Derivatives of 2-(hereto)aryl-substituted tetrahydroquinolines

IPC classes for russian patent Derivatives of 2-(hereto)aryl-substituted tetrahydroquinolines (RU 2375354):

C07D493/04 - Ortho-condensed systems

C07D401/04 - directly linked by a ring-member-to-ring- member bond

A61P43 - Drugs for specific purposes, not provided for in groups ; A61P0001000000-A61P0041000000

A61P35 - Antineoplastic agents

A61K31/47 - Quinolines; Isoquinolines

Another patents in same IPC classes:

Method of polyolefin composition nucleation by acetal compounds / 2348637

Invention concerns method of polyolefin composition nucleation by mixing the composition with compound of the structural formula: , where: n is 0, 1 or 2; Ar₁ and Ar₂ are independently selected out of group including non-substituted aryl groups and aryl groups substituted by substitutes selected out of group including alkyl groups, alkenyl groups, alkinyl groups, alkoxy groups, carboxy groups and halogens; and R is selected out of group including alkenyl groups, alkyl groups, alkoxy groups, hydroxyalkyl groups and alkylhalide groups. Also invention claims the compound itself, method of its obtaining and moulded or cast polyolefin article including this compound.

Method of obtaining epotilone derivatives / 2343155

Method ensures carrying out aldole condensation in presence of epoxide mesilate and tosilate, using auxiliary chiral sultamic group as carboxyl- protecting group, as a result, reduction and oxidation stages, requiring extra time, before carrying out final stage of macrolactonisation are excluded. Introduction of epoxidic group at early stages of method allows also excluding stage of epoxilation of more complex intermediate compounds at further stages of process.

New tetracyclic compounds containing heteroatom, used as selective modulators of oestrogen receptors / 2331645

Invention pertains to new tetracyclic compounds containing a heteroatom. The compounds can be used in treating and/or prevention of disorders, associated with oestrogen depletion, such as hot flash, vaginal dryness, osteopenia and osteoporosis; sensitive cancerous diseases hormone and hyperplasia of the lacteal gland, endometrium, cervix uteri and prostate; endometriosis, uterus fibrosis and osteoarthritis, and as contraceptive agents, used either separately or combined with progestogen or a progestogen antagonist.

Analogs of himbacin, their using and pharmaceutical composition based on thereof possessing property of thrombin receptor antagonist / 2319704

Invention relates to heterocycle-substituted tricyclic compounds of the formula (I): or their pharmaceutically acceptable salts wherein R means hydrogen atom; R¹ and R² are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R³ means hydrogen atom; n₁ and n₂ = 0-3 independently under condition that they both do not mean 0; Het means pyridyl wherein pyridyl is added to B through cyclic carbon atom and it comprises from 1 to 4 substitutes (W) chosen independently from group comprising -NR⁴R⁵, -NHCOR²⁶, -NHSO₂R¹⁶; R²¹ means aryl and R²¹ means heteroaryl wherein heteroaryl represents furyl, thienyl, pyridyl, thiazolyl, pyrrolidinyl, azethidinyl; R⁴ and R⁵ mean hydrogen atom or alkyl comprising 1-6 carbon atoms, or R⁴ and R⁵ mean in common -(CH₂)₃-, -(CH₂)₄-, -(CH₂)₅- or -(CH₂)₂NR⁷-(CH₂)₂- wherein R⁷ means hydrogen atom or alkyl comprising 1-6 carbon atoms; R⁸, R, R¹⁰ and R¹¹ mean hydrogen atom; B means -(CH₂)_n4CR¹²=CR^12a(CH₂)_n5 wherein n₄ and n₅ = 0-2 independently; R¹² and R^12a are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R²¹ means from 1 to 3 substitutes chosen independently from group comprising hydrogen atom, trifluoromethyl, trifluoromethoxy, halogen atom, cyano, alkyl comprising 1-6 carbon atoms, alkoxy group comprising 1-6 carbon atoms, or -CR²⁹(=NOR²⁸); R²² means -COR²³, -S(O)R³¹, -S(O)₂R³¹ or -COOR²⁷; R²³ means cycloalkyl comprising 3-7 carbon atoms, (C₃-C₇)-cycloalkyl-(C₁-C₆)-alkyl, cycloalkyl comprising 3-7 carbon atoms containing from 1 to 3 substitutes chosen from group comprising halogen atom, (C₁-C₃)-alkoxy-(C₁-C₃)-alkyl, hydroxy group and alkoxy group comprising 1-6 carbon atoms, aryl, aryl-(C₂-C₆)-alkyl; R²⁷ means alkyl comprising 1-6 carbon atoms, phenyl or benzyl; R²⁸ and R²⁹ are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R³¹ means alkyl comprising 1-6 carbon atoms, halogenalkyl comprising 1-6 carbon atoms, aryl, aryl-(C₁-C₆)-alkyl. Also, invention relates to pharmaceutical compositions containing these substances and their using for preparing a drug used in treatment of thrombosis, atherosclerosis, restenosis, hypertension, stenocardia, arrhythmia, heart failure and cancer.

