2,2,2-cryptgetuserkey in 30 ml of dichloromethane, at a temperature of 0°add 356 mg (3.6 mmol) of triethylamine and a solution of 356 mg (1.2 mmol) of triphosgene in 30 ml of dichloromethane. The mixture is stirred throughout the night when the temperature is raised to room temperature. After that, the solvent is evaporated, the residue is treated with 15 ml of THF and then treated with 100 mg (0.48 mmol) of the methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)amino]propionic acid and to 48.5 mg (0.48 mmol) of triethylamine. The mixture is stirred for 4 hours at room temperature and 1 hour at a temperature of 50°With, then is evaporated to dryness and the remaining residue is purified by preparative chromatography HPLC (RP 18, acetonitrile, water, 0.01% TFOC), receiving 67 g (36%) of the target product.

M+N+= 394.

LC-MS: retention time = 1,032 minutes

Example 193

Obtaining 3-(8-chloro-3,4,4-trimethylchitosan-6-yl)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

200 mg (0.28 mol) of bis[(2-Chloro-4-(4,4-dimethyl-2,5-dioxo-3-pyridin-4-immatrikulation-1-yl)]phenoldisulfonic dissolved in 10 ml of methanol and treated with 22 mg (0,56 mmol) sodium borohydride. After stirring for 30 minutes at room temperature the mixture is evaporated to dryness. The residue is dissolved in 10 ml of 75%sulfuric acid and added to 20 ml of 75%sulfuric acid, which is saturated with isobutylene. The mixture is stirred for 30 minutes at a temperature of 40°yet is bubbled through a solution of uniform air flow. After standing overnight the mixture is carefully added to a cooled solution of sodium hydroxide in water. The aqueous alkaline phase is extracted three times with ethyl acetate, the combined organic phases are dried over sodium sulfate and remaining after evaporation of the substance is filtered through silica gel (dichloromethane:methanol = 95:5). The resulting crude product was then purified by preparative chromatography HPLC (RP 18, acetonitrile, water, 0.01% TFUC)to give 70 mg (56%) of the target product.

M+N+= 444.

LC-MS: retention time = 1,240 minutes

Example 194

Getting trifenatate 1-(2-chlorothiazole-5-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

20 mg (of 0.65 mmol) of 5,5-Dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 115 mg (0.82 mmol) of potassium carbonate and 276 mg (1,64 mmol) 2-chloro-5-chloromethylthiazole dissolved in 2 ml DMF and stirred at room temperature for 2 days. The mixture was poured into water, extracted three times with ethyl acetate, the combined organic phases are dried over sodium sulfate and remaining after evaporation of the substance is purified by preparative chromatography HPLC (RP 18, acetonitrile, water, 0.01% TFOC), leading to obtain 143 mg (50%) of the target product.

M+N+= 436.

LC-MS: retention time = 1,784 minutes

Example 195

Obtain 3-[3-chloro-4-(propane-2-sulfonyl)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

40 mg (0.1 mmol) 3-(3-Chloro-4-isopropylaniline)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione are dissolved in 2 ml dichloromethane and treated with a solution of 37 mg (0.15 mmol) of m-chlormadinone acid in 2 ml of dichloromethane. The reaction is monitored by thin-layer chromatography (TLC) and stop when sulfoxide and sulfon are formed in equal amounts. The mixture is evaporated to dryness and the residue purified flash chromatography (SiO2, dichloromethane:methanol = 98:2), leading to the 4 mg 3-[3-chloro-4-(propane-2-sulfonyl)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione and 7 mg of 3-[3-chloro-4-(propane-2-sulfinil)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione.

M+N+= 436.

LC-MS: time is of derivare = 0,970 minutes

Example 196

Obtain 3-[3-chloro-4-(propane-2-sulfinil)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive, as described above.

M+N+= 420.

LC-MS: retention time = 0,932 minutes

2-(Isoquinoline-5-ylamino)-2-methylpropionitrile

5.0 g (to 34.7 mmol) 5-Aminoisoquinoline, 5,1 ml (69,4 mmol) of acetone and 945 mg (6,94 mmol) of zinc chloride dissolved in 100 ml of acetonitrile and at a temperature of 0°is treated with 6.9 g (69,4 mmol) trimethylsilylacetamide. The mixture is refluxed for 3 hours, then the solvent is evaporated and the residue is treated with 200 ml of a solution of sodium bicarbonate and extracted 3 times with ethyl acetate. The combined organic phases are dried and the remaining after evaporation the residue is purified flash chromatography (SiO2, dichloromethane:methanol = 95:5), leading to obtain 6.0 g (82%) of the target product.

M+N+= 212.

LC-MS: retention time = 0,696 minutes

General method 2

Synthesis of alkylchlorosilanes

1.1 g (8 mmol) of 4-Aminothiophenol and 896 mg (8 mmol) of potassium tert-butylate are dissolved in 10 ml DMF and stirred for 45 minutes in an argon atmosphere. Then add 8,8 mmol of the corresponding allylbromide, the mixture is stirred for 3 hours at room temperature, poured into water and extracted with ethyl acetate. The joint organization of the definition phase is dried and evaporated. The residual product is essentially pure and can be used without additional purification.

4-(3-Methoxypropionitrile)phenylamine

Receive according to the General method 2.

M+N+= 197.

LC-MS: retention time = 0,777 minutes

4-Isopropylcyclopentadienyl

Receive according to the General method 2.

M+N+= 266.

LC-MS: retention time = 0,173 minutes

4-[3-(4-Methylpiperazin-1-yl)propylsulfonyl]phenylamine

Receive according to the General method 2.

M+N+= 168.

LC-MS: retention time = 0,894 minutes

General method 3

Obtaining 3-(3-chloro-4-alkylsulfanyl)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-diones

371 mg (2.3 mmol) of Carbonyldiimidazole, 41 mg (0.5 mmol) of imidazole and 1.9 mmol of the corresponding alkylsulfonyl dissolved at a temperature of 0°With, in 10 ml THF and stirred for 1 hour. Then add 280 mg (1.35 mmol) of the methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)amino]propionic acid, dissolved in 5 ml of THF, and the mixture is refluxed for 5 hours. After that, the solvent is evaporated and the remaining after evaporation of the substance is purified by preparative chromatography HPLC (RP 18, acetonitrile, water, 0.01% TFUC).

Example 197

Getting trifenatate 5,5-dimethyl-3-(4-methylsulfinylphenyl)-1-pyridin-4-immatrikulation-,4-dione

Receive according to the General method 3.

M+N+= 342.

LC-MS: retention time = 0,942 minutes

Example 198

Getting trifenatate 3-[4-(3-methoxypropionitrile)phenyl]-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 3.

M+N+= 400.

LC-MS: retention time = 1,007 minutes

Example 199

Getting trifenatate 3-(4-isopropylaniline)-5,5-dimethyl-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 3.

M+N+= 370.

LC-MS: retention time = 1,096 minutes

Example 200

Getting trifenatate 5,5-dimethyl-3-{4-[3-(4-methylpiperazin-1-yl)propylsulfonyl]phenyl}-1-pyridin-4-immatrikulation-2,4-dione

Receive according to the General method 3.

M+N+= 468.

LC-MS: retention time = 0,689 minutes

Example 201

5,5-Dimethyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 0.65 g of 5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione in 40 ml of anhydrous THF in an inert atmosphere of argon and at a temperature of about 20°add 0.1 g of sodium hydride (60%). Stirring is continued at this temperature for 30 minutes. Add to 0.47 g of 4-chloromethyl-6-methoxyquinoline dissolved in 10 ml of THF. Reaction medium boil fix a refrigerator for 16 hours. After cooling, add 100 ml of water and 75 ml of ethyl acetate. After decanting, the organic phase is dried over sodium sulfate, filtered, and then concentrated under reduced pressure. The resulting brown oil purified flash chromatographia (SiO2, ethyl acetate/cyclohexane = 50:50 (volume/volume) as the eluting means, Ar). The fractions containing the product are concentrated under reduced pressure. Thus obtain 0.36 g of 5,5-dimethyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,45 (s, 6N), of 3.96 (s, 3H), 5,10 (ush., 2H), 7,46 (DD, J=9 and 3 Hz, 1H), 7,54 (d, J=3 Hz, 1H), 7,56 (l ush., J= 9 Hz, 2H), to 7.61 (d, J=4.5 Hz, 1H), 7,68 (l ush., J=9 Hz, 2H), 8,00 (d, J=9 Hz, 1H), 8,72 (d, J=4.5 Hz, 1H).

MS (IE): m/z = 459 M+, the peak of the molecular ion;

m/z = 213 C12H9N2O2+;

m/z = 172 C11H10NO+.

Connection 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione prepared as in the method described in example 63.

Getting 4-chloromethyl-6-methoxyquinoline

To a solution of 1.2 g of 4-hydroxymethyl-6-methoxyquinoline in 45 ml of dichloromethane, in an inert atmosphere of argon and at a temperature of about 20°With, successively added to 1.16 ml of triethylamine and 0.64 ml of methanesulfonanilide. Stirred at this temperature the round for 3 hours. Reaction medium was concentrated under reduced pressure, obtaining the remainder brown. The product is used without purification in the next stage.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: of 3.97 (s, 3H), and 5.30 (s, 2H), of 7.48 (DD, J= 9 and 3 Hz, 1H), 7,52 (d, J=3 Hz, 1H), 7.62mm (d, J=4.5 Hz, 1H), 8,00 (d, J=9 Hz, 1H), up 8.75 (d, J= 4.5 Hz, 1H).

MS (IE): m/z = 207 M+;

m/z = 172 (M-Cl)+, the peak of the molecular ion;

m/z = 157 (m/z = 172 - CH3)+;

m/z = 129 (m/z = 157 - CO)+.

Getting 4-hydroxymethyl-6-methoxyquinoline

To a solution of 4 g of 4-etoxycarbonyl-6-methoxyquinoline in 100 ml of anhydrous THF in an inert atmosphere of argon and at a temperature of about 5°C, dropwise add 17 ml of 1 M solution of LiAlH4in tetrahydrofuran. The reaction medium is maintained with stirring for 16 hours at a temperature of about 20°C. Add 50 ml water and 50 ml of ethyl acetate. After decanting, the organic phase is dried over sodium sulfate, filtered, and then concentrated under reduced pressure. The resulting meringue purified flash chromatography (SiO2the ethyl acetate as the eluting means, Ar). The fractions containing the product are concentrated under reduced pressure. So get 0,86 g of 4-hydroxymethyl-6-methoxyquinoline, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 3,93 (who, 3H), 5,02 (d, J=5.5 Hz, 2H), 5,57 (t, J= 5.5 Hz, 1H), 7,30 (d, J= 3 Hz, 1H), 7,38 (DD, J=9 and 3 Hz, 1H), 7,50 (d, J=4.5 Hz, 1H), 7,92 (d, J=9 Hz, 1H), 8,69 (d, J=4.5 Hz, 1H).

MS (IE): m/z = 189 M+, the peak of the molecular ion;

m/z = 174 (M-CH3)+;

m/z = 160 (M - CHO)+;

m/z = 146 (m/z = 174 - CO)+;

m/z = 117 (m/z = 146 - CHO)+.

Example 202

5,5-Dimethyl-1-(6-hydroxyquinolin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 0.26 g of 5,5-dimethyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione in 40 ml of dichloromethane, in an inert atmosphere of argon and at a temperature of approximately 0°add 6 ml of 1 M solution tribromide boron in CH2Cl2. The reaction medium is maintained with stirring at a temperature of about 20°C for 16 hours. Added dropwise 5 ml of methanol. After stirring for 30 minutes at this temperature, add 50 ml of water, 30 ml of CH2Cl2and 10 ml of a saturated solution of NaHCO3. After decanting, the organic phase is dried over sodium sulfate, filtered, and then concentrated under reduced pressure. The resulting meringue beige purified flash chromatography (SiO2the ethyl acetate as the eluting means, Ar). The fractions containing the product are concentrated under reduced pressure. Thus obtained 0.17 g of 5,5-dimethyl-1-(6-hydroxyquinolin-4-and is methyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,46 (C, 6N), 5,00 (ush., 2H), 7,30-7,40 (m, 2H), 7,51 (d, J=4.5 Hz, 1H), 7,55 (l ush., J=8.5 Hz, 2H), 7,69 (d, J=8.5 Hz, 2H), 7,94 (d, J=9 Hz, 1H), 8,64 (d, J=4.5 Hz, 1H), 10,12 (m, 1H).

MS (EI): m/z = 445 M+;

m/z = 199 C11H7N2O2+;

m/z = 158 C10H8NO+, the peak of the molecular ion.

Example 203

5,5-Dimethyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

The product is obtained following the procedure described in example 59, from 0,94 g of methyl ester of 2-methyl-2-[(7-methoxyquinoline-4-ylmethyl)amino]propanoic acid instead of methyl ester of 2-methyl-2-[(quinoline-4-ylmethyl)amino]propanoic acid used according to example 59, and 1.7 g of 4-(trifloromethyl)isocyanate. After purification column flash chromatography (SiO2, cyclohexane/ethyl acetate = 70:30 by volume, then CH2Cl2/methanol = 90:10 by volume, as the eluting means; Ar) obtain 1.45 g of the target product.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), of 3.96 (s, 3H), 5,12 (ush., 2H), 7,35 (DD, J=9 and 3 Hz, 1H), 7,47 (d, J=3 Hz, 1H), 7,49 (d, J=4.5 Hz, 1H), 7,55 (l ush., J=9 Hz, 2H), 7,68 (l ush., J=9 Hz, 2H), 8,19 (d, J=9 Hz, 1H), 8,80 (d, J=4.5 Hz, 1H).

MS (EI): m/z = 459 M+, the peak of the molecular ion;

m/z = 444 (M CH 3)+;

m/z = 213 C12H9N2O2+;

m/z = 172 C11H10NO+.

Obtaining methyl ester-2-[(7-methoxyquinoline-4-ylmethyl)amino]propanoic acid

A mixture of 1.23 g of methyl ester hydrochloride α-aminoadamantane acid and 1.12 ml of triethylamine in 30 ml of dichloromethane is stirred at a temperature of 0°C for 20 minutes. Then add 1 g of magnesium sulfate and 1.5 g of 7-methoxyquinoline-4-carbaldehyde. Stirring is maintained for 15 hours at room temperature, the mixture is then concentrated under reduced pressure. The residue is treated with 35 ml of methanol, the resulting solution is cooled to a temperature of 0°then added in several portions 0.31 g sodium borohydride. The reaction medium is stirred at a temperature of about 20°C for 15 hours. Reaction medium was concentrated under reduced pressure. The resulting residue is treated with 100 ml of ethyl acetate. The precipitation is filtered off and the filtrate is concentrated under reduced pressure, then purified column flash chromatography (SiO2the ethyl acetate as the eluting means, Ar); obtain 0.95 g of the target product.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,35 (C, 6N), 2,63 (t, J= 7.5 Hz, 1H), 3,70 (s, 3H), 3,93 (s, 3H), of 4.05 (d, J=7.5 Hz, 2H), 7,28 (DD, J=9 and 3 Hz, 1H), 7,41 (d, J=3 Hz, 1H), 7,43 (d, J=4,5Hz, 1H), 8,12 (d, J=9 Hz, 1H), 8,76 (d, J=4.5 Hz, 1H).

MS (IC) (mass spectrometry with chemical ionization):

m/z = 289 MN+,the peak of the molecular ion;

m/z = 229 (M - C2H4About2)+.

Getting 7-methoxyquinoline-4-carbaldehyde

A mixture of 1.9 grams of oxide of selenium in the form of a solution in 35 ml of dioxane are added dropwise to a solution of 2.7 g of 4-methyl-7-methoxyquinoline in 35 ml of dioxane, preheated to a temperature of 65°C. after the addition, the suspension is chestnut colored heated at a temperature of about 80°C for 5 hours. The reaction medium is stirred for 16 hours at a temperature of about 20°C. Suspension greenish sucked off, then washed with ethyl acetate. The filtrate is concentrated under reduced pressure. The resulting suspension is crystallized from diisopropyl ether, receiving 1.54 g 7-methoxyquinoline-4-carbaldehyde.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 3,99 (s, 3H), of 7.48 (DD, J=9 and 3 Hz, 1H), EUR 7.57 (d, J=3 Hz, 1H), of 7.90 (d, J=4.5 Hz, 1H), 8,89 (d, J=9 Hz, 1H), 9,19 (d, J=4.5 Hz, 1H), 10,52 (s, 1H).

MS (IC): m/z = 188 MN+, the peak of the molecular ion.

Getting 4-methyl-7-methoxyquinoline

To a solution of 6 g of 4-bromo-7-methoxyquinoline in 100 ml of DMF in an inert atmosphere of argon and at a temperature of about 20°add 4 g of triphenylphosphine, with 5.3 g of lithium chloride, 14 ml tetramethylurea and 2.1 g of bis(Trifan lfopen)palladium(II)chloride. The reaction medium is heated at a temperature of about 120°C for 16 hours. After cooling, the insoluble part is filtered off. The filtrate is concentrated under reduced pressure. The resulting residue is treated with 300 ml of ethyl acetate and 300 ml of water. After decanting, the organic phase is dried over magnesium sulfate, filtered, and then concentrated under reduced pressure. The oil obtained is treated with 300 ml of ethyl acetate and 300 ml of water, then acidified with hydrochloric acid until pH = 1. The aqueous phase is alkalinized with sodium hydroxide up to pH = 10, then extracted with 300 ml of ethyl acetate. After decanting, the organic phase is dried over magnesium sulfate, filtered, and then concentrated under reduced pressure, obtaining 2.7 g of 4-methyl-7-methoxyquinoline, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: to 2.65 (s, 3H), of 3.94 (s, 3H), 7.23 percent (l ush., J=4.5 Hz, 1H), 7,28 (DD, J=9 and 3 Hz, 1H), 7,40 (d, J=3 Hz, 1H), 8,01 (d, J=9 Hz, 1H), 8,58 (d, J=4.5 Hz, 1H).

MS (IE): m/z = 173 M+, the peak of the molecular ion;

m/z = 158 (M-CH3)+;

m/z = 143 (M - CH2O)+;

m/z = 130 (m/z = 158 - CO)+.

