Partly saturated nitrogen-containing heterocyclic compound

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of the formula (I'),

(wherein W represents the formula -CR11R12CR13R14-; R11 represents a hydrogen atom, a fluorine atom, C1-4 alkyl or phenyl; R12 represents a hydrogen atom, a fluorine atom or C1-4 alkyl; provided that R11 and R12, together with the adjacent carbon atom, optionally form C3-8 cycloalkane or tetrahydropyran; R13 represents a hydrogen atom, a carbamoyl, C1-4 alkyl (C1-4 alkyl is optionally substituted by one group selected from the group consisting of hydroxy, C1-3 alkoxy and di-C1-3 alkylamino), halo-C1-4 alkyl, phenyl, pyridyl, benzyl or phenethyl; R14 represents a hydrogen atom, C1-4 alkyl or halogen-C1-4 alkyl; Y represents a single bond or C1-6 alkanediyl (C1-6 alkanediyl is optionally substituted by one hydroxy group and one of the carbon atoms in C1-6 alkanediyl is optionally substituted by cycloalkpropane-1,1-diyl); R2 represents a hydrogen atom, C1-6 alkyl, C3-8 cycloalkyl {C3-8 cycloalkyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl (C1-6 alkyl is optionally substituted by one phenyl group), phenyl (phenyl is optionally substituted by one halogen atom), C1-6 alkoxy [C1-6 alkoxy is optionally substituted by one group selected from the group consisting of C3-8 cycloalkyl, phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom and C1-6 alkyl) and pyridyl (pyridyl is optionally substituted by one halogen atom)], C3-8 cycloalkoxy, phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl) and pyridyloxy (pyridyloxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl)}, phenyl (phenyl is optionally substituted by one to three groups that are the same or different and which are selected from the group of α3 substituents), naphthyl, indanyl, tetrahydronaphthyl, pyrazolyl [pyrazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl (phenyl optionally substituted by one C1-6 alkyl)], imidazolyl [imidazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl], isoxazolyl [isoxazolyl is optionally substituted by one phenyl group (phenyl is optionally substituted by one halogen atom)], oxazolyl [oxazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl and phenyl], thiazolyl [thiazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl, phenyl and morpholino], pyridyl (pyridyl is optionally substituted by one or two groups that are are the same or different and are selected from the group of α5 substituents), pyridazinyl [pyridazinyl is optionally substituted by one C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl group)], pyrimidinyl [pyrimidinyl is optionally substituted by one group selected from the group consisting of halogen-C1-6 alkyl, C3-8 cycloalkyl, phenyl and phenoxy (phenoxy is optionally substituted by one C1-6 alkyl)], pyrazinyl [pyrazinyl is optionally substituted by one group selected from the group consisting of C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl), and phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl and C3-8 cycloalkyl)], benzothiophenyl, quinolyl, methylenedioxyphenyl (methylenedioxyphenyl is optionally substituted by one or two fluorine atoms), azetidinyl (azetidinyl is optionally substituted with one pyrimidinyl group), piperidinyl (piperidinyl is optionally substituted by one group selected from the group consisting of pyrimidinyl, phenyl-C1-3 alkyl, C3-8 cycloalkyl-C1-3 alkylcarbonyl and phenyl-C1-3 alkoxycarbonyl) or the following formula (I") -CONR5CH2-R6 (I") [wherein in formula (I") R5 represents a hydrogen atom or C1-3 alkyl and R 6 is phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom, halogen-C1-6 alkyl and phenyl)], Y4 represents C1-4 alkanediyl; R3 represents a hydrogen atom or methyl; R4 represents -COOH or -CONHOH).

EFFECT: compound has a superior PHD2 inhibitory effect.