Azaheterocycles, combinatory library, focused library, pharmaceutical composition and method for preparing (variants) / 2318818

Invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C₅-C₇)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; R^a ₁ represents a substitute of amino group but not hydrogen atom, such as substituted (C₁-C₆)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; R^b represents carbamoyl group -C(O)NHR^a wherein R^a represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; R^c represents a substitute of cyclic system, such as possibly substituted (C₁-C₆)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or R^b and R^c form in common aminocyanomethylene group [(=C(NH₂)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.

C-glycoside derivatives and their salts / 2317288

Invention relates to novel compounds representing C-glycoside derivatives and their salts of the formula: wherein ring A represents (1) benzene ring; (2) five- or six-membered monocyclic heteroaryl ring comprising 1, 2 or 4 heteroatoms chosen from nitrogen (N) and sulfur (S) atoms but with exception of tetrazoles, or (3) unsaturated nine-membered bicyclic heterocycle comprising 1 heteroatom representing oxygen atom (O); ring B represents (1) unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (2) saturated or unsaturated five- or six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (3) unsaturated nine-membered bicyclic carbocycle, or (4) benzene ring; X represents a bond or lower alkylene wherein values for ring A, ring B and X correlate so manner that (1) when ring A represents benzene ring then ring B is not benzene ring, or (2) when ring A represents benzene ring and ring B represents unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O and comprising benzene ring or unsaturated nine-membered bicyclic carbocycle comprising benzene ring then X is bound to ring B in moiety distinct from benzene ring comprised in ring B; each among R¹-R⁴ represents separately hydrogen atom, -C(=O)-lower alkyl or lower alkylene-aryl; each R⁵-R¹¹ represents separately hydrogen atom, lower alkyl, halogen atom, -OH, =O, -NH₂, halogen-substituted lower alkyl-sulfonyl, phenyl, saturated six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N and O, lower alkylene-OH, lower alkyl, -COOH, -CN, -C(=O)-O-lower alkyl, -O-lower alkyl, -O-cycloalkyl, -O-lower alkylene-OH, -O-lower alkylene-O-lower alkyl, -O-lower alkylene-COOH, -O-lower alkylene-C(=O)-O-lower alkyl, -O-lower alkylene-C(=O)-NH₂, -O-lower alkylene-C(=O)-N-(lower alkyl)₂, -O-lower alkylene-CH(OH)-CH₂(OH), -O-lower alkylene-NH, -O-lower alkylene-NH-lower alkyl, -O-lower alkylene-N-(lower alkyl)₂, -O-lower alkylene-NH-C(=O)-lower alkyl, -NH-lower alkyl, -N-(lower alkyl)₂, -NH-lower alkylene-OH or NH-C(=O)-lower alkyl. Indicated derivatives can be used as inhibitor of co-transporter of Na⁺-glucose and especially as a therapeutic and/or prophylactic agent in diabetes mellitus, such as insulin-dependent diabetes mellitus (diabetes mellitus 1 type) and non-insulin-dependent diabetes mellitus (diabetes mellitus 2 type), and in diseases associated with diabetes mellitus, such as insulin-resistant diseases and obesity.