Getting 4-bromo-7-methoxyquinoline

22,74 g of 4-Hydroxy-7-methoxyquinoline added to 200 g of oxybromide phosphorus, preheated to a temperature of about 110°C. the Reaction environment nagrevaete this temperature for 3 hours. Reaction medium was poured in a hot condition in a mixture of 500 ml of ethyl acetate and 500 ml of ice water. The medium is neutralized with potassium carbonate until pH = 7. After decanting, the organic phase is dried over magnesium sulfate, evaporated under reduced pressure, then purified column chromatographie (SiO2, ethyl acetate/cyclohexane = 50:50 by volume as the eluting means, Ar); obtain 14.6 g of the target product.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: of 3.97 (s, 3H), 7,43 (DD, J=9 and 3 Hz, 1H), 7,49 (d, J=3 Hz, 1H), 7,79 (d, J=4.5 Hz, 1H), of 8.06 (d, J=9 Hz, 1H), 8,67 (d, J=4.5 Hz, 1H).

MS (IE): m/z = 237 M+, the peak of the molecular ion.

4-Hydroxy-7-methoxyquinoline receive according to the method described in J. Am. Chem. Soc.,68, 1268 (1946).

Example 204

5,5-Dimethyl-1-(7-hydroxyquinolin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

A mixture of 0.89 g of 5,5-dimethyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione and 5.5 g of pyridine hydrochloride is heated at a temperature of about 220°C for 4 hours. After cooling, add 200 ml of water and 100 ml of CH2Cl2. After decanting, the organic phase is dried over sodium sulfate, filtered, and then concentrated under reduced pressure. The obtained solid is purified flash chromatographia (SiO2, atilas the tat/CH 2Cl2= 40:60 by volume as the eluting means; Ar). The fractions containing the product are concentrated under reduced pressure. Thus obtain 85 mg of 5,5-dimethyl-1-(7-hydroxyquinolin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,45 (s, 6N), 5,08 (ush., 2H), 7,24 (DD, J=9 and 3 Hz, 1H), 7,30 (d, J=3 Hz, 1H), 7,38 (d, J=4.5 Hz, 1H), 7,55 (l ush., J=9 Hz, 2H), 7,68 (l ush., J=9 Hz, 2H), 8,10 (d, J=9 Hz, 1H), 8,71 (d, J=4.5 Hz, 1H), 9,90-10,50 (m ush., 1H).

MS (IE): m/z = 445 M+, the peak of the molecular ion;

m/z = 430 (M - CH3)+;

m/z = 199 C11H7N2O2+;

m/z = 158 C10H8NO+.

Example 205

5,5-Dimethyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 0.8 g of 5,5-dimethyl-1-(N-oksihinolina-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione in 10 ml of chloroform, in an inert atmosphere of argon and at a temperature of about 5°add 0,44 g taillored. After stirring for 30 minutes at the same temperature, add 1.5 ml of 32%aqueous ammonium hydroxide solution. Stand to raise the temperature up to 20°C. the Reaction medium is stirred at a temperature of about 20°C for 16 hours. Add 100 ml of water. After decanter and the organic phase is dried over sodium sulfate, filtered, then concentrated under reduced pressure. The obtained solid is purified flash chromatographia (SiO2the ethyl acetate as the eluting means; Ar). The fractions containing the product are concentrated under reduced pressure. Thus receive 200 mg of 5,5-dimethyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,49 (C, 6N), 4,96 (ush., 2H), 6,36 (ush., 2N), for 6.81 (s, 1H), 7.23 percent (m, 1H), 7,51 (m, 2H), 7,58 (l ush., J=9 Hz, 2H), 7,68 (l ush., J= 9 Hz, 2H), to $ 7.91 (d, J=8.5 Hz, 1H).

MS (IE): m/z = 444 M+, the peak of the molecular ion;

m/z = 429 (M - CH3)+;

m/z = 198 C11H8N3O+;

m/z = 158 C10H10N2+.

Example 206

5,5-Dimethyl-1-(N-oksihinolina-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 1.95 g of 5,5-dimethyl-1-(quinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione in 200 ml of chloroform and 10 ml of methanol in an inert atmosphere of argon and at a temperature of about 20°add 0,78 g m-chlormadinone acid. The reaction medium is stirred at a temperature of about 20°C for 4 hours. Add an additional 0.8 g m-chlormadinone acid. Reaction medium was concentrated under reduced giving the situation. The product is crystallized from diisopropyl ether, receiving of 1.76 g of 5,5-dimethyl-1-(N-oksihinolina-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,45 (s, 6N), 5,09 (ush., 2H), 7,55 (l ush, J=8.5 Hz, 2H), 7,63 (d, J=4.5 Hz, 1H), 7,68 (l ush., J=8.5 Hz, 2H), 7,85 (t ush., J=8.5 Hz, 1H), to $ 7.91 (t ush., J=8.5 Hz, 1H), 8,35 (l ush., J=8.5 Hz, 1H), 8,56 (d, J=4.5 Hz, 1H), 8,64 (l ush., J=8.5 Hz, 1H).

MS (ES) (mass spectrometry with ionization electron spray): m/z = 446 MN+, the peak of the molecular ion.

Example 207

5,5-Dimethyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 4 ml of DMF and 2 ml of toluene in an inert atmosphere of argon and at a temperature of about 5°add to 0.17 ml of phosphorus oxychloride. After stirring for 30 minutes at the same temperature, add 0.4 g of 5,5-dimethyl-1-(N-oksihinolina-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione in 10 ml of toluene. The reaction medium is maintained with stirring at a temperature of about 5°With over two and a half hours. Stand to raise the temperature up to 20°C. the Reaction medium was concentrated under reduced pressure. The resulting residue is treated with 50 ml of ethyl acetate and washed with saturated solution of NaHCO3. After de is antali the organic phase is dried over sodium sulfate, filtered, then concentrated under reduced pressure. The product is crystallized from diisopropyl ether, receiving and 0.37 g of 5,5-dimethyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1.50 in (C, 6N), 5,17 (ush., 2H), 7,56 (l ush., J=8.5 Hz, 2H), 7,71 (l ush., J=8.5 Hz, 2H), 7,76 (s, 1H), 7,76 (t DD, J=8 and 1.5 Hz, 1H), 7,89 (t DD, J=8 and 1.5 Hz, 1H), 8,03 (l ush, J=8 Hz, 1H), 8,31 (l ush., J=8 Hz, 1H).

MS (IE): m/z = 463 M+, the peak of the molecular ion;

m/z = 448 (M - CH3)+;

m/z = 428 (M - Cl)+;

m/z = 358 (m/z = 428 - C4H6O)+;

m/z = 217 C11H6N2OCl+;

m/z = 176 C10H7NCl+.

Example 208

5,5-Dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 0.1 g of 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione in 2 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0,028 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution of 0.1 g of 2-chloro-4-(methyl bromide)of pyridine in 2 ml of dimethylformamide, and then, after 10 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 20 mm, filled with 17 g of silica with grafted octadecylsilyl groups who, 50 μm, air-conditioned successively with acetonitrile, then with water. Elution is performed by the gradient using a mixture of water/acetonitrile with 0-100% acetonitrile. The fraction containing the target product, concentrate under reduced pressure. So get 0,130 g crude product which is purified by double chromatography using a column Packed with 10 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (8:2, vol/vol) with a flow rate of 5 ml/min Fractions collected between 30 ml and 75 ml concentrate under reduced pressure. Thus obtained 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione in the form of a white powder whose characteristics are the following:

So pl.: 134°C.

MS (IE): m/z = 413 M+,the peak of the molecular ion;

m/z = 398 (M - CH3)+;

m/z = 203 C8H4NO2F3+;

m/z = 167 C7H4N2OCl+;

m/z = 126 C6H5NCl+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), of 4.67 (s, 2H), 7,50 (d ush., J=5.5 Hz, 1H), 7,54 (d ush., J=9 Hz, 2H), to 7.61 (ush., 1H), 7,66 (l ush., J=9 Hz, 2H), 8,40 (d, J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione described in example 63.

Example 209

5,5-Dimethyl-1-(2-ethoxypyridine-4-elmet the l)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution 0,175 g of 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione in 2 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0.015 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution 0,185 g 2 ethoxy-4-(methyl bromide)of pyridine in 2 ml of anhydrous dimethylformamide, and then, after 10 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 37 mm, filled with 65 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution is performed with the mixture of water/acetonitrile (95:5, vol/vol) for 20 minutes, then linear gradient of 5-95% acetonitrile in 60 minutes, with a flow rate of 10 ml/min Fractions collected between 700 and 760 ml ml concentrate under reduced pressure. So get 0,145 g of 5,5-dimethyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 423 M+;

m/z = 408 (M - CH3)+, the peak of the molecular ion;

m/z = 395 (M - C2H4)+;

m/z = 203 C8H4NO2F3+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ m is.: of 1.32 (t, J=7 Hz, 3H), of 1.42 (s, 6N), 4,30 (kV, J=7 Hz, 2H), 4,58 (ush., 2H), 6,85 (ush., 1H), 7,01 (l ush., J=5.5 Hz, 1H), 7,52 (d ush., J=8.5 Hz, 2H), 7,63 (l ush., J=8.5 Hz, 2H), 8,10 (d, J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione described in example 63.

Example 210

5,5-Dimethyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution 0,064 g of 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione in 1 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0,009 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution 0,062 g 2-ethyl-4-(methyl bromide)of pyridine in 0.5 ml of anhydrous dimethylformamide, and then, after 10 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 27 mm, filled with 25 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution is performed with the mixture of water/acetonitrile (95:5, vol/vol) for 20 minutes, then linear gradient of 5-95% acetonitrile in 60 minutes, with a flow rate of 10 ml/min Fractions collected between 750 and 790 ml ml concentrate under reduced pressure. Thus obtain 0.06 g of 5,5-dimethyl-1-(2-ethylpyridine-4-ylmethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 407 M+, the peak of the molecular ion;

m/z = 392 (M - CH3)+;

m/z = 203 C8H4NO2F3+;

m/z = 120 C8H10N+.

1H-NMR-spectrum (400 MHz, (CD3)2SO-d6) δ in ppm: of 1.27 (t, J=7.5 Hz, 3H), of 1.44 (s, 6N), a 2.75 (q, J=7.5 Hz, 2H), of 4.54 (s, 2H), 7,10 (l ush., J=5.5 Hz, 1H), 7,15 (ush., 1H), 7,39 (l ush., J=8.5 Hz, 2H), 7,49 (d, J=8.5 Hz, 2H), compared to 8.26 (d, J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione described in example 63.

Example 211

5,5-Dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution 0,175 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 3 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0,046 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution 0,166 g of 2-chloro-4-(methyl bromide)of pyridine in 2 ml of anhydrous dimethylformamide, and then, after 10 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 37 mm, filled with 65 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Blueraven the e carried out with a mixture of water/acetonitrile (95:5, volume/volume) for 20 minutes, then linear gradient of 5-95% acetonitrile in 60 minutes, with a flow rate of 10 ml/min Fractions collected between 740 and 780 ml ml concentrate under reduced pressure. Thus obtain 0.03 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a white powder whose characteristics are the following:

TPL: 111°C.

MS (IC): m/z = 447 MNH4+;

m/z = 430 MH+, the peak of the molecular ion.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), 4,67 (ush., 2H), 7,49 (l ush., J=5.5 Hz, 1H), to 7.61 (ush., 1H), 7,70 (l ush., J=8.5 Hz, 2H), 7,88 (l ush., J=8.5 Hz, 2H), scored 8.38 (d, J=5.5 Hz, 1H).

Getting 5,5-dimethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione

To a solution of 4 g of 4-triftormetilfullerenov in 40 ml of toluene in an inert atmosphere of argon and at a temperature of about 20°add 5,12 ml of triethylamine and 2.8 g of methyl ester hydrochloride α-aminoadamantane acid. The thus obtained mixture is refluxed for 24 hours, then cooled to a temperature of about 20°C. the Reaction mixture is concentrated to dryness under reduced pressure, the obtained residue is treated with diethyl ether, filtered off. So get with 5.3 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin,4-dione, the characteristics of which are the following:

MS (IC): m/z = 322 MNH4+;

m/z = 102 triethylamine H+the peak of the molecular ion.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), a 7.62 (d ush., J=8.5 Hz, 2H), 7,85 (l ush., J=8.5 Hz, 2H), 8,72 (m, 1H).

The thus obtained insoluble substance is treated with dichloromethane, then washed with water. Thus obtain 2.76 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione, which is used for further synthesis.

Example 212

5,5-Dimethyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution 0,185 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 3.2 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0,049 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution 0,184 g 2 ethoxy-4-(methyl bromide)of pyridine in 2 ml of anhydrous dimethylformamide, and then, after 10 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 37 mm, filled with 65 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Eleirovania is carried out with a mixture of water/acetonitrile (95:5, volume/volume) for 20 minutes, then linear gradient of 5-95% acetonitrile in 60 minutes, with a flow rate of 10 ml/min Fractions collected between 520 ml and 700 ml concentrate under reduced pressure. Thus obtained residue is purified flash chromatography using a column Packed with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (9:1, volume/volume). The fraction containing the target product, concentrate under reduced pressure. So get 0.01 g of 5,5-dimethyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 439 M+;

m/z = 424 (M - CH3)+, the peak of the molecular ion;

m/z = 411 (M - C2H4)+;

m/z = 219 C8H4NOSF3+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: to 1.32 (t, J=7 Hz, 3H), of 1.42 (s, 6N), 4,30 (kV, J=7 Hz, 2H), 4,58 (ush., 2H), 6,86 (ush., 1H), 7,01 (l ush., J=5.5 Hz, 1H), 7,69 (l ush., J=8.5 Hz, 2H), 7,88 (l ush., J=8.5 Hz, 2H), 8,10 (l ush., J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione described in example 211.

Example 213

5,5-Dimethyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The solution is 0.135 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione is in 2 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0,021 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution of 0.126 g of 2-ethyl-4-(methyl bromide)of pyridine in 1 ml of anhydrous dimethylformamide, and then, after 10 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 37 mm, filled with 65 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution is performed with the mixture of water/acetonitrile (95:5, vol/vol) for 20 minutes, then linear gradient of 5-95% acetonitrile in 60 minutes, with a flow rate of 10 ml/min Fractions collected between 800 and 880 ml ml concentrate under reduced pressure. So get 0,120 g of 5,5-dimethyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 423 M+, the peak of the molecular ion;

m/z = 408 (M - CH3)+;

m/z = 219 C8H4NOSF3+;

m/z = 120 C8H10N+.

1H-NMR-spectrum (400 MHz, (CD3)2SO-d6) δ in ppm: of 1.23 (t, J=7.5 Hz, 3H), of 1.42 (s, 6N), 2,75 (sq, J=7.5 Hz, 3H), 4,62 (ush., 2H), 7,25 (l ush., J=5.5 Hz, 1H), 7,30 (ush., 1H), of 7.70 (d, J=8.5 Hz, 2H), 7,88 (d, J=8.5 Hz, 2H), 8,43(d, J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione described in example 211.

Example 214

5,5-Dimethyl-1-(2-bromopyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 0.081 g of 5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione in 2 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°With add is 0.023 g of sodium hydride, stirring maintain at this temperature for 35 minutes, add a solution 0,071 g of 2-bromo-4-(methyl bromide)of pyridine in 1 ml of anhydrous dimethylformamide, and then, after 15 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 16 mm, was filled with 5 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution carried out with a linear gradient of 5-95% acetonitrile for 30 minutes, then the mixture of water/acetonitrile (5:95, volume/volume) for 10 minutes, with a flow rate of 5 ml/min Fractions collected between 90 ml and 100 ml, concentrate under reduced pressure. So get 0,015 g of 5,5-dimethyl-1-(2-bromopyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 457 M+, permolecular ion;

m/z = 442 (M - CH3)+;

m/z = 211 C7H4N2OBr+;

m/z = 203 C8H4NO2F3+;

m/z = 170 C6H5NBr+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), 4,67 (ush., 2H), 7,52 (d ush., J=5.5 Hz, 1H), 7,54 (d ush., J=9 Hz, 2H), 7,66 (l ush., J=9 Hz, 2H), 7,75 (ush., 1H), of 8.37 (d, J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-trifloromethyl)-imidazolidin-2,4-dione described in example 63.

Example 215

5,5-Dimethyl-1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution of 0,096 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 2 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0.025 g of sodium hydride, stirring maintain at this temperature for 25 minutes, add a solution to 0.060 g of 2-fluoro-4-(methyl bromide)of pyridine in 1 ml of anhydrous dimethylformamide, and then, after 15 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 16 mm, was filled with 5 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution carried out with a linear gradient of 5-95% acetonitrile for 30 mi the ut, then a mixture of water/acetonitrile (5:95, volume/volume) for 10 minutes, with a flow rate of 5 ml/min Fractions collected between 105 ml and 125 ml concentrate under reduced pressure. So get 0,069 g of 5,5-dimethyl-1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a white powder whose characteristics are the following:

TPL: 82°C.

MS (IE): m/z = 413 M+, the peak of the molecular ion;

m/z = 398 (M - CH3)+;

m/z = 219 C8H4NOSF3+;

m/z = 151 C7H4N2OF+;

m/z = 110 C6H5NF+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,45 (s, 6N), 4,72 (ush., 2H), 7,29 (ush., 1H), 7,43 (l ush., J=5.5 Hz, 1H), 7,71 (l ush., J=8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 8,23 (d, J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione described in example 211.

Example 216

5,5-Dimethyl-1-(2-cyano-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution of 0,139 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 4 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0,037 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution 0,090 g 2-cyano-4-(methyl bromide)of pyridine in 1 ml besod the CSOs of dimethylformamide, then, after 15 minutes of reaction, ice water. The reaction mixture is placed in a column with a diameter of 20 mm, filled with 10 g of silica with grafted octadecylsilyl groups, 40-60 μm, air-conditioned successively with a mixture of water/acetonitrile (5:95, volume/volume), then a mixture of water/acetonitrile (95:5, vol/vol). Elution carried out with a linear gradient of 5-95% acetonitrile for 30 minutes, then the mixture of water/acetonitrile (5:95, volume/volume) for 10 minutes, with a flow rate of 5 ml/min Fractions collected between 210 ml 230 ml, concentrated under reduced pressure. Thus obtained 0.1 g of 5,5-dimethyl-1-(2-cyano-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a solid whose characteristics are the following:

TPL: 148°C.