16 cl, 28 tbl, 11 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to oxazolopyrimidine compounds of formula (I) , in which A is selected from NH, O and S; R1 is selected from (C1-C6)-alkyl, (C3-C7)-cycloalkyl-CtH2t and Het-CtH2t-, where t is selected from 0, 1, 2 and 3; R2 is selected from phenyl and residue of aromatic 5-member - 6-member monocyclic heterocycle, which includes 1, 2 similar or different ring heteroatoms, selected from N, O and S, in which one of ring nitrogen atoms can carry atom of hydrogen or substituent R21, and in which phenyl and aromatic heterocycle residue are optionally substituted in one or more ring carbon atoms with one or more similar or different substituent R22; R3 is selected from (C1-C6)-alkyl, or R3 represents residue of saturated or unsaturated 3-member - 10-member, monocyclic or bicyclic ring, which includes 0, 1, 2 or 3 similar or different ring nitrogen atoms can carry hydrogen atom or (C1-C4)-alkyl substituent and one or two ring sulphur atoms can carry one or two oxo groups, and in which ring residue is optionally substituted in one or more ring carbon atoms with similar or different substituents R31, on condition that R3 cannot be (C1-C6)-alkyl, if A represents S; other values of radicals are given in i.1 of formula.

EFFECT: compounds of formula (I) are suitable for wound healing.

16 cl, 2 tbl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to oxazolopyramidine compounds of formula I, where A represents O; R1 is selected from phenyl or pyrimidine, which are optionally substituted with R11; R2 represents phenyl, which is optionally substituted wby 1-3 ring carbon atoms with similar or different substituents R22, R11 represents halogen; R22 is selected from hydroxy group, (C1-C4)-alkyl, which is optionallysubstituted with 1-3 atoms of fluorine, (C1-C4)-alkyloxy, (C1-C4)-alkyl-S(O)m-; m equals 2. Invention also relates to pharmaceutical composition, which contains formula I compounds, and to method of obtaining formula I compounds.

EFFECT: formula I compounds, intended for activation of EDG-1 receptor and applied for wound healing.

15 cl, 2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to oxazolopyramidine compounds of formula (I), where A represents O; X represents (C1-C6)-alkanediyl or (C1-C6)-alkanediyloxy, where oxygen atom of (C1-C6)-alkanediyloxy is bound to group R2; Y represents pyrrolidinyl; R1 represents (C1-C4)-alkyl; R2 represents phenylene, optionally substituted by one or two carbon atoms in ring with similar or different substituent R22; R3 is selected from group, which consists of cycloalkyl-CuH2u-, where u equals 1; radical of saturated 3-10-member monocyclic ring, phenyl or pyridyl, where ring radical is optionally substituted by one or two carbon atoms of ring with substituent R31; R4 represents hydrogen; R22 represents (C1-C4)-alkyl; R31 is selected from group, which consists of halogen and (C1-C4)-alkyl. Invention also relates to (S)-l-[2-(2,6-dimethyl-4-{5-[methyl-(3,3,3-trifluoropropyl)amino]-7-propoxyoxazolo[5,4-d]pyrimidine-2-yl}phenoxy)acetyl]pyrrolidine-2-carboxylic acid, pharmaceutical composition and to method of obtaining compounds of formula (I) .

EFFECT: compounds of formula (I), intended for activation of EDG-1 receptor and applied for wound healing.

16 cl, 2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of structural formula

,

having Aβ42 secretion inhibiting activity. In formula I , hetaryl I is a five- or six-member heteroaryl group containing 1-3 heteroatoms selected from O, S or N, hetaryl II is a five- or six-member heteroaryl group containing 1-3 heteroatoms as defined above for hetaryl I, or is a bicyclic ring system containing 1-4 heteroatoms selected from S, O or N, where at least one ring is aromatic by nature, R1 is C1-7-alkyl, C1-7-alkoxy, C1-7-alkyl substituted with a halogen, or a halogen; R2 is a halogen, C1-7-alkyl, C1-7-alkoxy, hydroxy, C1-7-alkyl substituted with a halogen, C1-7-alkyl substituted with a hydroxy, or benzo[1,3]dioxolyl or is -(CHR)p-phenyl, optionally substituted with a halogen, C1-7-alkyl, C1-7-alkoxy, S(O)2-C1-7-alkyl, cyano, nitro, C1-7-alkoxy substituted with a halogen, dimethylamino, -(CH2)p-NHC(O)O-C1-7-alkyl or C1-7-alkyl, substituted with a halogen. The values of radicals R, R3, R4,p, n, m, o are given in the claim.

EFFECT: invention relates to a method of producing said compounds, a medicinal agent containing said compounds and a method of treating Alzheimer's disease, cerebral amyloid angiopathy, Hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), vascular dementia, dementia pugilistica or Down syndrome, associated with β amyloid activity.