Tetracyclic heterocompounds as estrogen receptor modulating agents / 2305099

Invention relates to novel tetracyclic heterocompounds of the formula (I): wherein X, Y, Z, R¹ - R⁴, n and m has values given in the invention description and used as selective modulating agents for estrogen receptors. Also, invention relates to a method for synthesis of these compounds and pharmaceutical compositions comprising thereof, and their using in treatment and/or prophylaxis of disorders mediated by one or more estrogen receptors. Proposed compounds are useful in treatment and/or prophylaxis of disorders associated with depleting estrogen and comprising such disorders as rush of blood, vaginal dryness, osteopenia and osteoporosis, hormone-dependent cancer and hyperplasia of breast, endometrium, uterus cervix and prostate, endometriosis, uterus fibroma, osteoarthritis that can be used as contraceptive agents both separately and in combination with progestogen or progestogenous antagonist.

Method for isolating epotilons from reaction mixture and desorption from synthetic resin (variants), using low-polar or nonpolar solvent for realization of method / 2285007

Invention relates to a method for isolation of epotilons used in medicine in treatment of cancer diseases. Method for desorption of epotilons A, B, D and/or E from synthetic resin is based on using low-polar or nonpolar solvent chosen from the group comprising (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Used aromatic solvent is chosen from the group including naphthalene, benzene or naphthalene and benzene substituted with one or some substitutes chosen from the following group: (lower)-alkyl, (lower)-alkoxy-group, halogen atom, nitro-group and (lower)-alkoxy-(lower)-alkyl wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Solvent is removed to the required level but up to preparing a dry residue preferably. If necessary, residue is dissolved in mixture alcohol/hydrocarbon in the corresponding volume ratio. Alcoholic phase is evaporated until dry and then alcoholic extract is crystallized from mixture alcohol and hydrocarbon. Then formed crystallized product is dissolved in mixture nitrile/water but preferably in mixture acetonitrile/water taken in the ratio = 2:3 (vol./vol.). Formed solution is applied on column (if necessary, after separation for some distillates) for preparative chromatography in reversed phase followed by elution with mixture nitrile/water, removing nitrile and extraction of an aqueous phase with ester. Ester extract is evaporated and formed product is subjected for crystallization. Method for preparing epotilons A, B, D and/or E from resin or reaction mixture involves the following steps: (a) desorption of epotilons with low-polar or nonpolar solvent chosen from the group including (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents being the desorption step can be repeated up to achievement of the more complete desorption; (b) removal of solvent used in desorption from formed solutions by evaporation; (c) optional crystallization of epotilon(s) after desorption and first of all for crystallization of epotilon B by addition of mixture of alcohol with hydrocarbon and the following evaporation of alcoholic phase until dry and crystallization of epotilon B from the corresponding mixture of solvents; (d) (obligatory step) separation of epotilons by method of chromatography in reversed phase and the following dissolving a residue obtained in previous step in suitable solvent, elution with mixture nitrile/water and removing nitrile from epotilon-containing fractions by evaporation. If necessary, water remained with epotilon is extracted with ester followed by evaporation of epotilon-containing ester phase until dry; (e) optional purification by adsorption chromatography method, and final recrystallization of purified epotilon from corresponding solvents or mixture of solvents. If necessary, in this process between each step formed solutions or suspensions are concentrated, and/or liquid or solid components are separated of one another. Separation of epotilons A and B is carried out by chromatography method based on a mobile layer modeling. Invention provides simplifying methods for preparing large amounts of epotilons for satisfying requirement in these agents.