MS (IE): m/z = 420 M+, the peak of the molecular ion;

m/z = 405 (M - CH3)+;

m/z = 219 C8H4NOSF3+;

m/z = 158 C7H4N3O+;

m/z = 117 C7H5N2+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), 4,74 (ush., 2H), 7,72 (l ush., J=9 Hz, 2H), 7,81 (DD, J=5.5 and 2 Hz, 1H), 7,89 (l ush., J = 9 Hz, 2H), 8,15 (ush., 1H), 8,72 (l ush., J=5.5 Hz, 1H).

Connection 5,5-dimethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione described in example 211.

Example 217

5,5-Dimethyl-1-(2-hydroxyaryl espiridion-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

A solution of 0.09 g of 5,5-dimethyl-1-(2-cyano-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 5 ml of 5 N. hydrochloric acid is refluxed for about 16 hours. The reaction mixture was concentrated under reduced pressure and the thus obtained crude product is purified flash chromatography, using a column with a diameter of 200 mm, filled with 10 g of silica, 20-40 μm, and condition, then elute with a mixture of dichloromethane/methanol (9:1, vol/vol), with a flow rate of 8 ml per minute. The fraction collected between 40 and 200 ml concentrated under reduced pressure. Thus obtain 0.06 g of 5,5-dimethyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 439 M+;

m/z = 395 (M - CONH2)+, the peak of the molecular ion;

m/z = 219 C8H4NOSF3+;

m/z = 185 C7H9N2O2S+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,45 (s, 6N), 4,76 (ush., 2N), of 7.70 (d, J=8.5 Hz, 2H), 7,72 (m, 1H), 7,89 (d, J=8.5 Hz, 2H), 8,12 (ush., 1H), 8,68 (d, J=5.5 Hz, 1H).

Example 218

5,5-Dimethyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The solution to 0.055 g of 5,5-dimethyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl milfoil)imidazolidin-2,4-dione in 2 ml of dichloromethane, in an inert atmosphere of argon and at a temperature of about 20°add sequentially 0.025 g of methylaminopropane, 0.005 g of hydroxybenzotriazole, 0,105 ml of triethylamine and 72 mg of the hydrochloride of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, stirring maintain at this temperature for about 16 hours. The reaction mixture was poured into water, the organic phase is dried over magnesium sulfate, filtered, and then concentrated under reduced pressure. The thus obtained crude product is purified flash chromatography, using a column with a diameter of 16 mm, was filled with 5 g of silica, 20-40 μm, and condition, then elute with a mixture of dichloromethane/methanol (95:5, vol/vol), with a flow rate of 10 ml per minute. The fraction containing the target product, concentrate under reduced pressure. So get 0,013 g of 5,5-dimethyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a white powder whose characteristics are the following:

MS (IE): m/z = 452 M+;

m/z = 395 (M - C2H3ON)+, the peak of the molecular ion;

m/z = 219 C8H4NOSF3+;

m/z = 148 C8H8N2O+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), 2,85 (d, J=5 Hz, 3H), 4,76 (ush, 2H), to 7.67 (DD, J=5 and 2 Hz, 1H), 7,70 (l ush., J=8.5 Hz, 2H), 7,89 (l ush.,J=8.5 Hz, 2H), 8,10 (ush., 1H), at 8.60 (d, J=5 Hz, 1H), 8,75 (kV ush., J=5 Hz, 1H).

Example 219

5,5-Dimethyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

A solution of 0.04 g of 5,5-dimethyl-1-(2-cyano-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 1 ml of 98%sulfuric acid is heated at a temperature of 40°C for 30 minutes. The mixture is treated with 15 ml of ice water, then neutralize 1N solution of sodium hydroxide. The thus obtained solution is extracted with 100 ml of ethyl acetate. The organic phase is dried over magnesium sulfate, filtered, and then concentrated under reduced pressure, the thus obtained crude product is purified flash chromatography, using a column with a diameter of 16 mm, was filled with 5 g of silica, 20-40 μm, and condition, then elute with dichloromethane with a flow rate of 10 ml per minute. The fraction containing the target product, concentrate under reduced pressure. So get 0,017 g of 5,5-dimethyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of an amorphous white powder, the characteristics of which are the following:

MS (IE): m/z = 438 M+, the peak of the molecular ion;

m/z = 423 (M - CH3)+;

m/z = 393 (M - CH3NO)+;

m/z = 219 C8H4NOSF3+;

m/z = 135 7H7N2O+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (C, 6N), 4,76 (ush., 2H), 7,60-of 7.70 (m, 2H), 7,71 (l ush., J=8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 8,11 (ush., 2N), at 8.60 (d, J=5.5 Hz, 1H).

Example 220

5,5-Dimethyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.05 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, 0.5 ml of dimethylformamide, 0,034 g of potassium carbonate and 0,021 ml of the research, put in microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 210°C for about 50 minutes. The reaction mixture contribute in column BOND ELUT VARIAN according to the standard 1225-6053 containing 2 g SCX phase, which is air-conditioned dimethylformamide. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (8:2, vol/vol) with a flow rate of 10 ml/min Fractions collected between 160 ml and 260 ml, concentrated to dryness under reduced pressure. Thisway get 0.01 g of 5,5-dimethyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione in the form of powder, the characteristics of which are the following:

MS (IE): m/z = 464 M+;

m/z = 433 (M - CH3O)+, the peak of the molecular ion;

m/z = 419 (M - C2H5O)+;

m/z = 407 (M - C3H5O)+;

m/z = 379 (M - C4H5NO)+;

m/z = 203 C8H4NO2F3+;

m/z = 176 C10H12N2O+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), 3,44 (t ush., J=5 Hz, 4H), and 3.72 (t ush., J= 5 Hz, 4H), 4.53-in (with ush., 2H), 6.75 in (l ush., J= 5.5 Hz, 1H), 6,85 (ush., 1H), 7,54 (d ush., J= 8.5 Hz, 2H), to 7.64 (d, J=8.5 Hz, 2H), 8,10 (d, J=5.5 Hz, 1H).

Example 221

5,5-Dimethyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.05 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.5 ml of the research, put in microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 160°C for about 70 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN based on the standard 1225-6053 containing 2 g SCX phase, which is air-conditioned with methanol. Exercise is romescu methanol, then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtain 0.03 g of 5,5-dimethyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a powder whose characteristics are the following:

MS (IE): m/z = 480 M+;

m/z = 449 (M - CH3O)+, the peak of the molecular ion;

m/z = 435 (M - C2H5O)+;

m/z = 423 (M - C3H5O)+;

m/z = 219 C8H4NOSF3+;

m/z = 176 C10H12N2O+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), 3,45 (t ush., J=5 Hz, 4H), 3,71 (t ush., J= 5 Hz, 4H), 4,54 (ush., 2H), 6.75 in (l ush., J= 5.5 Hz, 1H), 6,84 (ush., 1H), 7,68 (l ush., J= 8.5 Hz, 2H), 7,88 (d, J=8.5 Hz, 2H), of 8.09 (d, J=5.5 Hz, 1H).

Example 222

5,5-Dimethyl-1-(2-dimethylaminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.05 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.4 ml of Isopropylamine, 0.1 ml of dimethylformamide are placed in a microwave oven Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 140°With approximately 130 minutes. The reaction mixture was purified preparative LC/MS. The fractions containing CE the eve of the product, concentrate to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6053 containing 2 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. So get 0,013 g of 5,5-dimethyl-1-(2-dimethylaminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in the form of a powder whose characteristics are the following:

MS (IC): m/z = 439 MN+, the peak of the molecular ion.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), 3,03 (C, 6N), 4,53 (ush., 2H), 6,62 (l ush., J= 5.5 Hz, 1H), 6,65 (ush., 1H), 7,68 (l ush., J= 8.5 Hz, 2H), 7,87 (d, J=8.5 Hz, 2H), 8,03 (d, J=5.5 Hz, 1H).

Example 223

5,5-Dimethyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.5 ml of N-methylpyrrolidone-2, 0,016 mg methylaminopropane, 0,064 ml of triethylamine are placed in a microwave oven Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 180°C for about 80 minutes. Reactio the ing a mixture of purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6054 containing 3 g of SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction containing the target product are concentrated to dryness under reduced pressure. So get 0,021 g of 5,5-dimethyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in the form of an amorphous white powder, the characteristics of which are the following:

MS (IE): m/z = 424 M+, the peak of the molecular ion;

m/z = 396 (M - CH2N)+;

m/z = 219 C8H4NOSF3+;

m/z = 120 C7H8N2+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), 2,77 (d, J=5 Hz, 3H), 4,48 (ush., 2H), 6.42 per (m, 1H), 6,46 (ush., 1H), 6,52 (l ush., J= 5.5 Hz, 1H), 7,69 (l ush., J=8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 7,94 (d, J=5.5 Hz, 1H).

Example 224/b>

5,5-Dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of cyclohexylamine, placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 50 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6054 containing 3 g of SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 15 ml and 45 ml), concentrated to dryness under reduced pressure. So get 0,017 g of 5,5-dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of amorphous powder, the characteristics of which are the following:

MS (IE): m/z = 492 M+;

m/z = 449 (M - C3H7)+;

m/z = 435 (M - C3H7)+;

m/z = 410 (M - C6H10)+, the peak of the molecular ion;

m/z = 219 C8H4NOSF3+;

m/z = 175 C11H15N2+;

m/z = 98, C6H12N+.

1H-NMR-spectrum (400 MHz, (CD3)2SO-d6) δ in ppm: 1,10-1,40 (m, 5H), USD 1.43 (s, 6N), 1.55V is 2.00 (m, 5H), to 3.67 (m, 1H), of 4.45 (s, 2H), 6,28 (d, J=8 Hz, 1H), 6,44 (ush., 1H), 6,46 (l ush., J= 5.5 Hz, 1H), 7,68 (l ush., J= 9 Hz, 2H), a 7.85-to 7.95 (m, 3H).

Example 225

5,5-Dimethyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of Isopropylamine, placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 70 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, air-conditioned which m is canola. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 10 ml and 35 ml concentrated to dryness under reduced pressure. Thus receive 0.008 g of 5,5-dimethyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of amorphous powder whose characteristics are the following:

MS (IE): m/z = 452 M+;

m/z = 437 (M - CH3)+, the peak of the molecular ion;

m/z = 410 (M - C3H6)+;

m/z = 219 C8H4NOSF3+;

m/z = 134 C8H10N2+;

m/z = 58 C3H8N+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,13 (d, J=6,5 Hz, 6N), of 1.42 (s, 6N), 3,98 (m, 1H), 4,45 (ush., 2H), 6,27 (l ush., J=7.5 Hz, 1H), 6.42 per (ush., 1H), 6,46 (l ush., J=5.5 Hz, 1H), 7,68 (l ush., J=8 Hz, 2H), 7,88 (l ush., J=8 Hz, 2H), of 7.90 (d, J=5.5 Hz, 1H).

Example 226

5,5-Dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dime the Il-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of piperidine are placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 30 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 10 ml and 30 ml, concentrated to dryness under reduced pressure. Thus obtain 0.07 g of 5,5-dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in the form of amorphous powder whose characteristics are the following:

MS (IE): m/z = 478 M+, the peak of the molecular ion;

m/z = 449 (M - C2H5)+;

m/z = 422 (M - C4H8)+;

m/z = 395 (M - C5H9N)+;/p>

m/z = 219 C8H4NOSF3+;

m/z = 161 C10H13N2+;

m/z = 84 C8H10N+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), 1,45-of 1.65 (m, 6N), 3,52 (t ush., J=5 Hz, 4H), to 4.52 (ush., 2H), 6,64 (l ush., J= 5.5 Hz, 1H), 6,83 (ush., 1H), 7,68 (d , J= 8.5 Hz, 2H), 7,88 (d, J=8.5 Hz, 2H), 8,04 (d, J=5.5 Hz, 1H).

Example 227

5,5-Dimethyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of N-methylpiperazine, placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 30 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained is the residue purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 105 ml 135 ml, concentrated to dryness under reduced pressure. So get 0,028 g of 5,5-dimethyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in the form of amorphous powder whose characteristics are the following:

MS (IE): m/z = 493 M+;

m/z = 423 (M - C4H8N)+, the peak of the molecular ion;

m/z = 219 C8H4NOSF3+;

m/z = 176 C10H14N3+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), of 2.23 (s, 3H), 2.40 a (t ush., J=5 Hz, 4H), 3,50 (t ush., J=5 Hz, 4H), 4.53-in (with ush., 2H), 6,70 (l ush., J= 5.5 Hz, 1H), 6,85 (ush., 1H), 7,69 (d, J= 8.5 Hz, 2H), 7,88 (d, J=8.5 Hz, 2H), 8,07 (d, J=5.5 Hz, 1H).

Example 228

5,5-Dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of aniline, placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 30 minutes. React the mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 40 ml and 85 ml, concentrated to dryness under reduced pressure. So get 0,082 g of 5,5-dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in the form of amorphous powder whose characteristics are the following:

MS (IE): m/z = 486 M+;

m/z = 485 (M - H)+, the peak of the molecular ion;

m/z = 417 (M - CF3)+;

m/z = 182 C12H10N2+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,46 (C, 6N), 4,55 (ush., 2H), 6,80 (l ush., J=5.5 Hz, 1H), 6,84 (ush., 1H), 6,88 (t ush., J= 7.5 Hz, 1H), 7,25 (DD, J= 8 and 7.5 Hz, 2H), to 7.67 (d ush., J=8 Hz, 2H), 7,69 (d, J=8.5 Hz, 2H), 7,88 (l ush., J=8.5 Hz, 2H), 8,01 (d, J=5.5 Hz, 1H), 9,01 (ush., 1H).

Example 29

5,5-Dimethyl-1-[2-(4-piperazine derivatives)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.6 ml of N-methylpyrrolidone-2, 0,123 g of piperazine are placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 30 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 45 ml and 110 ml, concentrated to dryness under reduced pressure. So get 0,042 g of 5,5-dimethyl-1-[2-(4-piperazine derivatives)pyridine-4-ylmethyl]-3-(4-triptime sulfanilyl)imidazolidin-2,4-dione in the form of amorphous powder, the characteristics of which are the following:

MS (IC): m/z = 480 MN+, the peak of the molecular ion.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,43 (C, 6N), and 2.79 (t ush., J=5 Hz, 4H), 3,41 (t ush., J= 5 Hz, 4H), to 4.52 (ush., 2H), 6,69 (l ush., J= 5.5 Hz, 1H), 6,82 (ush., 1H), 7,69 (l ush., J= 8.5 Hz, 2H), 7,88 (d, J=8.5 Hz, 2H), of 8.06 (d, J=5.5 Hz, 1H).

Example 230

5,5-Dimethyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.5 ml of N-methylpyrrolidone-2, 0,019 g etilamingidrokhlorida, 0,064 ml of triethylamine are placed in a microwave oven Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 120 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified F. the ash-chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 280 ml and 300 ml, concentrated to dryness under reduced pressure. So get 0,033 g of 5,5-dimethyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in the form of amorphous powder whose characteristics are the following:

TPL: 136°C;

MS (IE): m/z = 438 M+;

m/z = 423 (M - CH3)+, the peak of the molecular ion;

m/z = 395 (M - C2H5N)+;

m/z = 369 (M - CF3)+;

m/z = 121 C7H9N2+;

m/z = 44 C2H6N+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1.14 in (t, J=7 Hz, 3H), of 1.44 (s, 6N), 3,26 (m, 2H), 4,47 (ush., 2H), 6,40 (t ush., J= 5.5 Hz, 1H), 6,45 (ush., 1H), 6,50 (l ush., J= 5.5 Hz, 1H), 7,69 (l ush., J= 8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 7,92 (d, J=5.5 Hz, 1H).

Example 231

5,5-Dimethyl-1-(2-benzylaminopurine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of benzylamine, placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated with stirring magnet m is szalkai at a temperature of 200° C for about 30 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. The fraction collected between 10 ml and 50 ml, concentrated to dryness under reduced pressure. Thus receive 0.035 g of 5,5-dimethyl-1-(2-benzylaminopurine-4-ylmethyl)-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in the form of amorphous powder whose characteristics are the following:

TPL: 144°C;

MS (IE): m/z = 500 M+, the peak of the molecular ion;

m/z = 431 (M - CF3)+;

m/z = 196 C13H12N2+;

m/z = 106 C7H8N+;

m/z = 91 C7H7+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1.39 in (C, 6N), 4,47 (ush., 2H), 4,48 (d, J=6 Hz, 2H), 6,51(ush., 1H), 6,54 (l ush., J=5.5 Hz, 1H), 7,02 (t ush., J=6 Hz, 1H), 7,15-to 7.35 (m, 5H), 7,68 (l ush., J=8.5 Hz, 2H), 7,89 (d, J=8.5 Hz, 2H), 7,92 (d, J=5.5 Hz, 1H).

Example 232

5,5-Dimethyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of p-methoxybenzylamine, placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 30 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, filled with 2 g of silicon dioxide, 15-35 μm, and condition, then elute with dichloromethane with a flow rate of 5 ml per minute. Fractions between 5 ml and 5 ml, concentrate to dryness under reduced pressure. Thus receive 0.035 g of 5,5-dimethyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of amorphous powder whose characteristics are the following:

MS (IE): m/z = 530 M+;

m/z = 461 (M - CF3)+;

m/z = 136 C8H10NO+;

m/z = 121 C8H9O+, the peak of the molecular ion.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1.39 in (C, 6N), and 3.72 (s, 3H), 4,39 (d, J=5.5 Hz, 2H), 4,46 (c ush., 2H), 6.48 in (ush., 1H), 6,53 (l ush., J=5.5 Hz, 1H), 6.87 in (l ush., J=8.5 Hz, 2H), 6,93 (t, J=5.5 Hz, 1H), 7,25 (l ush., J=8.5 Hz, 2H), 7,68 (l ush., J=8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 7,92 (d, J=5.5 Hz, 1H).

Example 233

5,5-Dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution of 0.035 g of 5,5-dimethyl-1-[2-(4-methoxybenzylamine)-pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione in 0.5 ml of dichloromethane, at a temperature of about 20°add 0.5 ml triperoxonane acid, stirring maintain at this temperature for 5 hours. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN standard 1225-6027 containing 5 g SCX phase, to the which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. So get 0,015 g of 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a powder whose characteristics are the following:

TPL: 161°C.