21 cl, 283 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to 5,5-condensed heteroarylene compounds IIIB, where U2, V1, V2 and W1 are selected from O, N, NH, S or CR3a; U1, W2, X1 and X2 represent C or N; R1 and R2 represents hydrogen, -C(O)CH(NR1bR1c)R1a, -C(O)CH(N(R1c)C(O)OR1b)R1a or -C(O)OR1a; R3a represents hydrogen or R3; R3 represents halogen or -C(O)OR1a; L1 and L2 are such as given in invention formula, each Z1 and Z2 represents bond or -O-; each Rla, R1b and R1c represents hydrogen, C1-6 alkyl or C6-14 aryl; or Rlb and Rlc together with N atom, which they are bound to, form 5-6-membered heterocyclyl; q, r, s, t and u equal 1. Invention also relates to pharmaceutical compositions, containing 5,5-condensed heteroarylene compounds, and methods of treating or preventing HCV infection.

EFFECT: 5,5-condensed heteroarylene derivatives, possessing inhibiting activity with respect to hepatitis C virus.

43 cl, 42 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a novel method of obtaining fluorescent catecholamines selected from dopamine and adrenalin, and their metabolites, selected from homovanillic and vanillin-mandelic acids, by a method of derivation. The compounds can be used as highly sensitive and selective markers for the determination of various diseases. The method of derivation includes oxidation of the initial compounds and their interaction with amines that form condensed structures in a medium of the CAPS-buffer solution or glycin - KOH 0.2 mM hydrogen peroxide in the presence of horseradish peroxidase as a catalyst. The process in preferably carried out in a 0.1 M buffer solution with the concentration of horseradish peroxidase 0.01-1 mcM; concentration of hydrogen peroxide - 100 mcM, amine concentration - 0.1-33 mM; concentration of catecholamines and metabolites - 0.03-1 mcM.

EFFECT: method is simple and producible as it does not require higher temperature and is realised in a water solution.

2 cl, 2 dwg, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a number of substituted dihydrobenzocycloalkyloxymethyl oxazolpyrimidinone of formula

wherein n represents 1, 2 or 3; R1 represents hydrogen, methyl, fluoromethyl, ethyl, 2-fluoroethyl and propyl; R2 is specified in a group consisting of hydrogen, methyl, fluoromethyl, ethyl, 2-fluoroethyl, propyl, 1,1-difluoropropyl, methoxymethyl and 2-fluoroethoxymethyl; R3 and R4 represent (C1-C4)alkyl; and R5 and R6 are identical or different and are independently specified in a group consisting of hydrogen, halogen, (C1-C4)alkyl and (C1-C4)alkoxy. The invention also refers to specific compounds specified in cl.8 of the patent claim, to compounds of formula

a pharmaceutical composition and the use of the declared compounds.

EFFECT: dihydrobenzocycloalkyl-oxymethyloxazolpyrimidinone as metabotropic glutamate receptor mGluR2 modulators.

14 cl, 1 tbl, 15 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to nitroimidazoxazine derivatives of formula , wherein X represents O, OCH2, OCH2CH=CH or OCH2C≡C; Y represents a group of any of formulas IIa-IIc, wherein means an attachment point to X, and Z in formulas

represents CH2, CH=CH, C≡C or a direct bond; the numbers 2, 3 and 4 are positions of a terminal ring having R1 as a substitute; the terminal ring of formula I comprises C, CH or one nitrogen atom in each position, and each of R1 and R2 in formulas I and IIa represents one or two substitutes found in any accessible position of the ring and independently represents H, F, Cl, CF3, OCF2H, OCF3 or combinations thereof. Besides, the invention refers to a pharmaceutical compound based on a compound of formula I, a method of treating a microbial infection, specific compounds.

EFFECT: there are prepared new compound effective in treating the microbial infections, including in treating the diseases caused by Mycobacterium tuberculosis.