Crystals of taxane derivatives and method for their preparing / 2284328

Invention relates to a novel crystalline form of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylideneoxy]-5,20-epoxy-1-hydroxytax-11-ene-13-yl-(2R,3S)-3-(tert.-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate that shows the diffraction picture of roentgen rays in powder with characteristic peaks at diffraction angles (θ)= 6.2^o, 10.3^o, 10.7, 11.4^o and 12.0, and a method for its preparing. Method involves carrying out the crystallization step by using organic solvent chosen from group consisting of ketone type solvent, nitrile solvent type and their mixture, or mixture of said solvent and water. Also, invention relates to an antitumor agent based on the prepared crystalline form. Invention provides the stable quality of a medicinal agent based on its lower hygroscopicity.

Method for preparing 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens / 2282633

Invention relates to a method for synthesis of new compounds, namely, 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens of the formula: (Ia-f): wherein (Ia): R means hydrogen atom (H); R₁ means hydrogen atom (H); (Ib): R means bromine atom (Br); R₁ means hydrogen atom (H); (Ic): R means chlorine atom (Cl); R₁ means hydrogen atom (H); (Id): R means hydrogen atom (H); R₁ means bromine atom (Br): (Ie): R means hydrogen atom (H); R₁ means chlorine atom (Cl); (If): R means methoxy-group (-OCH₃); R₁ means hydrogen atom. Method involves formation of condensed tetracyclic system as result of the successive recyclization reactions of furan ring of derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol and the secondary cyclization of formed isochromen ketone in boiling of solution containing derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol of the formula: in ethanol medium in the presence of hydrogen chloride alcoholic solution for 15-40 min. Invention provides synthesis of new derivatives of isochromens possessing the potential anti-inflammatory activity.

Amide derivatives / 2375352

Invention refers to new compounds of formula I, to its pharmaceutically acceptable salts exhibiting properties of inhibitors of cytokine production, such as TNF (tumour necrosis factor) and various members of interleukins (IL) family, and properties of kinase inhibitors, particularly p38α kinase. The invention also concerns methods for producing; pharmaceutical compositions and application thereof for making the medicines for treating diseases affected by the compound of the invention with specified activity. In formula I , m represents 0, 1 or 2; R¹ represents halogeno, hydroxy, (1-6C) alkyl, (1-6C)alkoxy, (2-6C)alkenyl, (2-6C) alkinyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, amino-(2-6C) alkoxy, (1-6C)alkylamino-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, N-(1-6C)alkylcarbamoyl - (1-6C)alkoxy, di[(1-6C) alkyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkylamino, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy and wherein any heteroaryl or heterocyclyl group in substitute representing R¹, can probably have 1 or 2 substitutes chosen from hydroxy, halogeno, (1-6C) alkyl, (2-6C)alkinyl, (3-6C)cycloalkyl, (3-6C)cycloalkyl-(1-6C)alkyl, (1-6C)alkoxycarbonyl, (2-6C) alkanoyl, halogen-(1-6C)alkyl, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, cyano-(1-6C)alkyl, carboxy- (1-6C)alkyl and methylsulphonyl and wherein any said substitute representing R¹ which contains group CH₂ attached to 2 carbon atoms, or group CH₃ attached to carbon or nitrogen atom, can probably have with each specified group CH₂ or CH₃, one or two substitutes chosen from halogeno, hydroxy, amino, triflouromethyl, oxo, carboxy, acetamido, (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)alkoxy, (1-6C)alkyamino, di-[(1-6C)alkyl]amino, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, halogen-(1-6C)alkyl, (1-6C)alkoxycarbonyl, carbamoyl, N, N-di-[(1-6)alkyl]carbamoyl, (1-6C)alkylsulphonyl, heteroaryl, heteroaryl-(1-6)alkyl and heterocyclyloxy and wherein any heterocyclyl group in substitute representing R¹, can probably have 1 oxo-subsitute; R² represents trifluoromethyl or (1-6C)alkyl; R³ represents hydrogen or (1-6C)alkyl; and R⁴ represents (3-6C)cycloalkyl, and R⁴ can be optionally substituted with one or more substitutes chosen from (1-6C)alkyl; and wherein heteroaryl represents aromatic 5- or 6-merous monocyclic ring containing one or two heteroatoms chosen from oxygen, nitrogen and sulphur; heterocyclyl represents saturated 3-10-merous monocyclic or bicyclic ring, each containing one or two heteroatoms chosen from oxygen, nitrogen and sulphur.