MS (IE): m/z = 410 M+, the peak of the molecular ion;

m/z = 395 (M - CH3)+;

m/z = 219 C8H4NOSF3+;

m/z = 148 C7H6N3O+;

m/z = 107 C6H7N2+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,43 (C, 6N), 4,46 (ush., 2H), 5,86 (ush., 2H), 6,46 (ush., 1H), 6,53 (l ush., J=5.5 Hz, 1H), 7,69 (l ush., J=8.5 Hz, 2H), to 7.84 (d, J=5.5 Hz, 1H), 7,89 (l ush., J=8.5 Hz, 2H).

Example 234

5,5-Dimethyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

The solution 0,050 g of 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 5 ml of acetic anhydride is stirred in an inert atmosphere of argon for 24 hours at a temperature of about 80°C. the Reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in the colon is the BOND ELUT VARIAN according to the standard 1225-6027, containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. So get 0,006 g of 5,5-dimethyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a powder whose characteristics are the following:

MS (IE): m/z = 452 M+;

m/z = 410 (M - C2H2O)+, the peak of the molecular ion;

m/z = 395 (m/z = 410 - CH3)+;

m/z = 219 C8H4NOSF3+;

m/z = 150 C8H10N2O+;

m/z = 107 C6H7N2+;

m/z = 43 C2H3O+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,44 (ush., 6N), 2,11 (s, 3H)and 4.65 (ush., 2H), 7,15 (l ush., J=5.5 Hz, 1H), 7,68 (l ush., J=8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 8,14 (ush., 1H), 8,27 (d, J=5.5 Hz, 1H), 10,49 (m, 1H).

Example 235

5,5-Dimethyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution 0,029 g of di-tert-BUTYLCARBAMATE in 0,65 ml tert-butyl alcohol, in an inert atmosphere of argon and at a temperature of about 20°With small portions add 0.05 g of 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione, stirring under arrivat at this temperature for 24 hours. The reaction mixture is concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 16 mm, was filled with 5 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (8:2, vol/vol). The fraction collected between 260 ml and 400 ml, concentrated under reduced pressure. Thus receive 0.035 g of 5,5-dimethyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IC): m/z = 511 MN+, the peak of the molecular ion.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,43 (C, 6N), for 1.49 (s, N), 4,63 (ush., 2N), was 7.08 (DD ush., J=5.5 and 1.5 Hz, 1H), 7,68 (l ush., J=9 Hz, 2H), 7,84 (ush, 1H), 7,87 (l ush., J=9 Hz, 2H), 8,19 (d, J=5.5 Hz, 1H), 9,73 (ush., 1H).

Example 236

5,5-Dimethyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution 0,050 g of 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 0.4 ml of pyridine, in an inert atmosphere of argon and at a temperature of about 20°add 0,010 ml methanesulfonanilide, stirring maintain at this temperature for 2 hours. The reaction mixture is poured into 50 ml saturated sodium hydrogen carbonate solution, and then the extras is giraut 2 times 50 ml of ethyl acetate. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. So get 0,020 g of 5,5-dimethyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a white powder whose characteristics are the following:

TPL: 208°C.

MS (IE): m/z = 488 M+, the peak of the molecular ion;

m/z = 473 (M - CH3)+;

m/z = 409 (M - SO2CH3)+;

m/z = 219 C8H4NOSF3+;

m/z = 185 C7H9N2O2S+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,45 (s, 6N), with 3.27 (m, 3H), 4,63 (ush, 2H), 6,95-7,10 (m, 2H), 7,68 (l ush., J=8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 8,17 (m, 1H).

Example 237

5,5-Dimethyl-1-(2-methoxycarbonylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution 0,100 g of 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 1.5 ml of pyridine, in an inert atmosphere of argon and at a temperature of about 20°add 0,056 ml methylcarbamate, stirring maintain at this temperature for 20 hours, again add 0,056 ml methylcarbamate. Mixing support at this temperature for 20 hours. The reaction mixture is treated with 5 ml of ethyl acetate, then the industry is up sequentially with 5 ml of water, 5 ml of a saturated solution of sodium chloride, then 5 ml of water. The organic phase is dried over magnesium sulfate, filtered, and then concentrated under reduced pressure. The obtained residue is purified on a column KROMASIL C18, 5 μm (100 mm x 20 mm), elwira linear gradient from 5% to 95% of acetonitrile containing 0.07 per cent (vol/vol) triperoxonane acid (TFUC) in water containing 0.07 per cent (vol/vol) TFUCK, with a flow rate of 10 ml/min Fraction containing the target product are concentrated to dryness under reduced pressure. The resulting residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. So get 0,024 g of 5,5-dimethyl-1-(2-methoxycarbonylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a solid white color, the characteristics of which are the following:

MS (IE): m/z = 468 M+, the peak of the molecular ion;

m/z = 453 (M - CH3)+;

m/z = 410 (M - C2H2O2)+;

m/z = 219 C8H4NOSF3+;

m/z = 166 C8H10N2O2+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ WMD: the 1.44 (s, 6N), 3,70 (s, 3H)and 4.65 (ush., 2H), 7,12 (DD, J=5.5 and 2 Hz, 1H), 7,69 (l ush., J=9 Hz, 2H), 7,89 (l ush., J=9 Hz, 2H), of 7.90 (ush., 1H), 8,23 (d, J=5.5 Hz, 1H), 10,18 (ush., 1H).

Example 238

5,5-Dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution of 0,417 g of 5,5-dimethyl-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione in 20 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of approximately 0°add 0.1 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution 0,380 g of 2-chloro-4-(methyl bromide)of pyridine in 20 ml of anhydrous dimethylformamide, and then, after 10 minutes of reaction, ice water. The reaction mixture is treated with 400 ml of ethyl acetate, then washed with 400 ml of water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 27 mm, filled with 25 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (8:2, vol/vol). The fraction collected between 150 ml and 350 ml, concentrated to dryness under reduced pressure. Thus obtain 0.3 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of the eristic which is the following:

MS (IE): m/z = 463 M+, the peak of the molecular ion;

m/z = 448 (M - CH3)+;

m/z = 253 C8H3NOSClF3+;

m/z = 167 C7H4N2OCl+;

m/z = 126 C6H5NCl+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,43 (C, 6N), 4,68 (ush., 2H), 7,49 (l ush., J=5.5 Hz, 1H), 7,63 (ush., 1H), 7,71 (DD, J=9 and 3 Hz, 1H), of 7.97 (d, J=3 Hz, 1H), with 8.05 (d, J=9 Hz, 1H), scored 8.38 (d, J=5.5 Hz, 1H).

Getting 5,5-dimethyl-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione

To a suspension of 1.97 g of diphosgene and 0.03 g of vegetable carbon black in 22 ml of toluene, at a temperature of about -20°within 30 minutes, add a solution of 2 g of 3-chloro-4-triftormetilfullerenov in 22 ml of toluene. The mixture is stirred until it reaches a temperature of about 20°With, then refluxed for 3 hours. The mixture is cooled to a temperature of about 20°C, then filtered through celite, the filtrate is added 1.35 g of methyl ester hydrochloride α-aminoadamantane acid, 15 ml of toluene and of 2.23 ml of triethylamine. The thus obtained mixture is refluxed for 24 hours, then cooled to a temperature of about 20°C. the Reaction mixture was concentrated under reduced pressure, the obtained residue is purified flash chromatography on a column of diameter 37 mm, filled with silica, 20-40 μm, pricesconditions, then elute with a mixture of cyclohexane/ethyl acetate (5:5, vol/vol). The fraction collected between 110 ml and 250 ml, concentrated to dryness under reduced pressure and thus obtained 2 g of 5,5-dimethyl-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 338 M+, the peak of the molecular ion;

m/z = 253 C8H3NOSClF3+;

m/z = 184 (m/z = 253 - CF3)+;

m/z = 84 C4H6NO+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,42 (C, 6N), 7,63 (DD, J=8.5 and 2.5 Hz, 1H), of 7.90 (d, J=2.5 Hz, 1H), 8,02 (d, J=8.5 Hz, 1H), up 8.75 (m, 1H).

Example 239

5,5-Dimethyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.3 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.2 ml of N-methylpyrrolidone-2, 0.4 ml of p-methoxybenzylamine, placed in a microwave Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 70 minutes. The reaction mixture was purified flash chromatography, using a column with a diameter of 37 mm, filled with 50 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (8:2, vol/vol)Fractie, collected between 470 ml and 640 ml, concentrated to dryness under reduced pressure. So get 0,091 g of 5,5-dimethyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 564 M+;

m/z = 495 (M - CF3)+;

m/z = 136 C8H10NO+;

m/z = 121 C8H9O+, the peak of the molecular ion.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,38 (c, 6N), 3,71 (s, 3H), 4,39 (d, J=5.5 Hz, 2H), 4,45 (ush., 2H), 6.48 in (ush., 1H), 6,53 (l ush., J=5.5 Hz, 1H), 6,85 (d, J=8.5 Hz, 2H), 6.89 in (t, J=5.5 Hz, 1H), 7,24 (d, J=8.5 Hz, 2H), 7,69 (DD, J=8.5 and 2.5 Hz, 1H), 7,92 (d, J=5.5 Hz, 1H), 7,95 (d, J=2.5 Hz, 1H), of 8.06 (d, J=8.5 Hz, 1H).

Example 240

5,5-Dimethyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.4 ml of N-methylpyrrolidone-2, 0,044 g etilamingidrokhlorida, 0,120 ml of triethylamine are placed in a microwave oven Personal Chemistry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 70 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure, the Thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. So get 0,029 g of 5,5-dimethyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione, the characteristics of which are the following:

MS (IE): m/z = 472 M+;

m/z = 457 (M - CH3)+, the peak of the molecular ion;

m/z = 429 (M - C2H5N)+;

m/z = 403 (M - CF3)+;

m/z = 121 C7H9N2+;

m/z = 44 C2H6N+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1.14 in (t, J=7 Hz, 3H), USD 1.43 (s, 6N), with 3.27 (m, 2H), 4,46 (ush., 2H), 6,38 (t ush., J=5.5 Hz, 1H), 6,45 (ush., 1H), 6,51 (l ush., J=5.5 Hz, 1H), of 7.70 (DD, J=8.5 and 2.5 Hz, 1H), 7,92 (d, J=5.5 Hz, 1H), of 7.96 (d, J=2.5 Hz, 1H), of 8.06 (d, J=8.5 Hz, 1H).

Example 241

5,5-Dimethyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione

Hermetically sealed tube with a capacity of 2.5 ml containing 0.1 g of 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione, 0.5 ml of N-methylpyrrolidone-2, 0.030 mg of methylaminopropane, 0,120 ml of triethylamine are placed in a microwave oven Personal Chemisry Emrys Optimiser. The mixture is irradiated under stirring with a magnetic stirrer at a temperature of 200°C for about 70 minutes. The reaction mixture was purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 20 mm, filled with 10 g of silica, 20-40 μm, and condition, then elute with dichloromethane with a flow rate of 8 ml per minute. The fraction collected between 70 ml and 100 ml, concentrate to dryness under reduced pressure. So get 0,015 g of 5,5-dimethyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of an amorphous white powder, the characteristics of which are the following:

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,43 (C, 6N), 2,77 (d, J=5 Hz, 3H), 4,48 (ush., 2H), 6,40 (kV ush., J=5 Hz, 1H), 6,46 (ush., 1H), 6,54 (l ush., J=5.5 Hz, 1H), of 7.70 (DD, J=8.5 and 3 Hz, 1H), 7,94 (d, J=5.5 Hz, 1H), of 7.97 (d, J=3 Hz, 1H), of 8.06 (d, J=8.5 Hz, 1H).

Example 242

5,5-Dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione

To a solution 0,080 g of 5,5-dimethyl-1-[2-(4-methoxybenzylamine)-pyridine-4-ylmethyl]-3-(3-chloro-4-triftormetilfullerenov)-imidazolidin-2,4-dione in 1 ml dichloromethane, at a temperature of about 20°add 3 ml triperoxonane acid, stirring maintain at this temperature for about 16 hours. The reaction mixture is concentrated to dryness under reduced pressure. The resulting residue is purified preparative LC/MS. The fraction containing the target product are concentrated to dryness under reduced pressure. The thus obtained residue is treated with methanol, then bring in column BOND ELUT VARIAN according to the standard 1225-6027 containing 5 g SCX phase, which is air-conditioned with methanol. Rinse with methanol, and then elution with 2 M ammonia solution in methanol. The ammonia fractions are concentrated to dryness under reduced pressure. So get 0,027 g of 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(3-chloro-4-triftormetilfullerenov)imidazolidin-2,4-dione in the form of a powder whose characteristics are the following:

MS (IE): m/z = 444 M+, the peak of the molecular ion;

m/z = 429 (M - CH3)+;

m/z = 148 C7H6N3O+;

m/z = 107 C6H7N2+.

1H-NMR spectrum (300 M is C, (CD3)2SO-d6) δ in ppm: 1,43 (C, 6N), 4,46 (ush., 2H), 5,86 (ush., 2H), 6,46 (ush., 1H), 6,54 (DD ush., J=5.5 and 1.5 Hz, 1H), of 7.70 (DD, J=8.5 and 2.5 Hz, 1H), 7,86 (d, J=5.5 Hz, 1H), of 7.97 (d, J=2.5 Hz, 1H), of 8.06 (d, J=8.5 Hz, 1H).

Example 243

5,5-Dimethyl-1-(2,6-dibromopyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione

To a solution of 0,230 g of 5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione in 2 ml of anhydrous dimethylformamide, in an inert atmosphere of argon and at a temperature of about 20°add 0.036 g of sodium hydride, stirring maintain at this temperature for 30 minutes, add a solution 0,349 g of 2,6-dibromo-4-(methyl bromide)of pyridine in 3 ml of anhydrous dimethylformamide, and then, after 20 minutes of reaction, ice water. The reaction mixture is treated with ethyl acetate, then washed with water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 27 mm, filled with 25 g of silica, 20-40 μm, and condition, then elute with dichloromethane. The fraction collected between 65 ml 135 ml, concentrated under reduced pressure. Thus obtain 0.25 g of 5,5-dimethyl-1-(2,6-dibromopyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione, the characteristics of which are the following:

<> MS (IC): m/z = 569 MNH4+, the peak of the molecular ion;

m/z = 552 MH+;

m/z = 474 (M - Br + 2H)+;

m/z = 396 (m/z = 474 - Br + H)+.

1H-NMR spectrum (300 MHz, (CD3)2SO-d6) δ in ppm: 1,45 (s, 6N), 4,67 (ush., 2H), 7,72 (l ush., J=8 Hz, 2H), 7,83 (s, 2H), 7,89 (l ush., J=8 Hz, 2H).

Connection 5,5-dimethyl-3-(4-triftormetilfullerenov)-imidazolidin-2,4-dione described in example 211.

Synthesis reagents

Reference example a

2-Chloro-4-(methyl bromide)pyridine

To a solution of 0,706 g dibromothiophene 9.5 ml of dichloromethane, in an inert atmosphere of argon and at a temperature of about 20°With added dropwise a solution of 0.2 g of 2-chloro-4-(hydroxymethyl)pyridine and 2.5 ml of dichloromethane, stirring maintain at this temperature for about 1 hour. The reaction medium is treated with 50 ml of dichloromethane, then washed with 3 times 50 ml of water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 20 mm, filled with 10 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (8:2, vol/vol) with a flow rate of 8 ml/min Fractions collected between 8 ml and 24 ml, concentrated under reduced pressure. So get 0.1 g 2-chlorine is-4-(methyl bromide)pyridine.

Reference example 208b

2-Chloro-4-(hydroxymethyl)pyridine

To a solution of 1.7 g of ethyl-2-chloropyridin-4-carboxylate in 20 ml of ethanol, in an inert atmosphere of argon and at a temperature of approximately 0°With, in the form of several portions add 2,04 g of sodium borohydride. The reaction mixture is refluxed under stirring for 3 hours, then concentrated to dryness under reduced pressure. The thus obtained residue is treated with dichloromethane, then washed with water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. Thus obtain 1 g of 2-chloro-4-(hydroxymethyl)pyridine.

Reference example s

Ethyl-2-chloropyridin-4-carboxylate

To a solution of 2.2 g of 2-chloropyridin-4-carboxylic acid in 30 ml of ethanol was added 1 ml of concentrated sulfuric acid. The reaction mixture is refluxed under stirring for 16 hours, then concentrated to dryness under reduced pressure. The thus obtained residue is treated with 30 ml of water, extracted with 3 times 30 ml of dichloromethane. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. The thus obtained oil is purified by filtration through 13 g of silicon dioxide, elwira dichloromethane. Faction is, containing the target product are concentrated to dryness under reduced pressure. Thus obtained 2.1 g of ethyl-2-chloropyridin-4-carboxylate.

Reference example a

2 Ethoxy-4-(methyl bromide)pyridine

To a solution of 1,025 g dibromothiophene in 12 ml of dichloromethane, in an inert atmosphere of argon and at a temperature of about 20°With added dropwise a solution of 0.31 g of 2-ethoxy-4-(hydroxymethyl)pyridine in 6 ml of dichloromethane, stirring maintain at this temperature for about 1 hour. The reaction medium is treated with 100 ml dichloromethane, then washed with 3 times 100 ml of water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 27 mm, filled with 20 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (9:1, vol/vol) with a flow rate of 8 ml/min Fractions collected between 80 ml and 180 ml concentrate under reduced pressure. So get of 0.37 g of 2-ethoxy-4-(methyl bromide)pyridine.

Reference example 209b

2 Ethoxy-4-(hydroxymethyl)pyridine

To a solution of 0,524 g ethyl-2-ethoxypyridine-4-carboxylate 5.2 ml of ethanol, in an inert atmosphere of argon and at a temperature of approximately 0°With as several servings EXT is make 0,508 g of sodium borohydride. The reaction mixture is refluxed under stirring for 3 hours, then concentrated to dryness under reduced pressure. The thus obtained residue is treated with 50 ml of dichloromethane, then washed with 50 ml of water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. So get 0,310 g 2 ethoxy-4-(hydroxymethyl)pyridine.

Reference example s

Ethyl-2-ethoxypyridine-4-carboxylate

To a solution of 1 g of 2-herperidin-4-carboxylic acid in 15 ml of ethanol is added 0.5 ml of concentrated sulfuric acid. The reaction mixture is refluxed under stirring for 48 hours, then concentrated to dryness under reduced pressure. The thus obtained residue is treated with 100 ml water, then extracted with 3 times 100 ml of dichloromethane. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. The thus obtained crude product is purified flash chromatography, using a column with a diameter of 37 mm, filled with 50 g of silica, 20-40 μm, and condition, then elute with a mixture of dichloromethane/methanol (90:10, vol/vol) with a flow rate of 8 ml/min Fractions collected between 350 ml and 390 ml, concentrated under reduced pressure. the thus get 0,524 g ethyl-2-ethoxypyridine-4-carboxylate in the form of oil.