8 cl, 28 dwg, 3 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to nitroimidazooxazine derivatives of general formula I, where n equals 1, V and W independently denote H or CH3, and one of X and Y is H and the other is one of the formulae and , where formula IIa includes a single ring labelled at position 3 and position 4 and containing R1 as a substitute, and formula IIb includes a first ring labelled at position 3 and position 4 and containing as substitutes both R2 and a terminal ring, labelled at position 4 and containing R1 as a substitute, where the single ring of formula IIa and the first ring and the terminal ring of formula IIb include C, CH, or N at each ring position, where the single ring of formula IIa and the first ring and the terminal ring of formula IIb independently contain no more than two nitrogen atoms; Z in formulae IIa and IIb is CH2 or a direct bond, R1 is independently any one or two of H, F, C1, CF3, OCF3 or OCH2Ph, and R2 is H. The invention also relates to a pharmaceutical composition based on the compound of formula I, a method of preventing and treating a microbial infection based on use of the compound of formula , and specific nitroimidazooxazine derivatives.

EFFECT: obtaining novel compounds with useful biological activity.

7 cl, 21 dwg, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to heterocyclic compounds of formula I

and to their pharmaceutically acceptable salts, where A is selected from CH or N; R1 is selected from the group, consisting of C3-6-cycloalkyl, C3-6-cycloalkyl-C1-7-alkyl, C1-7-alkoxy-C1-7-alkyl, halogen-C1-7-alkyl; R2 and R6 independently on each other represent hydrogen of halogen; R3 and R5 independently on each other are selected from the group, consisting of hydrogen, C1-7-alkyl and halogen; R4 is selected from the group, consisting of hydrogen, C1-7-alkyl, halogen and amino; R7 is selected from the group, consisting of C1-7-alkyl, C1-7alkoxy-C1-7-alkyl, C1-7-alkoxyimino-C1-7-alkyl, 4-6-membered heterocyclyl, containing one heteroatom O, phenyl, with said phenyl being non-substituted or substituted with one hydroxy group, and 5-10-membered heteroaryl, containing 1-3 heteroatoms, selected from N, S and O, said heteroaryl is not substituted or is substituted with one or two groups, selected from the group, consisting of C1-7-alkyl, hydroxy, C1-7-alkoxy, cyano, C1-7-alkylaminocarbonyl and halogen. Invention also relates to pharmaceutical composition based on formula I compound and to method of obtaining formula I compound.

EFFECT: obtained are novel heterocyclic compounds, which are agents, increasing level of LDLP.

17 cl, 2 tbl, 89 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new (R)-stereoisomers of substituted 2-thioxo-imidazolidin-4-ones of formula 1 or to spiroanalogues thereof, which possess the properties of an androgen receptor agonist, to versions of a method for producing them, and to intermediate compounds 2.1-2.4 for producing compounds of formula 1. The invention also refers to a pharmaceutical composition presented in the form of tablets, capsules, injections. In formula 1 R1 represents OH, NH2, or OR4 group; R2 and R3 represent methyl, or R2 and R3 represent CH2-CH2 group; R4 represent C1-C4alkyl or cyclopropyl. The compounds 2.1-2.4 are described by structural formulas:

EFFECT: compounds of formula 1 can be used for producing the medicinal product applicable for treating a cancer disease, such as prostate cancer, breast cancer.

17 cl, 1 tbl, 10 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing pyrazoline carboxamidine derivatives of formula . Said compounds are known as powerful 5-HT6 antagonists. The disclosed method comprises reacting a corresponding substituted 4,5-dihydro-(1H)-pyrazole or an isomer thereof with isothiocyanate R6-N=C=S to obtain an amide of substituted 4,5-dihydro-(1H)-pyrazole-1-carbothioic acid or tautomeric substituted 4,5-dihydro-(1H)-pyrazole-1-carboxymidothioic acid . The obtained intermediate compounds are reacted with a corresponding alkylating agent to obtain an intermediate S-alkylated compound . Said intermediate compound is reacted with a sulphonamide derivative R7SO2NH2 and the target compound of formula (I) is separated from the reaction mixture. The invention also relates to novel intermediate products (IIIa), (IIIb) and (IV). Symbols given in the formulae have values given in the description.

EFFECT: providing an alternative method which improves atom efficiency of synthesis of desired compounds with higher output compared to existing methods for synthesis of said compounds.