Double nk1/nk3 antagonists for treating schizophrenia / 2374229

Present invention relates to use of compounds of formula (I) where R¹ is lower alkyl or halogen; R² is hydrogen or halogen; R³ is (CHR')_nOH, phenyl, possibly substituted with a -(CHR')_nOH group, or is a saturated, partially saturated or aromatic 5- or 6-member heterocyclic ring with one heteroatom, selected from a group which consists of -N(R⁴)-, -N=, -S- or -S(O)₂, where the rings are possibly substituted with a -(CHR')_nOH group; R' is hydrogen or a -(CH₂)_nOH, independent of the value of n; R⁴ is hydrogen, -S(O₂)-lower alkyl group or -C(O)-lower alkyl; X is -O-, -CH₂O-, -S- or a bond; n equals 1 or 2; or their pharmaceutically active acid addition salts for making medicine for treating schizophrenia, as well as to compounds of formula (I).

Phenyl substituted pyrrolidones / 2371433

Present invention relates to phenyl substituted pyrrolidones of formula: , where R¹ and R⁵ represent substitutes, which are independently chosen from a group which contains H, CN, halogen, C₁-C₄alkyl and OR⁸, where R⁸ represents C₁-C₄alkyl, R² and R⁴ represent substitutes, which are chosen from a group which contains H, halogen, CN and C₁-C₄alkyl, R³ represents H, R⁶ represents a condensed phenyl heterocyclic ring system, chosen from , where R¹⁶ represents a substitute, chosen from a group which contains H, C(O)NR¹⁸R¹⁹ and S(O)₂R²⁰, where R¹⁸ and R¹⁹ represent H or C₁-C₆alkyl; R²⁰ represents C₁-C₆alkyl or phenyl; and R¹⁷ represents a substitute, which is chosen from a group which contains H, NH₂, (CH₂)_mOH, C(O)NR²¹R²², SO₂R²³ and NHSO₂R²³; where R²¹ and R²² represent substitutes, which are independently chosen from a group which contains H and substituted or unsubstituted C₁-C₆alkyl, or, together with a nitrogen atom to which they are bonded, optionally form a ring; R²³ represents C₁-C₆alkyl; and m equals 1; or R⁶ represents a group, where R⁹ and R¹¹ represent substitutes, which are independently chosen from a group which contains H, halogen, CN, C(O)NR¹²R¹², NR¹²R¹² and OR¹², where each R¹² represents H or C₁-C₄alkyl, and under the condition that, at least one of substitutes R⁹ and R¹¹ is not hydrogen; R¹⁰ represents CN, NR¹³R¹⁴, SO₂NHR¹³, NHSO₂R¹³, O(CH₂)_nSO₂R¹⁵, SO₂R¹⁵, SO₂(CH₂)_nNR¹³R¹⁴ or C(O)NR¹³R¹⁴, where R¹³ and R¹⁴ represent H or C₁-C₄alkyl; R¹⁵ represents C₁-C₄alkyl, n equals 1-2, and R⁷ represents halogen, C₁-C₄alkyl, C₂-C₄alkenyl or C₂-C₄alkynyl.

N-phenyl-2-pyrimidine derivatives / 2370493

Invention concerns novel compounds of the formula I , where R₃ is (4-methylpiperazinyl)methyl and the other four radicals R₁, R₂, R₄, and R₅ are independently hydrogen; cyano; lower alkyl; hydroxy- or amino-substituted simple alkyl; trifluoromethyl; free or etherified hydroxy-group; (lower)alkoxy; (lower)alkanoyloxy; free, alkylated or acylated amino group; mono- or di(lower)alkylamino; (lower)alkanoylamino; benzoylamino; free or etherified carboxy-group; (lower)alkoxycarbonyl, and halogen; R₆ is halogen, NH₂, NO₂, NHC(O)CF₃, NHC(O)CH₃ or NHC(NH)NH₂, R₇ is methyl, and R₈ is hydrogen; or the compound salt, or crystalline form, method of obtainment, application in obtaining compound of the formula IV, and pharmaceutical composition for leukemia treatment, based on the claimed compounds.