Reference example 210A

2-Ethyl-4-(methyl bromide)pyridine

To a solution of 1.25 g of dibromothiophene in 4 ml of dichloromethane, in an inert atmosphere of argon and at a temperature of approximately 0°With added dropwise a solution of 0.3 g of 2-ethyl-4-(hydroxymethyl)pyridine in 3.5 ml of dichloromethane. The mixture is stirred for about 1 hour until a temperature of about 20°C. the Reaction medium is treated with 50 ml of dichloromethane, then washed with 3 times 50 ml of water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 20 mm, filled with 10 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (9:1, vol/vol) with a flow rate of 8 ml/min Fractions collected between 80 ml and 120 ml concentrate under reduced pressure. So get 0,062 g 2-ethyl-4-(methyl bromide)pyridine.

Reference example 210b

2-Ethyl-4-(hydroxymethyl)pyridine

The solution to 5.08 g of ethyl-2-ethylpyridine-4-carboxylate in 53 ml of ethanol, in an inert atmosphere of argon and at a temperature of approximately 0°With, in the form of several portions add are 5.36 g of sodium borohydride. The reaction mixture is refluxed under stirring for 3 hours, then conc the shape to dryness under reduced pressure. The thus obtained residue is treated with 500 ml of dichloromethane, then washed with 500 ml of water. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. So get to 3.16 g of 2-ethyl-4-(hydroxymethyl)pyridine.

Reference example s

Ethyl-2-ethylpyridine-4-carboxylate

To a solution of 5 g of 2-ethylpyridine-4-carboxylic acid in 75 ml of ethanol is added 2.35 ml of concentrated sulfuric acid. The reaction mixture is refluxed under stirring for about 64 hours, then concentrated to dryness under reduced pressure. The thus obtained residue is treated with 500 ml of water, then extracted with 500 ml of dichloromethane. The organic phase is dried over magnesium sulfate, filtered, then concentrated to dryness under reduced pressure. So get to 5.08 g of ethyl-2-ethylpyridine-4-carboxylate in the form of oil.

Reference example a

2-Bromo-4-(methyl bromide)pyridine

To a solution of 0.172 g of 2-bromo-4-methylpyridine in 2.5 ml of carbon tetrachloride, in an inert atmosphere of argon and at a temperature of about 20°add 0,073 ml of acetic acid, the mixture while stirring bring to a temperature of 50°Since, at this temperature successively added 0,356 g of N-bromosuccinimide and 0,048 g benzoyl peroxide is. The reaction mixture was kept at a temperature of 80°C for about 18 hours. Reaction medium, after cooling, make a column with a diameter of 20 mm, filled with 10 g of silica, 20-40 μm, pre-conditsionirovanie, then carry out the elution dichloromethane with a flow rate of 5 ml/min Fractions collected between 30 ml and 40 ml, concentrated under reduced pressure. So get 0,071 g of 2-bromo-4-(methyl bromide)pyridine.

Reference example a

2-Fluoro-4-(methyl bromide)pyridine

To a solution of 0,111 g of 2-fluoro-4-methylpyridine in 2.5 ml of carbon tetrachloride, in an inert atmosphere of argon and at a temperature of about 20°add 0,073 ml of acetic acid, the mixture while stirring bring to a temperature of 50°Since, at this temperature successively added 0,356 g of N-bromosuccinimide and 0,048 g of benzoyl peroxide. The reaction mixture was kept at a temperature of 80°C for about 16 hours. Reaction medium, after cooling, make a column with a diameter of 20 mm, filled with 10 g of silica, 20-40 μm, pre-conditsionirovanie, then carry out the elution dichloromethane with a flow rate of 5 ml/min Fractions collected between 28 ml 38 ml, concentrated under reduced pressure. So get 0,063 g of 2-fluoro-4-(methyl bromide)pyridine.

Reference example a

2-Cyano-4-(methyl bromide)pyridi the

To a solution of 0,236 g 2-cyano-4-methylpyridine in 5 ml of carbon tetrachloride, in an inert atmosphere of argon and at a temperature of about 20°add 0,146 ml of acetic acid, the mixture while stirring bring to a temperature of 50°Since, at this temperature successively added 0,712 g of N-bromosuccinimide and 0,096 g of benzoyl peroxide. The reaction mixture was kept at a temperature of 80°C for about 18 hours. Reaction medium, after cooling, make a column with a diameter of 27 mm, filled with 25 g of silica, 20-40 μm, pre-conditsionirovanie, then carry out the elution dichloromethane with a flow rate of 10 ml/min Fractions collected between 140 ml and 175 ml, concentrated under reduced pressure. So get 0,097 g 2-cyano-4-(methyl bromide)pyridine.

Reference example a

2,6-Dibromo-4-(methyl bromide)pyridine

To a solution of 0.95 g of dibromothiophene in 5 ml of dichloromethane, in an inert atmosphere of argon and at a temperature of approximately 0°With added dropwise a solution of 0.5 g of 2,6-dibromo-4-(hydroxymethyl)pyridine in 7 ml of dichloromethane. The mixture is stirred for about 2 hours until the temperature is about 20°C. the Reaction medium is treated with 100 ml dichloromethane, then washed with 100 ml of water. The organic phase is dried over magnesium sulfate, filtered, then concentrated of Dosh is under reduced pressure. Thus obtained residue is purified flash chromatography, using a column with a diameter of 37 mm, filled with 50 g of silica, 20-40 μm, and condition, then elute with a mixture of cyclohexane/ethyl acetate (9:1, vol/vol) with a flow rate of 8 ml/min Fractions collected between 135 ml and 200 ml, concentrated under reduced pressure. So get 0,349 g of 2,6-dibromo-4-(methyl bromide)pyridine.

A General method of obtaining the products of examples 244-255

To a suspension 0,064 ml of 0.53 mmol) diphosgene and 20 mg vegetable soot in 1 ml of toluene, at a temperature of about -20°C, add a solution 0,481 mmol aniline derivative in 0.6 ml of toluene. The mixture is stirred until it reaches a temperature of about 20°With, then refluxed for 3 hours. The mixture is cooled to a temperature of about 20°C, then filtered through celite. To the filtrate add a solution of 100 mg (0.48 mmol) of the methyl ester of 2-methyl-2-[(pyridine-4-ylmethyl)amino]propanoic acid in 0.6 ml of toluene. The thus obtained mixture is refluxed for 16 hours, then cooled to a temperature of about 20°C. the Precipitate is filtered off and the filtrate is concentrated under reduced pressure. The resulting residue is purified preparative LC/MS.

Summary table source derivatives of aniline and the resulting products

Example No.The original name derived anilineThe amount derived aniline (mg)The structure of the obtained productThe name of the resulting productBrutto-formula obtained productThe molecular weight of the obtained productReceiving-TES quantity (mg)
2442-nitro-4-(triptoreline)-aniline106,75,5-dimethyl-3-

(2-nitro-4-triptoreline-phenyl)-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2
C18

H15

F3N4

O5
424,3454,2
2454-(1,1,2,2-tetrafluoroethoxy)-anilineto 100.45,5-dimethyl-1-pyridin-4-ylmethyl-3-[4-(1,1,2,2-titrator-ethoxy)-phenyl]-imidazolidin-2,4-dione-2C19

H17

F4N3

O3
411,3632,1
2464-(deformedarse)-aniline76,43-(4-deformedarse-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18

H17

F2N3

O3
361,35a 3.9
2473-chloro-4-(Tr is formatosi)-aniline 101,63-(3-chloro-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18

H15

Cl F3 N3 O3
413,7946,2
2483-bromo-4-(triptoreline)-aniline122,93-(3-bromo-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15

Br F3 N3 O3
458,2443,2
2492,6-dichloro-4-(triptoreline)-aniline118,13-(2,6-dichloro-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H14 Cl2 F3 N3 O3448,23to 19.9
2503-chloro-4-(trifter-methylthio)aniline109,33-(3-chloro-4-trifluoromethyl-sulfanilyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15

ClF3 N3O2S
429,8533
2512.2-debtor-5-aminobenzothiazole83,13-(2,2-debtor-1,3-benzodioxol-5-yl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-24-Dion-2 C18 H15 F2 N3 O4375,337,4
2522-bromo-4-(triptoreline)-aniline122,93-(2-bromo-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 Br F3 N3 O3458,24of 21.9
2534-(getattr-propylthio)aniline140,83-(4-heptafluoropropyl-sulfanilyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C20 H16 F7 N3 O2S495,42a 38.5
2542-methyl-4-(triptoreline)-aniline91,85,5-dimethyl-3-(2-methyl-4-triptoreline-phenyl)-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C19 H18 F3 N3 O3393,3768,8
2552-chloro-4-(triptoreline)-aniline101,63-(2-chloro-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 Cl F3 N3 O3413,7977,6

Summary table of physicochemical characteristics of the obtained products

Example No.The name of the resulting productGross-form-La obtained productThe molecular weight of the obtained productDescription of the mass spectrum (electron impact)Description of the mass spectrum (analytical LC/MS); hold time-

tion; m/z
Description NMR spectrum (1H-NMR spectrum (300 MHz, (CD3)2SO-d6that δ in ppm))
2445,5-dimethyl-3-

(2-nitro-4-triptoreline-phenyl)-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2
C18 H15 F3 N4 O5424,34m/z=424 M+.

m/z=409 (M-CH3)+

m/z=407 (M-OH)+

m/z=378 (M-NO2)+.

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+

the peak of the molecular ion
1.44MB (ush., 6N), 4,69 (ush, 2H), 7,41 (l ush., J=5.5 Hz, 2H), 7,98 (d, J=8.5 Hz, 1H), 8,07 (l ush., J=8.5 Hz, 1H), 8,29 (d, J=2.5 Hz, 1H), 8,56 (l ush., J=5.5 Hz, 2H)
2455,5-dimethyl-1-pyridin-4-ylmethyl-3-[4-(1,1,2,2-tetrafluoroethoxy)-phenyl]-imidazolidin-2,4-dione-2C19 H17 F4 N3O3411,36m/z=411 M+. the peak of the molecular ion battery

m/z=396 (M-CH3)+

m/z=294

(m/z=396 - C2H2F4)+

m/z=235 C9H5NO2F4+.

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+
of 1.43 (s, 6N)and 4.65 (s, 2H), 6,85 (TT, J=51 and 3 Hz, 1H),

7,46 (m, 4H), a 7.62 (dt, J=8.5 and 2.5 Hz, 2H), 8,56 (DD, J=6 and 1.5 Hz, 2H)
246 3-(4-deformational)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H17 F2 N3 O3361,35t=2,64 min

m/z=362 (M+1)
2473-(3-chloro-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 Cl F3 N3 O3413,79m/z=413 M+.

m/z=398 (M-CH3)+

m/z=237 8H3NO2ClF3+.

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+

the peak of the molecular ion
of 1.43 (s, 6N), of 4.66 (s, 2H), 7,46 (d, J=6 Hz, 2H), 7,66 (DD, J=8.5 and 2.5 Hz, 1H), to 7.77 (DD ush., J=8.5 and 1 Hz, 1H), to 7.93 (d, J=2.5 Hz, 1H), 8,55 (l ush., J=6 Hz, 2H)
2483-(3-bromo-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 Br F3 N3 O3458,24m/z=457 M+.

m/z=442 (M-CH3)+

m/z=281 C8H3NO2BrF3+.

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+

the peak of the molecular ion
of 1.43 (s, 6N)and 4.65 (s, 2H), 7,46 (l ush., J=6 Hz, 2H), 7,68 (DD, J=8.5 and 2.5 Hz, 1H), 7,74 (l ush., J=8.5 Hz, 1H), with 8.05 (d, J=2.5 Hz, 1H), 8,55 (DD, J=6 and 1.5 Hz, 2H).
2493-(2,6-dichloro-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H14 Cl2 F3 N3 O3448,23m/z=447 M+.

m/z=432 (M-CH3)+

m/z=412 (M-Cl)+.

m/z=271 C8H2NO2Cl2F3+.

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+

the IR molecular ion
of 1.47 (s, 6N), to 4.73 (s, 2H), 7,47 (l ush., J=6 Hz, 2H), 8,00 (ush., 2H), 8,58 (DD, J=6 and 1.5 Hz, 2H).
2503-(3-chloro-4-trifluoromethyl-sulfanilyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 Cl F3 N3 O2 S429,85m/z=429 M+. the peak of the molecular ion battery

m/z=414 (M-CH3)+

m/z=253

C8H3NOSClF3+.

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+
of 1.43 (s, 6N), of 4.66 (s, 2H), 7,46 (l ush., J=6 Hz, 2H), of 7.70 (DD, J=8.5 and 2 Hz, 1H), of 7.97 (d, J=2 Hz, 1H), with 8.05 (d, J=8.5 Hz, 1H), 8,54 (DD, J=6 and 1.5 Hz, 2H)
2513-(2,2-debtor-1,3-benzodioxol-5-yl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 F2 N3O4375,33t=2,80 min m/z=376 (M+1)
2523-(2-bromo-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 Br F3 N3 O3458,24m/z=457 M+.

m/z=414 (M-CH3)+

m/z=378 (M-Br)+. The peak of the molecular ion battery

m/z=350

(m/z=378-CO)+

m/z=281

C8H3NO2BrF3+.

m/z=244

(m/z=378 -

C7H6N2O)+

m/z=147

C9H11N2+

m/z=133

C7H5N2O+

m/z=92 C6H6N+
of 1.43 (s, 3H), of 1.48 (s, 3H), 4,68 (AB isol., J=17 Hz, 2H), 7,42 (l ush., J=6 Hz, 2H), 7,66 (DD ush., J=8.5 and 2 Hz, 1H), 7,83 (d, J=8.5 Hz, 1H), 8,07 (l ush., J=2 Hz, 1H), 8,56 (DD, J=6 and 1.5 Hz, 2H).
2533-(4-GE is cafebabel-sulfanilyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2 C20 H16 F7 N3 O2 S495,42m/z=495 M+. the peak of the molecular ion battery

m/z=480 (M-CH3)+

m/z=319

C10H4NOSF7+.

m/z=150

(m/z=319-C3F7)+

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+
1,43 (c, 6H), 4,66 (c, 2H), 7,46 (l ush., J=6 Hz, 2H), 7,71 (l ush., J=8.5 Hz, 2H), 7,89 (l ush., J=8.5 Hz, 2H), 8,55 (DD, J=6 and 1.5 Hz, 2H)
2545,5-dimethyl-3-(2-methyl-4-triptoreline-phenyl)-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C19 H18 F3 N3 O3393,37m/z=393 M+. the peak of the molecular ion battery

m/z=378 (M-CH3)+.

m/z=217

C9H6NO2F3+

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+
of 1.43 and 1.44 (2 s, 6N),

of 2.21 (s, 3H)and 4.65 (ush., 2N), was 7.36 (d ush., J=8.5 Hz, 1H), 7,42 (l ush., J= 6 Hz, 2H), 7,45 (ush., 1H), 7,55 (d, J=8.5 Hz, 1H), 8,55 (DD, J=6 and 1.5 Hz, 2H).
2553-(2-chloro-4-triptoreline-phenyl)-5,5-dimethyl-1-pyridin-4-ylmethyl-imidazolidin-2,4-dione-2C18 H15 Cl F3 N3 O3413,79m/z=413 M+.

m/z=398 (M-CH3)+

m/z=378 (M-Cl)+. The peak of the molecular ion battery

m/z=350

(m/z=378-CO)+

m/z=237 C8H3NO2ClF3+.

m/z=147 C9H11N2+

m/z=133 C7H5N2O+

m/z=92 C6H6N+
1,43 (c, 3H), of 1.48 (s, 3H), 4,67 (ush., 2H), 7,42 (l ush., J=6 Hz, 2H), 7.62mm (DDD, J=8,5-2.5 and 1 Hz, 1H), a 7.85 (d, J=8.5 Hz, 1H), 7,88 (l ush., J=2.5 Hz, 1H), to 8.57 (DD, J=6 and 1.5 Hz, 2H).

The products of examples 256-263 receive according to the above method.

the example 256

Methyl ester 5-(5-hydroxy-4,4-dimethyl-2-oxo-3-quinoline-4-immatrikulation-1-yl)-2-cryptomaterial acid

1H-NMR (DMSO):

(R-318000-112-1): to 1.47 ppm (s, 6N), the 3.89 ppm (s, 3H), of 5.15 ppm (s, 2H), 7,65-7,73 ppm (m, 3H), of 7.82 ppm (t ush., J=8.5 Hz, 1H), 7,92 ppm (DD, J=2,5-8,5 Hz, 1H), 8,07 ppm (d ush., J=8.5 Hz, 1H), 8.17 and ppm (d, J=2.5 Hz, 1H), compared to 8.26 ppm (d ush., J=8.5 Hz, 1H), 8,86 ppm (d, J=4.5 Hz, 1H).

LC/MS: MN+= 488.

Example 257

3-(3-Bromo-4-trifloromethyl)-5,5-dimethyl-1-quinoline-4-immatrikulation-2,4-dione

1H-NMR (DMSO):

(R-31800-101-1): a 1.45 ppm (s, 6N), of 5.15 ppm (s, 2H), 7,62-7,72 ppm (m, 4H), 7,80 ppm (t ush., J=8.5 Hz, 1H), 8,08 ppm (m, 2H), compared to 8.26 ppm (d ush., J=8.5 Hz, 1H), 8,86 ppm (d, J=4.5 Hz).

LC/MS: MN+= 508.

Example 258

3-(3-Chloro-4-trifloromethyl)-5,5-dimethyl-1-quinoline-4-immatrikulation-2,4-dione

1H-NMR (DMSO):

R-31800-105-1 NMR No. 6354R: the 1.44 ppm (s, 6N), 5,14 ppm (s, 2H), to 7.61-to 7.84 ppm (m, 5H), 7,94 ppm (d, J=2.5 Hz, 1H), 8,07 ppm (d ush., J=8.5 Hz, 1H), 8,24 ppm (d ush., J=8.5 Hz, 1H), 8,83 ppm (d, J=4.5 Hz, 1H).

LC/MS: MN+= 464.