8 cl, 1 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted 3-(4-methylcarbamoyl-3-fluorophenylamino)tetrahydrofuran-3-ene carboxylic acid or esters thereof of general formula 1 and stereoisomers. The compounds of formula 1 are intermediate products in synthesis of androgen receptor inhibitors of formula A1, A2, A3, which are of interest as anticancer drugs. The invention also relates to methods of producing compounds of formula 1 and compounds of formulae A1, A2, A3. In general formula 1 R1=H, C1-C4alkyl; R2=H, CH2OCH2CH2Si(CH3)3. The method of producing compounds of formula (1) involves reacting compounds of general formula 2 with compounds 3(1) or 3(2) in dimethylformamide, K2CO3 while simultaneously adding copper iodide, water and triethylamine to the reaction mass. 2: By reacting compounds of formula 1, obtained using said method, with 4-isothiocyanato-2-trifluoromethylbenzonitrile in a mixture of dimethyl sulphoxide and ethyl acetate in ratio of 1:2 and at high temperature, compounds A1, A2, A3, whose structure is given in the claim, are obtained, respectively.

EFFECT: use of novel intermediate products improves output and stereoselectivity of the method of producing compounds A1, A2, A3.

4 cl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention describes a group of substituted N-phenylbipyrrolidincarboxamides of formula (I), where m equals 1 or 2; n equals to 1 or 2; p equals to 1 or 2; R1 is hydrogen, (C1-C4)-alkyl, CF3, (C1-C4)-alkoxy-(C1-C4)-alkyl; and R2 is hydrogen, halogen, (C1-C4)-alkyl or CF3; or their salt, or enantiomer, or diastereomer. In particular, compounds in accordance with the invention are modulators of H3 receptors and, therefore, are suitable for application as pharmaceutical preparations, in particular, in treatment and (or) prevention of different diseases, modulated by H3 receptors, including diseases associated with the central nervous system.

EFFECT: obtained are novel compounds, possessing useful biological properties.

15 cl, 1 tbl, 44 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to spiro-5,6-dihydro-4H-2,3,5,10b-tetra-aza-benzo[e]azulene derivatives of formula I, where X-Y represents C(RaRb)-O, where each of Ra and Rb independently represents H or C1-4-alkyl, C(RcRd)-S(O)p, where each of Rc and Rd independently represents H, C(O)O, CH2OCH2, CH2CH2O, Z represents CH or N; R1 represents halogeno, R2 represents H, C1-6-alkyl, non-substituted or having as substituents one OH, -(CH2)q-Re, where Re represents pyridyl, -C(O)-C1-6-alkyl, -C(O)(CH2)qNRiRii, -C(O)O-C1-6-alkyl, -S(O)2NRiRii, each of Ri and Rii independently represents C1-6-alkyl, R3 represents Cl or F, n has value 1 or 2, m has value 0, 1, p has value 0 or 2, q has value 1, or to their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition, possessing antagonistic activity with respect to receptors V1a, on the basis of said compounds.

EFFECT: obtained are novel compounds and pharmaceutical composition on their basis, which can be applied in medicine as drugs of peripheral and central action in case of the following states: dysmenorrhea, male or female sexual disfunction, hypertension, chronic heart failure, inadequate secretion of vasopressin, liver cirrhosis, nephritic syndrome, anxiety, depressive disorders, obsessive-compulsive disorder, autism spectrum disorders, schizophrenia and aggressive behaviour.

20 cl, 10 tbl, 37 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula I where A is such as given in the invention formula, R is selected from the group consisting of H and C1-6 alkyl, n and p each is independently selected from 0, 1 and 2, on condition that n + p = 2; Y represents -O- or -S-; R1, R2, R3, R4 in each position are independently selected from H and C1-6 alkyl; R5 is selected from the group consisting of -C(O)-CH2-indol-3-yl, -C(O)-(CH2)2-indol-3-yl, -C(O)-(CH2)3-indol-3-yl, trans -C(O)-(CH=CH)-indol-3-yl, -SO2-4-fluorophenyl, -C(O)-CH(n-propyl)2, -C(O)-(4-hydroxy-3,5-di-tert-butylphenyl), -C(O)-CH(NH2)-CH2-indol-3-yl and -C(O)-CH2CH3; and R6 represents H. Invention also relates to pharmaceutical composition for modulation of muscarinic receptor M1, containing formula I compounds, and methods of treating disease or state, curable by modulator of muscarinic receptor M1.

EFFECT: formula I compounds as modulators of muscarinic receptor M1.