Example 259

5-(4,4-Dimethyl-2,5-dioxo-3-quinoline-4-immatrikulation-1-yl)-2-triftorperasin acid

1H-NMR (DMSO):

(R-29798-111-1): to 1.47 ppm (s, 6N), of 5.15 ppm (s, 2H), 7,62-7,72 ppm (m, 3H), 7,81 ppm (t ush., J=8.5 Hz, 1H), 7,88 ppm (DD, J=2,5-8,5 1H), 8,08 ppm (t ush., J=8.5 Hz, 1H), 8,15 ppm (d, J=2.5 Hz, 1H), compared to 8.26 ppm (d ush., J=8.5 Hz, 1H), 8,87 ppm (d, J=4.5 Hz, 1H), and 13.5 ppm (ush., 1H).

LC/MS: MN+= 474.

<> Example 260

5,5-Dimethyl-3-{3-[4-(4-methylpiperazin-1-yl)butyryl]-4-trifloromethyl}-1-quinoline-4-immatrikulation-2,4-dione

1H-NMR (DMSO):

(R-29798-112-1): 1,51 ppm (s, 6N), of 1.97 ppm (m, 2H), 2,82 ppm (s, 3H), 3,0-4,0 ppm (m ush., N), to 5.35 ppm (s, 2H), 7,63 ppm (kV, d, J=1.5 to 8.5 Hz, 1H), set at 7.75 ppm (DD, J=2,5-8,5 Hz, 1H), of 7.82 ppm (d, J= 2.5 Hz, 1H), 7,94 ppm (t ush., J=8.5 Hz, 1H), 8,10 ppm (m, 2H), 8,39 ppm (d ush., J=8.5 Hz, 1H), 8,51 ppm (d ush., J=8.5 Hz, 1H), 8,72 ppm (t ush., J=5.5 Hz, 1H), 9,15 ppm (d, J=5 Hz, 1H), of $ 11.97 ppm (ush., 1H).

MC (EI): M+= 612+.

Example 261

5-(5-Hydroxy-4,4-dimethyl-2-oxo-3-quinoline-4-immatrikulation-1-yl)-2-cryptomaterial acid

In a flask with a capacity of 30 ml, equipped with a magnetic stirrer, septum, above nitrogen, enter:

200 mg (0.41 mmol) of ester in 2 ml of simple ether;

8 mg (0,205 mmol) of LiAlH4or 8 ml of 1 M solution in 2 ml of THF.

The reaction medium is stirred at room temperature for 24 hours.

According to thin-layer chromatography; CH2Cl2/ethyl acetate (8:2): formed product, the more polar than the original product, however, remains the original product.

Again add 0.5 equivalent of LiAlH4and stirred for 5 hours. There remains little of the original product, but processed.

Hydrolyzing, Prilepa water to the reaction medium, and extracted 3 times with 10 ml of ethyl is the Etat. The organic extracts are combined, dried over magnesium sulfate and the ethyl acetate is evaporated. The crude reaction product is purified using an eluting the mixture of CH2Cl2/ethyl acetate (9:1). Thus receive 60 mg of alcohol.

1H-NMR (DMSO): 1,19 ppm (s, 3H), 1,24 ppm (s, 3H), 3,86 (s, 3H), 4.92 in ppm (system AB, J=18 Hz, 2H), are 5.36 ppm (s, 1H), 7,51 ppm (d, J=9.0 Hz, 1H), 7,58 ppm (d, J=4.5 Hz, 1H), 7,66 (m, 1H), 7,80 ppm (m, 1H), 8,00 ppm (DD, J=the 2.5 and 9.0 Hz, 1H), of 8.06 ppm (DD, J=1.5 to 8.5 Hz, 1H), 8,28 ppm (DD, J=1.5 to 8.5 Hz, 1H), 8,33 ppm (d, J=2.5 Hz, 1H), 8,84 ppm (d, J=4.5 Hz, 1H).

LC/MS: MH+= 489.

Example 262

4,4-Dimethyl-3-quinoline-4-ylmethyl-5-thioxo-1-(4-trifloromethyl)imidazolidin-2-he

Within 9 hours refluxed following reaction mixture:

- 317 mg (0,739 .10-3mol) as SB 31051-139,

- 78 mg (0,19-3mol) of Lawesson reagent,

- 1 cm3toluene,

then cooled, filtered and concentrated under reduced pressure. Recuperat a yellow foam which is purified several times by chromatography on silica, elwira a mixture of chloroform/acetone (97:3). Obtain 231 mg of pure resin yellow with Rf= 0,38; theoretically calculated quantity = 329 mg; yield = 70%.

1H-NMR (DMSO), δ in ppm:

(R-31051-146-2): of 1.57 ppm (s, 6N), of 5.24 ppm (s, 2H), EUR 7.57 ppm (m, 2H), 7,63 ppm (d, J=4.5 Hz, 1H), of 7.70 ppm (m, 3H), 7,81 ppm (t ush., J=8.5 Hz, 1H), 8,08 ppm (DD, J=1.5 to 8.5 Hz, 1H), compared to 8.26 ppm (DD, J=1.5 To 8.5 G is, 1H), 8,86 ppm (d, J=4.5 Hz, 1H).

LC/MS: MH+= 446.

Example 263

5,5-Dimethyl-1-quinoline-4-ylmethyl-2-thioxo-3-(4-trifloromethyl)imidazolidin-4-one

At room temperature for 20 hours mix the following reaction mixture:

0.6 g (mmol) of the derivative of quinoline,

- 0,918 g (mmol) thioisocyanate,

- 12 cm3anhydrous THF,

- 0.2 cm3of triethylamine.

Concentrate under reduced pressure, then purified on a column of AIT, 25 g, elwira a mixture of dichloromethane/acetone (95:5). Recuperat product with Rf= 0,12, namely 266 mg; yield = 26%.

1H-NMR (DMSO):

(R-31051-160-2): of 1.55 ppm (s, 6N), to 5.56 ppm (s, 2H), at 7.55 ppm (m, 3H), of 7.69 ppm (m, 3H), of 7.82 ppm (t ush., J=8.5 Hz, 1H), 8,08 ppm (DD, J=1.5 to 8.5 Hz, 1H), 8,28 ppm (DD, J=1.5 to 8.5 Hz, 1H), 8,83 ppm (d, J=4.5 Hz, 1H).

MC: M+= 445+.

The products of examples 264-332 are described below in table 1: these products are obtained, as indicated in the experimental part of this application, and, in particular, as indicated in the case of products of examples 70-200, and, thus, constitute the object examples 264-332 according to the present invention.

Example 333

The pharmaceutical composition

Get tablets that meet the following composition:

the product of example 9..................................0.2 g

excipient for tablets up to the total number.......1 g

(detailed composition of excipient: lactose, talc,

starch, magnesium stearate)

Example 334

The pharmaceutical composition

Get tablets that meet the following composition:

the product according to example 52........................ 0.2 g

excipient ready for tablets up................. 1 g

(specific composition of excipient: lactose, talc, starch, magnesium stearate)

Examples of pharmaceutical compositions 333 and 334 of the above, explain the present invention, keeping in mind that the same preparation can be carried out using other preferred products according to the present invention and they form part of the present invention.

The present invention also includes, as examples, the following products of formula (I): in the following list provides the names of the products of formula (I), such as the above, in which B2 means peredelnyj or finalininkiu radical, these products form part of the present invention can be synthesized by the methods described above to obtain products of formula (I) and, in particular, under the operating conditions described for obtaining the products of examples 61-63:

- 5,5-dimethyl-1-(2-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropylpyridine-4-elmet the l)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2,2'-bipyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-herperidin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ponyride the-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-triptime xifei)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1-methyl-4-piperidinyl)-carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ureidopenicillin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminoethyl anilinopiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-anilinomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylmethylamine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triform toxigenic)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-trifloromethyl them who solidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-amidinopropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-is ion;

- 5,5-dimethyl-1-(3-phenylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3,2'-bipyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-herperidin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-bromopyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminopyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethylaminomethyl-4-yl is ethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-diethylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-chlorobenzylidene-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-acetamidophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1-methyl-4-piperidinyl)-carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxycarbonylamino the pyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-onlinecarisoprodol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ureidopenicillin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-anilinomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-thienyl)sulfonylamino is iridin-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylmethylamine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triptime xifei)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dio is;

- 5,5-dimethyl-1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-amidinopropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 4-(2-methylpyridin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-tert-butylpyridinium)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isobutylpyrazine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexylpiperidine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(3-chlorophenyl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-chlorphen is)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-forfinal)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxyphenyl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2,2'-bipyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-hydroxymethylpropane)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-chloropyridin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-herperidin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-bromopyridin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminopyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminopropyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethylaminomethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropylaminoethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylaminopyrimidine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexylpiperidine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-diethylaminopropyl)-4-elmet is l-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-N-cyclohexyl-N-methylaminomethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-morpholinoethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-pyrazole-1-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-benzoylhydrazone)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminopurine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(3-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-perbenzoate)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxybenzylamine)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-acetamidophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylacetamide the INF)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperazine)acetamidophenyl]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexanecarboxaldehyde)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1-methyl-4-piperidinyl)carboalumination]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-fornicator)aminopyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxycarbonylpyrimidine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropoxycarbonyloxymethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-butoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-diethylaminoethylamine)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chloroanilino)carboalumination]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-onlinecarisoprodol)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminocarbonyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-pyridi is amino)carboalumination]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ureidopenicillin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminocarbonyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminoanthraquinone)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminomethylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-morpholinosydnonimine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminomethylene)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-anilinomethylene)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-vinylsulfonylacetamido)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-thienyl)sulfonylamine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylsulfonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)sulfonylamine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylmethylamine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-hydroxycarbonylmethyl)-4-ylmethyl-6-(4-triptoreline enyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxycarbonylphenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-tert-butoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(methylamino)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(dimethylamino)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinecarbonitrile)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-morpholinosydnonimine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-phenylpiperazine)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylenecarbonyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(methylpentylamino)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxyphenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-Tr is formatexception)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-morpholinium)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminocarbonylmethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methoxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1-pyrrolidinyl)ethoxypyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzyloxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzyloxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-tetrazol-5-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-amidinopropane)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminomethylene)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminomethylpyridine)-4-ylmethyl-6-(4-triptoreline is)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylpyridin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isopropylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-tert-butylpyridinium)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isobutylpyrazine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-cyclohexylpiperidine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-vinylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(3-chlorophenyl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-chlorophenyl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-forfinal)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxyphenyl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3,2'-bipyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-hydroxymethyluracil)-4-ylmethyl-6(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-chloropyridin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-herperidin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-bromopyridin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminopyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminopropyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethylaminomethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isopropylaminomethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylaminopropyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-cyclohexylpiperidine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-diethylaminopropyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-N-cyclohexyl-N-methylaminomethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinylidene)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinomethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-shall irsol-1-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-benzoylhydrazone)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminopurine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(3-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-perbenzoate)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxybenzylamine)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-acetamidophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylacetamido)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperazine)acetamidophenyl]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-cyclohexenecarboxaldehyde)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1-methyl-4-piperidinyl)carboalumination]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-fornicator)aminopyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diaza the pyro[2.4]heptane-5,7-dione;

- 4-(3-ethoxycarbonylpyrimidine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isopropoxycarbonyloxymethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-butoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-diethylaminoethylamine)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chloroanilino)carboalumination]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-onlinecarisoprodol)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminocarbonyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-pyridylamino)carboalumination]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ureidopenicillin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminocarbonyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminoanthraquinone)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminomethylpyridine)-4-ILM is Teal-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinosydnonimine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminomethylene)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-anilinomethylene)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-vinylsulfonylacetamido)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-thienyl)sulfonylamine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylsulfonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)sulfonylamine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylmethylamine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-hydroxycarbonylmethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxycarbonylphenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-tert-butoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxycarbonylamino)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-triptoreline enyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(methylamino)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(dimethylamino)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinecarbonitrile)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinosydnonimine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-phenylpiperazine)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylenecarbonyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(methylpentylamino)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxyphenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-morpholinium)carbonitriding]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminocarbonylmethyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methoxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-di is suspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1-pyrrolidinyl)ethoxypyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzyloxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzyloxypyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-tetrazol-5-yl)pyridine]-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-amidinopropane)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminomethylene)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminomethylpyridine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 5-methyl-1-(2-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- -methyl-1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2,2'-bipyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-herperidin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-bromopyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-d is he;

- 5-methyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin,4-dione;

- 5-methyl-1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)who gazolidon-2,4-dione;

- 5-methyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ureidopenicillin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-anilinomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-trifloromethyl)who gazolidon-2,4-dione;

- 5-methyl-1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylmethylamine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-yl-methyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-imidazol-2-yl)pyridine-4-metil]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-amidinopropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triptoreline enyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3,2'-bipyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-herperidin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-bromopyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminopyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-diethylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triptime Setenil)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-acetamidophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triptime is oxyphenyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-onlinecarisoprodol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ureidopenicillin-4-ylmethyl)-3-(4-trift methoxyphenyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-anilinomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylmethylamine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazole the n-2,4-dione;

- 5-methyl-1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triptoreline the Nile)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-amidinopropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-ethylpyridine-4-ylmethyl)-3-(4-t is eformatexif)-imidazolidin-2,4-dione;

- 1-(2-isopropylpyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-phenylpyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-benzylpyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2,2'-bipyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-triptoreline-phenyl)imidazolidin-2,4-dione;

- 1-(2-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-herperidin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-bromopyridin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-AMI is pyridin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- -[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-acetamidophenyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-phenylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triptorelin iphenyl)imidazolidin-2,4-dione;

- 1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-ureidopenicillin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-anilinomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)and idazole-2,4-dione;

- 1-(2-benzylmethylamine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione

- 1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-phenoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-methoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[2-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-amidinopropane-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-ethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-isopropylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-phenylpyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-benzylpyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3,2'-bipyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-chloropyridin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-perperi the Jn-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-bromopyridin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-aminopyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-methylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-diethylaminopropyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-morpholinopropan-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-chlorobenzylamino)pyridine-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-acetamidophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-phenylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-trifloromethyl them who solidin-2,4-dione;

- 1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-onlinecarisoprodol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-ureidopenicillin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-anilinomethylene-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov-2,4-dione;

- 1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-benzylmethylamine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(meth is phenylamino)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-phenoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-methoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-amidinopropane-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triptoreline the Il)imidazolidin-2,4-dione;

- 1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylpyridine-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperid is Ino)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1-methyl-4-piperidinyl)-carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-diethylaminoethylamine)-pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-pyridylamino)to beilenopcion-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylmethylamine-4-ylmethyl)-3-(4-triptorelin sulfanilyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov them who solidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxyphenyl)-methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-diet aminopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-AC is amidopirin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1-methyl-4-piperidinyl)-carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-diethylaminoethylamine)-pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-unlinkability the pyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ureidopenicillin-4-ylmethyl)-3-(4-triptorelin-sulfanilyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-tripto methanesulfonyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)who imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxyphenyl)-methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethy the-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 4-(2-methylpyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-tert-butylpyridinium)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isobutylpyrazine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(3-chlorine is phenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-forfinal)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxyphenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2,2'-bipyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-hydroxymethylpropane)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-chloropyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-herperidin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-bromopyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminopyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropylaminoethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylaminopyrimidine)-4-elmet is l-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-diethylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-N-cyclohexyl-N-methylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-morpholinoethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-pyrazole-1-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-benzoylhydrazone)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminopurine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(3-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-perbenzoate)pyridine]-4-ILM is Teal-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxybenzylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-acetamidophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylacetamido)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperazine)acetamidophenyl]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexanecarboxaldehyde)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1-methyl-4-piperidinyl)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-fornicator)aminopyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxycarbonylpyrimidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropoxycarbonyloxymethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-diethylaminoethylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxycarbonylamino)-4-ylmethyl-6-(4-triptorelin sulfanilyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chloroanilino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-onlinecarisoprodol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-pyridylamino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ureidopenicillin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminoanthraquinone)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminomethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-anilinomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-vinylsulfonylacetamido)-4-ylmethyl-6-(4-trifloromethyl anifani)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-thienyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylsulfonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylmethylamine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-hydroxycarbonylmethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxycarbonylphenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-tert-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(methylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(dimethylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinecarbonitrile)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]g is PTEN-5,7-dione;

- 4-(2-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-phenylpiperazine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylenecarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(methylpentylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxyphenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-morpholinium)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminocarbonylmethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1-pyrrolidinyl)ethoxypyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dio is;

- 4-(2-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-tetrazol-5-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-amidinopropane)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminomethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylpyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isopropylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-tert-butylpyridinium)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isobutylpyrazine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-d is he;

- 4-(3-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-vinylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(3-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-forfinal)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxyphenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3,2'-bipyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-hydroxymethyluracil)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-chloropyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-herperidin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-bromopyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminopyridine)-4-ylmethyl-6-(4-shall reformationsschriften)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isopropylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-diethylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-N-cyclohexyl-N-methylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinylidene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-pyrazole-1-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-benzoylhydrazone)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminopurine)-4-ylmethyl-6-(4-trifloromethyl the Nile)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(3-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-perbenzoate)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxybenzylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-acetamidophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylacetamido)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperazine)acetamidophenyl]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-cyclohexenecarboxaldehyde)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1-methyl-4-piperidinyl)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-fornicator)aminopyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxycarbonylpyrimidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazep the ro[2.4]heptane-5,7-dione;

- 4-(3-isopropoxycarbonyloxymethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-diethylaminoethylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chloroanilino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-onlinecarisoprodol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-pyridylamino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ureidopenicillin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminoanthraquinone)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminomethylpyridine)-4-ylmethyl-6-(4-triptime analfinger)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-anilinomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-vinylsulfonylacetamido)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-thienyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylsulfonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylmethylamine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-hydroxycarbonylmethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxycarbonylphenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-tert-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diesase what about[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(methylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(dimethylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinecarbonitrile)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-phenylpiperazine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylenecarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(methylpentylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxyphenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-morpholinium)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminocarbonylmethyl)-4-ylmethyl-6-(4-triptime sulfanilyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1-pyrrolidinyl)ethoxypyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-tetrazol-5-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-amidinopropane)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminomethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 5-methyl-1-(2-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazole the in-2,4-dione;

- 5-methyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-triptorelin sulfanilyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperidino)pyridine-4-ILM is Teal]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1-methyl-4-piperidinyl)Carboni is aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imides is lidin-2,4-dione;

- 5-methyl-1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov them who solidin-2,4-dione;

- 5-methyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl--(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-triptorelin sulfanilyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-diethylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperidino)pyridine-4-ILM is Teal]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1-methyl-4-piperidinyl)Carboni is aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imides is lidin-2,4-dione;

- 5-methyl-1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov them who solidin-2,4-dione;

- 5-methyl-1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-METI the pyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)who imidazolidin-2,4-dione;

- 1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-benzoylhydrazone)the feast of the DIN-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triternata sulfanilyl)imidazolidin-2,4-dione;

- 1-(2-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzyloxy the one-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]--(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)who gazolidon-2,4-dione;

- 1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-diethylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-trifter ethanolgasoline)imidazolidin-2,4-dione;

- 1-(3-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-onlinecarisoprodol-4-ylmethyl)-3-(4-triptorelin llanerfyl)imidazolidin-2,4-dione;

- 1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triptoreline the Il)imidazolidin-2,4-dione;

- 1-(3-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1[3-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethoxypyridine-4-ylmethyl)-3-(4-trifloromethyl-phenyl)imidazolidin-2,4-dione;

- 1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov is)imidazolidin-2,4-dione;

- 1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzyl what iridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperazine)diethylaminopropyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-what ethylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1-methyl-4-piperidinyl)-carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-diethylaminoethylamine)-pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-pyridylamino)to beilenopcion-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzylmethylamine-4-ylmethyl)-3-(4-triptorelin wltnylfj)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov them who solidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-methoxyphenyl)-methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[2(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-diet aminopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperazine)diethylaminopropyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-d is methyl-1-(3-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1-methyl-4-piperidinyl)-carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-diethylaminoethylamine)-pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-unlinkability the pyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov);

- 5,5-dimethyl-1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov is)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)who imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-methoxyphenyl)-methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethy the-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 4-(2-methylpyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-tert-butylpyridinium)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isobutylpyrazine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(3-chlorine is phenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-forfinal)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxyphenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2,2'-bipyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-hydroxymethylpropane)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-chloropyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-herperidin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-bromopyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminopyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropylaminoethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylaminopyrimidine)-4-elmet is l-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-diethylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-N-cyclohexyl-N-methylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-morpholinoethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperazine)diethylaminophenyl]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-pyrazole-1-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-benzoylhydrazone)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminopurine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(3-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-perbenzoate)p is ridin]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxybenzylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-acetamidophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylacetamido)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperazine)acetamidophenyl]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-cyclohexanecarboxaldehyde)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1-methyl-4-piperidinyl)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-fornicator)aminopyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxycarbonylpyrimidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-isopropoxycarbonyloxymethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-diethylaminoethylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxycarbonylamino)-4-ylmethyl-6-(4-triptorelin wltnylfj)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chloroanilino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-onlinecarisoprodol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-pyridylamino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ureidopenicillin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminoanthraquinone)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminomethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-anilinomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-vinylsulfonylacetamido)-4-ylmethyl-6-(4-trifloromethyl hilfer)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(2-thienyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylsulfonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzylmethylamine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-hydroxycarbonylmethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxycarbonylphenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-tert-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(methylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(dimethylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinecarbonitrile)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]g is PTEN-5,7-dione;

- 4-(2-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-phenylpiperazine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenylenecarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(methylpentylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-methoxyphenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-chlorophenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4-morpholinium)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminocarbonylmethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-phenoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ethoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1-pyrrolidinyl)ethoxypyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dio is;

- 4-(2-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[2-(1H-tetrazol-5-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-amidinopropane)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminomethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylpyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isopropylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-tert-butylpyridinium)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isobutylpyrazine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-d is he;

- 4-(3-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-vinylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(3-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-chlorophenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-forfinal)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxyphenyl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3,2'-bipyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-hydroxymethyluracil)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-chloropyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-herperidin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-bromopyridin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminopyridine)-4-ylmethyl-6-(4-shall triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-isopropylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-cyclohexylpiperidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-diethylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-N-cyclohexyl-N-methylaminomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinylidene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinomethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperazine)diethylaminophenyl]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-pyrazole-1-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-benzoylhydrazone)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminopurine)-4-ylmethyl-6-(4-triternata sulfanilyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(3-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-chlorobenzylamino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-perbenzoate)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxybenzylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-acetamidophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylacetamido)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperazine)acetamidophenyl]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-cyclohexenecarboxaldehyde)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1-methyl-4-piperidinyl)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-fornicator)aminopyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxycarbonylpyrimidine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazep the ro[2.4]heptane-5,7-dione;

- 4-(3-isopropoxycarbonyloxymethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-diethylaminoethylamine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chloroanilino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-onlinecarisoprodol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-pyridylamino)carboalumination]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ureidopenicillin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylaminocarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminoanthraquinone)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminomethylpyridine)-4-ylmethyl-6-(4-triptime unsulfonated)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-anilinomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-vinylsulfonylacetamido)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(2-thienyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylsulfonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)sulfonylamine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzylmethylamine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-hydroxycarbonylmethyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxycarbonylphenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-tert-butoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxycarbonylamino)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diesase what about[2.4]heptane-5,7-dione;

- 4-[3-(4-methylpiperidino)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(methylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(dimethylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinecarbonitrile)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-morpholinosydnonimine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-phenylpiperazine)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenylenecarbonyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(methylpentylamino)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-methoxyphenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-chlorophenyl)methylaminomethyluridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4-morpholinium)carbonitriding]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminocarbonylmethyl)-4-ylmethyl-6-(4-triptime sulfanilyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-phenoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ethoxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1-pyrrolidinyl)ethoxypyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-benzyloxypyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-imidazol-2-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-[3-(1H-tetrazol-5-yl)pyridine]-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-amidinopropane)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminomethylene)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminomethylpyridine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 5-methyl-1-(2-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazole the in-2,4-dione;

- 5-methyl-1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-triptorelin wltnylfj)imidazolidin-2,4-dione;

- 5-methyl-1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperazine)diethylamino ridin-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1-methyl-4-piperidinyl)Carboni is aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ureidopenicillin-4-ylmethyl)-3-(4-triptorelin-sulfanilyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imide alidin-2,4-dione;

- 5-methyl-1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov them who solidin-2,4-dione;

- 5-methyl-1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[2-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl--(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-triptorelin wltnylfj)imidazolidin-2,4-dione;

- 5-methyl-1-(3-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-diethylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperazine)diethylamino ridin-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1-methyl-4-piperidinyl)Carboni is aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imides is lidin-2,4-dione;

- 5-methyl-1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov them who solidin-2,4-dione;

- 5-methyl-1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-METI the pyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)who imidazolidin-2,4-dione;

- 1-(2-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-diethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperazine)diethylaminopropyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-benzoyl is draino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methoxybenzylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-cyclohexanecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethoxycarbonylpyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

-1-(2-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-onlinecarisoprodol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triternata sulfanilyl)imidazolidin-2,4-dione;

- 1-(2-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenylaminopyrimidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzyloxy the one-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[2-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isopropylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-tert-butylpyridinium-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isobutylpyrazine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)pyridine-4-ylmethyl]--(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(3-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-chlorophenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-forfinal)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methoxyphenyl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3,2'-bipyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-hydroxymethylpropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-chloropyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-herperidin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-bromopyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminopyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isopropylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)who gazolidon-2,4-dione;

- 1-(3-cyclohexylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-diethylaminopropyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-N-cyclohexyl-N-methylaminomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-morpholinopropan-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperazine)diethylaminopropyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1H-pyrazole-1-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-benzoylhydrazone)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzoylpiperidine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(3-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-chlorobenzylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-perbenzoate)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methoxybenzylamine)pyridine-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-acetamidophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperazine)acetamidophenyl-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-cyclohexenecarboxaldehyde-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1-methyl-4-piperidinyl)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-fornicator)aminopyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-isopropoxycarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-diethylaminoethylamine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chloroanilino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-onlinecarisoprodol-4-ylmethyl)-3-(4-triptorelin lifeifei)imidazolidin-2,4-dione;

- 1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-pyridylamino)carboalumination-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ureidopenicillin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzylaminocarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylaminoanthraquinone-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-anilinomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-vinylsulfonylacetamido-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(2-thienyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylsulfonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)sulfonylamine-4-ylmethyl]-3-(4-triftormetilfullerenov the Il)imidazolidin-2,4-dione;

- 1-(3-benzylmethylamine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-hydroxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethoxycarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-tert-butoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenoxycarbonylamino-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-methylpiperidino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(methylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(dimethylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-piperidinecarbonitrile-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-morpholinosydnonimine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-phenylpiperazine)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenylenecarbonyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(methylpentylamino)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1[3-(4-methoxyphenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-chlorophenyl)methylaminomethyluridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4-morpholinium)carbonitriding-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminocarbonylmethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-phenoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ethoxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1-pyrrolidinyl)ethoxypyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-benzyloxypyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(4,5-dihydro-1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1H-imidazol-2-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-[3-(1H-tetrazol-5-yl)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-amidinopropane-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-dimethylaminomethylene-4-ylmethyl)-3-(4-triftormetilfullerenov is)imidazolidin-2,4-dione;

- 1-(3-aminomethylpyridine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminophenol-4-ylmethyl)-3-(4-triptoreline enyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-aminoquinoline-4-ylmethyl)-3-(4-triptime is oxyphenyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-piperidinyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-ftorhinolon-4-ylmethyl)-3-(4-trif ormeloxifene)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 4-(2-methylinosine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methoxyaniline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-chlorhydrin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ftorhinolon)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminophenol)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylinosine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methoxyaniline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-chlorhydrin)-4-ylmethyl-6-(4-triptoreline is)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ftorhinolon)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminopropyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methylinosine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methoxyaniline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-chlorhydrin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-ftorhinolon)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methylaminophenol)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-dimethylaminophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-piperidinophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methylinosine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methoxyquinoline)-4-ylmethyl-6-(4-trifloromethyl)-,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-chlorhydrin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-ftorhinolon)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methylaminophenol)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-dimethylaminophenyl)-4-ylmethyl-6-(4-triptoreline-phenyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-piperidinophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methylinosine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methoxyquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-chlorhydrin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-ftorhinolon)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methylaminophenol)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-dimethylaminophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-piperidinophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methylinosine)-4-ylmethyl-6-(4-trifloromethyl)-4,6-is azaspiro[2.4]heptane-5,7-dione;

- 4-(8-methoxyquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-chlorhydrin)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-ftorhinolon)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methylaminophenol)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-dimethylaminophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-piperidinophenyl)-4-ylmethyl-6-(4-trifloromethyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 5-methyl-1-(2-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-,4-dione;

- 5-methyl-1-(3-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(5-p is peridiniidae-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(6-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(7-p is peridiniidae-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 5-methyl-1-(8-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(2-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)-and idazole-2,4-dione;

- 1-(3-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(3-piperidinyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(5-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(5-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(5-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(5-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(5-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(5-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(5-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(6-methylinosine-4-ylmethyl)-3-(-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(6-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(6-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(6-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(6-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(6-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(6-piperidinomethyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(7-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(7-methoxyquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(7-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(7-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(7-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(7-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(7-piperidinyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(8-methylinosine-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(8-methoxyquinoline-4-ylmethyl)3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(8-chlorhydrin-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(8-ftorhinolon-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(8-aminoquinoline-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(8-methylaminophenol-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

- 1-(8-piperidinophenyl-4-ylmethyl)-3-(4-trifloromethyl)-imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylinosine-4-ylmethyl)-3-(4-trift methansulfonate)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-dimethylaminophenol-4-ylmethyl)-3-4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-aminoquinoline-4-ylmethyl)-3-(4-trift methansulfonate)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 4-(2-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methoxyaniline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-chlorhydrin)-4-ylmethyl-6-(4-three is commanduihandler)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methoxyaniline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methylinosine)-4-ylmethyl-6-(4-triptime sulfanilyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methoxyaniline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methoxyquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-dimethylaminophenyl)-4-ylmethyl-6-(4-triptorelin hamiltoni)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methoxyquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methoxyquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl enyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 5-methyl-1-(2-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)who imidazolidin-2,4-dione;

- 5-methyl-1-(3-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazole the n-2,4-dione;

- 5-methyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,Dion;

- 5-methyl-1-(7-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylaminophenol-4-ylmethyl)--(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-what ethylaminoethanol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-ethylaminoethanol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-tripto methanesulfonyl)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(3-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-chlorhydrin-4-ILM is Teal)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(5-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(6-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methylinosine-4-elmet the l)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(7-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-dimethylaminophenyl-4-ylmethyl)-3-4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5,5-dimethyl-1-(8-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 4-(2-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methoxyaniline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(2-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methoxyaniline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-aminoquinoline)-4-ylmethyl-6-(4-trifloromethyl enyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-methylaminopropyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(3-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methoxyaniline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(5-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methoxyquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-chlorhydrin)-4-ylmethyl-6-(4-triform consultonline)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(6-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methylinosine)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methoxyquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(7-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methylinosine)-4-ylmethyl-6-(4-triptime sulfanilyl)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methoxyquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-chlorhydrin)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-ftorhinolon)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-aminoquinoline)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-methylaminophenol)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-dimethylaminophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 4-(8-piperidinophenyl)-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2.4]heptane-5,7-dione;

- 5-methyl-1-(2-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov the Il)imidazolidin-2,4-dione;

- 5-methyl-1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(3-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(5-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(6-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin,4-dione;

- 5-methyl-1-(7-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(7-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 5-methyl-1-(8-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-di is n;

- 1-(2-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(2-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(3-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-dimethylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(5-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(6-piperidinomethyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(7-piperidinyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-methylinosine-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-methoxyquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-chlorhydrin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-ftorhinolon-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-aminoquinoline-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-methylaminophenol-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-dimethylaminophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

- 1-(8-piperidinophenyl-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione.

Table 1 (examples 264-332)

1. The compounds of formula (I)

in which

p means an integer from 0 to 2;

R and R1means Of;

R2 and R3, identical or different, denote a hydrogen atom, (C1-C6)alkyl, possibly substituted by radicals selected among hydroxyl, phenyl, monocyclic or bicyclic unsaturated heterocyclic radical comprising one heteroatom selected among N, and S,

or R2 and R3 together with the atom angle of the ode, to which they are attached, form a carbocyclic 3-10-membered radical;

A1 and A2 denote a simple link, (C1-C6)alkyl;

Y and Y1, different, are such that one of Y and Y1 is chosen among OCF3, -O-CF2-CHF2, -O-CHF2, -O-CH2CF3, SF5, -S(O)n-(C1-C6)alkyl, possibly substituted by radicals chosen among the following values: halogen atom, cyano, (C1-C6)alkoxyl, hydroxyl, monocyclic saturated or unsaturated 5 or 6-membered heterocyclic radical comprising from 1 to several identical or different heteroatoms selected among N, and O, possibly substituted (C1-C6)alkyl;

and the other of Y and Y1 is chosen among the following values: hydrogen atom, halogen atom, the nitro-group, NR5R6,

or phenyl radical with their substituents Y and Y1 form the following radical:

where p means an integer 2, 3 or 4, where the radical may be substituted by one or more identical or different radicals, selected among halogen atoms or (C1-C6)alkyl;

R5 and R6, identical or different, chosen among hydrogen atom, (C1-C6)alkyl, (C3-C7)cycloalkyl, phenyl, monocyclic or bicyclic unsaturated 5 or 6-membered heterocyclic radical comprising from 1 to several equal or asnyk heteroatoms, choose among N and S, possibly substituted by one or more, odinakovimi or different radicals, selected among halogen atoms, (C1-C6)alkoxyl, -NR11R12, CF3;

or R5 and R6 together with the nitrogen atom to which they are attached, form a 3-10-membered heterocyclic radical comprising one or more heteroatoms selected among N, possibly substituted (C1-C6)alkyl, monocyclic unsaturated 6-membered heterocyclic radical comprising from 1 to several heteroatoms selected among N, by one or more radicals selected from oxo and tocography;

B2 means a monocyclic or bicyclic, saturated or unsaturated heterocyclic radical comprising from 1 to several identical or different heteroatoms chosen among O, S, N and NR7, possibly substituted by one or more, same or different substituents selected from Y2;

R7 means a hydrogen atom, (C1-C6)alkyl, possibly substituted (C1-C6)alkylphenyl;

Y2 denotes a hydrogen atom, halogen atom, hydroxyl, (C1-C6)alkyl, (C1-C6)alkoxy, COOR13, NR5R6, -NR10-CO-R13, -NR10-CO-NR5R6, -NR10-CS-NR5R6, -NR10-COOR13;

and

n means an integer from 0 to 2;

R8 is (C1-C6)alkyl;

R9 has the values of R8 or denotes hydrogen;

R10 denotes a hydrogen atom;

R11 and R12, identical or different, denote a hydrogen atom, (C1-C4)-alkyl, possibly substituted by phenyl;

or R11 and R12 together with the nitrogen atom to which they are bound, form a 5-7-membered cyclic radical containing one or more heteroatoms chosen among O and N; and

R13, identical or different from R5 and R6, choose among the values of R5 or R6;

provided that the compounds of formula (I) are as specified below in paragraphs. a)-d):

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3or S-Alk; A2 means a simple bond or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3That SO-Alk, S(O)2-Alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-Alk, always replaced by hydroxamate-CO-NHOH;

c) when the p means an integer of 0 R and R1 denote an oxygen atom, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means S(O)n-Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

d) when R denotes an integer from 0 to 2, R and R1 denote an oxygen atom, A1 means a simple bond; Y and Y1 are the same or different, are such that one means S(O)2-Alk or SO2NH2and the other means NR5R6; A2 means a simple link or alkylene and B2 means maybe substituted 5-10-membered heterocyclic radical, then R2 and R3 does not denote simultaneously a hydrogen atom;

where Alk denotes alkyl with 1-6 carbon atoms;

moreover, the above compounds of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric - isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or inorganic or organic bases of the above compounds of formula (I).