33 cl, 1 tbl, 27 ex

FIELD: chemistry.

SUBSTANCE: invention relates to spiro derivatives of parthenin of formula , where R/R' is selected from a group consisting of phenyl or a substituted phenyl such as 4-ClC6H4, 2-NO2C6H4; 2,4-(MeO)2C6H3, 4-MeC6H4, and formula , where R is 4-MeOC6H4, 2-NO2C6H4, 3-NO2C6H4, 3-MeC6H4, 3-MeCO2C6H4. The invention also relates to methods of producing said spiro derivatives and a pharmaceutical composition based on said derivatives.

EFFECT: compounds of formula 1b and 1d have anticancer activity.

14 cl, 6 dwg, 6 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to spirocyclic cyclohexane derivatives of formula I where values of R1-10 are given in claim 1.

EFFECT: compounds have affinity for the ORL1 receptor, which enables use thereof in producing a medicinal agent for treating pain, especially sharp, neuropathic or chronic pain.

12 cl, 1 tbl, 52 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel spiro-linked 3H-pyrroles - 8-amino-1-imino-6-morpholin-4-yl-2-oxa-7-azaspiro[4.4]nona-3,6,8-triene-9-carbonitriles of general formula (1) , where R1=R2=CH3 (1a); R1+R2=(CH2)5 (1b); R1+R2=(CH2)6 (1c); R1+R2=(CH2)10 (1d). The method involves suspension of the corresponding 4-oxoalkane-1,1,2,2-tetracarbonitrile of formula (2) , , R1=R2=CH3 (2a); R1+R2=(CH2)5 (2b); R1+R2=(CH2)6 (2c); R1+R2=(CH2)10 (2d) in a mixture of water and propanol-2 in ratio of 10:1, followed by addition of morpholine in molar ratio of 1:2.

EFFECT: high efficiency of the method.

2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (IX) wherein radicals and symbols have values given in the claim, and pharmaceutically acceptable salts or tautomers thereof. Said compounds are inhibitors of poly(ADP-ribose)polymerase (PARP) and can be used to treat cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitisers for cancer treatment. The invention also relates to a pharmaceutical composition containing said compounds, use of said compounds and a method of treating said diseases.

EFFECT: high efficiency of using the compounds.

10 cl, 18 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to derivatives of diaza-spiro[4.5]decan-1-one of formula (I) or to their pharmaceutically acceptable salts, where. R1 is a substituted phenyl, which contains one substituent, selected from the group, including C1-4-alkyl, C3-6-cycloalkyl halo-C1-4-alkyl and halo -C1-4-alkoxy, and which can additionally contain one substituent, selected from a halogen; R2 is hydrogen, C1-4-alkyl, phenyl, substituted phenyl, with the substituted phenyl containing one substituent, selected from the group, including C1-4-alkoxy; R3 is -R4, -C(OH)R5R6 or -C(O)NR7R8; R4 is phenyl, phenyl-C1-4-alkyl, substituted phenyl, substituted phenylcarbonyl, with the substituted phenyl, substituted phenylcarbonyl containing from one to two substituents, selected from the group, including a halogen, halo-C1-4-alkyl; one of R5 and R6 is hydrogen, C1-4-alkyl, and the other is aminocarbonyl, phenyl, substituted phenyl or substituted phenyl-C1-4-alkyl, with the substituted phenyl or substituted phenyl-C1-4-alkyl containing from one to two substituents, independently selected from the group, including a halogen; one of R7 and R8 is hydrogen C1-4-alkyl, and the other is C1-4-alkyl, C3-6-cycloalkyl, C1-4-alkoxy-C1-4-alkyl, phenyl-C1-4-alkyl, substituted phenyl or substituted phenyl-C1-4-alkyl, with the substituted phenyl or substituted phenyl-C1-4-alkyl containing one substituent, selected from the group, including a halogen, halo-C1-4-alkyl; or R7 and R8 together with a nitrogen atom, which they are bound to, form pyrrolidinyl; n equals zero or 1/ The invention also relates to a pharmaceutical composition based on the compound of formula (I), application of the formula (I) compound and a method of treatment.

EFFECT: obtained are novel heterocyclic compounds, useful as an inhibitor of hormone-sensitive lipase.

17 cl, 57 ex

Up!