2. The compounds of formula (I) according to claim 1, in which

p means an integer from 0 to 2;

R and R1 mean About;

R2 and R3, identical or different, mean and the om hydrogen, C1-Salkil or R2 and R3 together with the carbon atom to which they are attached, form a carbocyclic 3-10-membered radical;

A1 means a simple bond, C1-Salkil;

Y and Y1, different, are such that one of Y and Y1 is chosen among OCF3and S(O)n-C1-C6-alkyl, and the other of Y and Y1 is chosen among the following values: hydrogen atom, halogen atom; and

R5 and R6, identical or different, chosen among hydrogen atom, (C1-C6)alkyl, (C3-C7)cycloalkyl, 5 - or 6-membered geterotsiklicheskie containing from 1 to several heteroatoms N and S, phenyl, or R5 and R6 together with the nitrogen atom to which they are attached, form a 3-10-membered heterocyclic radical comprising one or more heteroatoms selected among N;

A2, identical to or different from A1, has values A1;

B2 means a saturated or unsaturated heterocyclic radical comprising from 1 to several identical or different heteroatoms chosen among O, S and NR7, possibly substituted by one or more, same or different substituents selected from Y2;

R7 means a hydrogen atom, C1-Salkil;

Y2 denotes a hydrogen atom, halogen atom, hydroxyl, C1-Salkil, C1-Sarcoxie, NR5R6;

n means an integer from 0 to 2;

R8 denotes C1-Salkil;

R9 has the values of R8 or denotes hydrogen

R10 denotes a hydrogen atom;

R11 and R12, identical or different, denote a hydrogen atom, (C1-C4)-alkyl, possibly substituted by phenyl;

or R11 and R12 together with the nitrogen atom to which they are bound, form a 5-7-membered cyclic radical containing one or more heteroatoms chosen among O, N;

provided that the compounds of formula (I) are as specified below in paragraphs. a)-d):

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3or S-Alk; A2 means a simple bond or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means OCF3That SO-Alk, S(O)2-Alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-Alk, always replaced by hydroxamate-CO-NHOH;

c) when p means an integer is number 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means S(O)n-Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

d) when R denotes an integer from 0 to 2, R and R1 denote oxygen atoms, A1 means a simple bond; Y and Y1 are the same or different, are such that one means S(O)2-Alk or SO2NH2and the other means NR5R6; A2 means a simple link or alkylene and B2 means maybe substituted 5-10-membered heterocyclic radical, then R2 and R3 do not mean simultaneously hydrogen atoms;

where Alk denotes an alkyl radical with 1-6 carbon atoms,

moreover, the above compounds of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric - isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or inorganic or organic bases of the above compounds of formula (I).

3. The compounds of formula (I) according to claim 1, in which Y and Y1 are different, are such that one of Y and Y1 is chosen among OCF3, -O-CF2-CHF2, -O-CHF2 , -O-CH2-CF3, -S(O)n-Alk, where Alk denotes an alkyl radical with 1-4 carbon atoms and the other of Y and Y1 is chosen among the following values: hydrogen atom, halogen atom, the nitro-group, NR5R6;

or phenyl radical with their substituents Y and Y1 form the following radical:

and thus the resulting radical possibly substituted by one or more C1-Sarkisinida radicals;

and the other substituents are the above compounds of formula (I) is chosen among the values specified in claim 1, and provided that

a) when R denotes an integer of 0, R means an oxygen atom; R1 means an oxygen atom; A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that at least one means a hydrogen atom, and the other means OCF3or S-Alk, A2 means a simple link or alkyl and B2 means maybe substituted heterocyclic radical, then R2 and R3 does not mean one is a hydrogen atom and the other imidazolylalkyl;

b) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom, and the other means OCF3, SOAlk, S(O)2-Alk or SO2NH2; A2 means CH2and B2 means maybe substituted heterocyclics radical, then R2 and R3 does not mean one is a hydrogen atom and the other is an alkyl chain, possibly interrupted O, S, N-Alk, always replaced by hydroxamate-CO-NHOH;

c) when R denotes an integer of 0, R and R1 denote oxygen atoms, A1 means a simple link or alkyl; Y and Y1 are the same or different, are such that one means a hydrogen atom and the other denotes S(O)n-Alk; A2 means a simple link and B2 means maybe substituted 5 - or 6-membered heterocyclic aromatic radical, then R2 and R3 do not choose among a hydrogen atom, alkyl, arylalkyl, aryl and heteroaryl;

where Alk denotes an alkyl radical with 1-6 carbon atoms,

moreover, the above compounds of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or inorganic or organic bases of the above compounds of formula (I).

4. The compounds of formula (I) according to claim 1 or 2, in which R indicates an integer of 0, and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

5. The compounds of formula (I) according to claim 1 or 2, in which R indicates an integer of 1, and the other substituents are the above compounds of formulas is (I) have the meanings listed on any of the claims.

6. The compounds of formula (I) according to claim 1 or 2, in which p denotes an integer of 2, and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

7. The compounds of formula (I) according to claim 1, in which R2 and R3, identical or different, denote C1-Salkil, possibly substituted by phenyl, or R2 and R3 together with the carbon atom to which they are attached, form a 3-10-membered carbocyclic radical.

8. The compounds of formula (I) according to claim 1, in which R2 and R3, identical or different, chosen among hydrogen atom, C1-C4-alkyl, phenyl-C1-C4-alkyl, pyridyl-C1-C4-alkyl, benzothiazyl-C1-C4-alkyl, or R2 and R3 together with the carbon atom to which they are bound, form a 3-6-membered cycloalkyl radical;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

9. The compounds of formula (I) according to claim 1, in which R2 and R3, identical or different, chosen among hydrogen atom, C1-C6-alkyl, hydroxy-C1-C6-alkyl, phenyl-C1-C6-alkyl, pyridyl-C1-C6-alkyl, benzothiazyl-C1-C6-alkyl; or R2 and R3 together with the carbon atom to which they are bound, form cycloalkyl radical comprising 3 to 6 carbon atoms;

and the other substituents are the above compounds of formula (I) have meant what I listed on any of the claims.

10. The compounds of formula (I) according to claim 9, in which R2 and R3, identical or different, chosen among hydrogen atom, C1-C6-alkyl, hydroxy-C1-C6-alkyl, phenyl-C1-C6-alkyl, or R2 and R3 together with the carbon atom to which they are bound, form cycloalkyl radical comprising 3 to 6 carbon atoms.

11. The compounds of formula (I) according to claim 1 or 2, in which R2 and R3, identical or different, denote a hydrogen atom and CH3or R2 and R3 together with the carbon atom to which they are bound, form cyclopropyl;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

12. The compounds of formula (I) according to claim 1 or 2, in which A1 means a simple link, and A2 denotes C1-C6-alkyl;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

13. The compounds of formula (I) according to claim 1, in which Y and Y1 are such that one means a hydrogen atom, halogen atom or amino group, and the other choose among-OCF3, -O-CF2-CHF2, -O-CHF2, -O-CH2CF3, SF5, -S(O)n-Alk, where Alk denotes alkyl with 1-4 carbon atoms;

and the other substituents are the above compounds of formula (I) have the values listed on any of the points the claims.

14. The compounds of formula (I) according to claim 1 or 2, in which Y represents a hydrogen atom, and Y1 is chosen among-OCF3, -S(O)n-CH3;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

15. The compounds of formula (I) according to claim 1 or 2, where B2 denotes monocyclic or bicyclic heteroaryl radical selected among pyridyl, pyrimidinyl, chinoline, thiazolyl, morpholinyl, pyrrolidinyl, furil, chromene, oxopropanal, and these radicals possibly substituted by one or more radicals selected from Y2;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

16. The compounds of formula (I) according to claim 1 or 2, in which B2 means a heteroaryl radical chosen among the 3 - or 4-pyridyl, pyrimidinyl, 3 - or 4-chinoline, thiazolyl, and these radicals possibly substituted by one or more radicals selected from Y2;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

17. The compounds of formula (I) according to claim 1 or 2, in which B2 means a heteroaryl radical chosen among the 3 - or 4-pyridyl, pyrimidinyl, 3 - or 4-ginalisa moreover, these radicals possibly substituted by one or more radicals, choose among the values of Y2;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

18. The compounds of formula (I) according to claim 1 or 2, where B2 denotes 4-pyridyl and 4-chinolin, possibly substituted by one or more radicals chosen among the values of Y2 specified in any of claims;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

19. The compounds of formula (I) according to claim 1, in which Y2 denotes a hydrogen atom, halogen atom, NR5R6;

R5 and R6, identical or different, chosen among hydrogen atom, C1-C6-alkyl, C3-C7-cycloalkyl, phenyl and radicals, which is a 5-6-membered ring containing 1-3 heteroatom selected among N, and S; or R5 and R6 together with the nitrogen atom to which they are bound, form a possibly substituted pyrrolidinyl, piperazinil or hintline;

R10 denotes a hydrogen atom;

other substituents of the above compounds of formula (I) have the values listed in any of the claims.

20. The compounds of formula (I) according to claim 1, in which Y2 denotes a hydrogen atom, halogen atom, hydroxyl, C1-C6-alkyl, C1-C6-alkoxy, NR5R6, -NR10-CO-R13, -NR10-CS-NR5R6;

R5 and R6, identical or different, chosen among ATO is and hydrogen, phenyl, pyridyl, chinoline, thiazolyl;

or R5 and R6 together with the nitrogen atom to which they are bound, form a radical pyrrolidinyl, piperazinil or hintline; and pyrrolidinyl may also be replaced by oxopropoxy;

R10 denotes a hydrogen atom;

other substituents of the above compounds of formula (I) have the values listed in any of the claims.

21. The compounds of formula (I) according to claim 1 or 2, where Y2 denotes a halogen atom, a hydroxyl;

other substituents of the above compounds of formula (I) have the values listed in any of the claims.

22. The compounds of formula (I) according to claim 1 or 2, where Y2 denotes a hydrogen atom, halogen atom, C1-C6-alkyl, hydroxyl, C1-C6-alkoxyl;

other substituents of the above compounds of formula (I) have the values listed in any of the claims.

23. The compounds of formula (I) according to claim 1 or 2, where Y2 denotes a hydrogen atom, F, Cl, CH3CH2CH3HE co3, NH2, NHAlk, where Alk denotes alkyl with 1-6 carbon atoms;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

24. The compounds of formula (I) according to claim 1 or 2, where B2 denotes 4-pyridyl and 4-chinolin substituted by one or two radicals which Lamy, selected among F, Cl, HE, and co3;

and the other substituents are the above compounds of formula (I) have the values listed in any of the claims.

25. The compounds of formula (I)according to claim 1, corresponding to the formula (IC)

in which

YC and Y1C are such that one means a hydrogen atom, halogen atom or amino group, and the other choose among-OCF3, -O-CF2-CHF2, -O-CHF3, -O-CH2-CF3, SF5, -S(O)n-Alk, where Alk denotes an alkyl radical containing from 1 to 4 carbon atoms;

or phenyl radical with his deputies YC and Y1C forms the following radical:

where Alk denotes an alkyl containing 1-4 carbon atoms;

R2C and R3C, identical or different, denote a hydrogen atom or a possibly substituted C1-C6-alkyl, or R2C and R3C, together with the carbon atom to which they are attached, form a (C3-C10-cycloalkyl;

AS means of simple communication;

B2C means radicals pyridyl, pyrimidinyl, hinely, thiazolyl, morpholinyl, pyrrolidinyl, furyl, bromanil, oxopropanal, possibly substituted by one or more radicals selected among values Y2C;

Y2C means a hydrogen atom, halogen atom, hydroxyl, C1-C6-alkyl, C1-C6-alkoxy is, COOH, COOAlk, NR5R6, -NR10-CO-R6 or-NR10-CS-NR5R6;

R5 and R6, identical or different, chosen among hydrogen atom, C1-C6-alkyl, C3-Cicloalchil, phenyl, pyridyl, chinoline, thiazolyl, all these radicals possibly substituted by a halogen atom, CF3, C1-C6-alkoxy, NR11R12; or R5 and R6 together with the nitrogen atom to which they are bound, form pyrrolidinyl or piperazinil, possibly substituted by oxopropoxy;

R10 denotes a hydrogen atom;

n means an integer from 0 to 2;

the above compounds of formula (IC) are all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or with inorganic and organic bases of the above compounds of formula (IC).

26. The compounds of formula (I) according to claim 1 or 2, corresponding to the formula (IA)

in which

Y1A means OCF3;

VA means radicals 4-chinolin and 4-pyridyl, possibly substituted by one or more radicals selected among values Y2A;

Y2A has the meaning specified in any of claims for Y2;

R2A and R3A, identical or different, denote a hydrogen atom or a possibly substituted C1-C6-alkyl, or R2A and R3A together with the carbon atom, the which they are associated, form (C3-C10-cycloalkyl; and

all the alkyl radical possibly substituted by one or more radicals selected among IT; and the above compounds of formula (IA) are all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or with inorganic and organic bases of the above compounds of formula (IA).

27. The compounds of formula (I) of claim 1 or 2, corresponding to the formula (IA)in which:

Y1A means OCF3;

VA means 4-chinolin or 4-pyridyl, possibly substituted by one or two radicals, selected among halogen atom, -HE, C1-C6-alkyl, C1-C6-alkoxy, -CO2H, -CO2-(C1-C6-alkyl), -NR5AR6A;

R5A and R6A, identical or different, denote a hydrogen atom, C1-C6-alkyl, C3-C7-cycloalkyl, phenyl; or R5A and R6A together with the nitrogen atom to which they are attached, form a cyclic radical chosen among pyrrolidinyl and piperazinil;

R2A and R3A, identical or different, denote a hydrogen atom or C1-Salkil, possibly substituted by radicals selected from hydroxyl; or R2A and R3A together with the carbon atom to which they are attached, form a (C3-C6)-cycloalkenyl radical;

the above link is of the formula (IA) are all possible, racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or with inorganic and organic bases of the above compounds of formula (IA).

28. The compounds of formula (I) according to claim 1 or 2, corresponding to the formula (IA)in which:

Y1A means OCF3; and

R2A and R3A, identical or different, denote a hydrogen atom and CH3; or R2A and R3A together with the carbon atom to which they relate, cyclopropyl; and

other substituents of the above compounds of formula (I) have the values listed in any of the claims,

the above compounds of formula (IA) are all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or with inorganic and organic bases of the above compounds of formula (IA).

29. The compounds of formula (I) according to claim 1 or 2, corresponding to the formula (IB)

in which R2, R3, A1, Y, Y1, A2, B2, and Y2 have the meanings specified in any of claims;

moreover, the above compounds of formula (IB) are all possible racemic, e is antimanic and diastereoisomeric, isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or with inorganic and organic bases of the above compounds of formula (IB).

30. The compounds of formula (IB), as specified in clause 29, in which:

Y1 means OCF3; and

R2 and R3, identical or different, denote a hydrogen atom and CH3; or R2 and R3 together with the carbon atom to which they are bound, form cyclopropyl; and

other substituents have the meanings mentioned in any of the claims,

the above compounds of formula (IB) are all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

and farmatsevticheskii acceptable additive salts with inorganic and organic acids or with inorganic and organic bases of the above compounds of formula (IB).

31. The compounds of formula (I) according to any one of claims 1, 2 or 29, which are:

triptorelin (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (S)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (S)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,Diana;

triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-methyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-methyl-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-methyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-isopropyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-(4-hydroxybenzyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-(4-hydroxybenzyl)-1-pyridin-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin (R)-5-(1-hydroxyethyl)-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione;

triptorelin 4-quinoline-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-di is suspiro[2,4]heptane-5,7-dione;

triptorelin 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione;

triptorelin 4-pyridin-4-ylmethyl-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione;

triptorelin (R)-1-(3-hydroxypyridine-4-ylmethyl)-5-methyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione;

triptorelin 5,5-dimethyl-1-quinoline-4-ylmethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-trifloromethyl)imidazolidin-2,4-dione;

triptorelin 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin 5,5-dimethyl-1-(3-methylpyridin-4-ylmethyl)-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-trifloromethyl)imidazolidin-2,4-dione;

triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin 1-(3-hydroxypyridine-4-ylmethyl)-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin 4-quinoline-4-ylmethyl-6-(4-trifloromethyl)-4,6-diesase what about[2,4]heptane-5,7-dione;

triptorelin 4-(3-methylpyridin-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione;

triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-trifloromethyl)-4,6-diazaspiro[2,4]heptane-5,7-dione;

triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione;

triptorelin 4-(3-hydroxypyridine-4-ylmethyl)-6-(4-triftormetilfullerenov)-4,6-diazaspiro[2,4]heptane-5,7-dione;

moreover, the above compounds of formula (I) are in all possible racemic, enantiomeric and diastereoisomeric, isomeric forms;

as well as pharmaceutically acceptable additive salts with inorganic and organic acids or with inorganic and organic bases of the above compounds of formula (I).

32. The compounds of formula (I) according to any one of claims 1, 2 or 29, which are:

triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide cyclopropanecarbonyl acids;

triptorelin 5,5-dimethyl-1-[2-(pyridine-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-isobutyramide;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide pyridine-2-carboxylic acid;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-piperidine-1-ylpropionic;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-[4-(2-hydroxyethyl)piperazine-1-yl]propionamide;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-morpholine-4-ylpropionic;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-pyrrolidin-1-ylpropionic;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(4-methylpiperazin-1-yl)propionamide;

1-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-phenylacetone;

1-[2-(6-ethylpyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

5,5-dimethyl-1-[2-(4-methylpyridin-2-ylamino)pyridine-4-ilma is Il]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

5,5-dimethyl-1-[2-(6-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

1-[2-(4,6-dimethylpyridin-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

1-[2-(3,5-dichloropyridine-2-ylamino)pyridine-4-ylmethyl]-5,5-dimethyl-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

5,5-dimethyl-1-[2-(pyridine-4-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

5,5-dimethyl-1-[2-(pyridine-3-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(2-oxazepan-1-yl)propionamide;

3-(benzylmethylamine)-N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}propionamide;

3,5-diacetoxy-2-acetoxymethyl-6-(3-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}touraid)tetrahydropyran-4-silt ether acetic acid;

5,5-dimethyl-1-[2-(5-methylpyridin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl} - for 3,5-dimethoxybenzamide;

triptorelin 5,5-dimethyl-1-[2-(pyrazin-2-ylamino)pyridine-4-ylmethyl]-3-(4-triftormetilfullerenov)imidazolidin-2,4-dione;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3-methylpiperidin-1-yl)propionamide;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-(3,5-dimethylpiperidin-1-yl)propionamide;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}-3-methoxybenzamide;

triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide pyrazin-2-carboxylic acid;

triptorelin {4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl}amide thiophene-2-carboxylic acid;

triptorelin N-{4-[5,5-dimethyl-2,4-dioxo-3-(4-triftormetilfullerenov)imidazolidin-1-ylmethyl]pyridine-2-yl