Piperizinylpiperidine derivatives as chemokine receptor antagonists / 2369604

Invention relates to compounds of formula I, with activity towards chemokine receptor, which can be used for treating immune or viral diseases I, where R¹ is heteroaryl; R² is H, heteroaryl, OR⁹ or SR⁹; R³ is F, Cl, Br, I, C₁-C₄ halogenalkyl or heteroaryl; R⁴ is C₁-C₆ alkyl; R⁵ is C₁-C₆ alkyl; R⁹ is H, C₁-C₆ alkyl, alkoxyalkyl or heteroaryl; r is 1 or 2.

New insecticides / 2369603

Description is given of a compound of formula (VIIa), in which R₀₁ represents hydrogen; amino group or nitro group; R₀₂ represents hydrogen or C₁-C₄alkyl; R₀₃ represents C₁-C₄alkyl, C₁-C₄alkyl, mono- or disubstituted with a cyano group, COOH, nitro group, C₁-C₄alkoxy group or cyclopropyl and other substitutes, indicated in paragraph 1 of the formula of invention; R₀₄ represents C₁-C₄halogenalkyl; R₀₅ represents a halogen; each of R₀₆ and R₀₁₀, which can be identical or different, represents hydrogen, C₁-C₆alkyl, C₁-C₆alkoxycarbonyloxy group, C₁-C₆alkylcarbonylamino group, hydroxy group, cyano group, halogen or C₁-C₆alkoxy group; R₀₇ represents hydrogen, nitro group or halogen; Y₀₁ represents C(R₀₈); R₀₈ represents hydrogen, halogen, C₁-C₄alkyl or nitro group; Y₀₂ represents C(R₀₉) and R09 represents hydrogen, phenyl, halogen substituted phenyl, or halogen. Described also is an insecticide composition, insect control method and plant propagation material.

New benzimidazole derivatives and their use as medicinal agents / 2369601

Invention relates to new benzimidazole derivatives with general formula (I), where A represents -CH₂-, -C(O), -C(O)-C(R_a)(R_b)-, X represents a -CH- radical; R_a and R_b independently represent a hydrogen atom or (C₁-C₆)alkyl radical; R₁ represents a hydrogen atom or (C₁-C₈)alkyl radical; R₂ represents a (C₁-C₈)alkyl radical; R₃ represents -(CH₂)_P-Z₃, -C(O)-Z'₃ or -C(O)-NH-Z"₃; Z₃ represents (C₁-C₆)alkyl, (C₂-C₆)alkenyl, (C₁-C₆)alkoxy, (C₁-C₆)alkylcarbonyl, (C₁-C₆)alkoxycarbonyl, (C₁-C₆)alkyl-N(R_N)carbonyl, (C₃-C₇)cycloalkyl, aryl, arylthio or heteroaryl radical, Z₃ is bonded to the -(CH₂)_P- through a carbon atom, heteroaryl radical, which is a 5-10- member heteroaryl, which contains 1-2 identical or different heteroatoms, chosen from sulphur, nitrogen or oxygen, and optionally substituted with one or more identical or different substitutes, chosen from halogen, nitro group or -(CH₂)_P'-V₃₀-Y₃; aryl radical, chosen from phenyl or naphthyl, optionally substituted with one or more identical or different substitutes, chosen from halogen, nitro group, cyano group, (C₂-C₆)alkenyl, pyrrolidinyl, phenyl, phenyloxy, phenylalkyloxy, 5-7- member heteroaryl, containing 1-3 nitrogen atoms and -(CH₂)_p'-V₃₁-Y₃; V₃₀ represents -O-, -C(O)-, -C(O)-O- or a covalent bond; V₃₁ represents -O-, -S-, -SO₂-, -C(O)-, -C(O)-O-, -N(RN)-, -NH-C(O)- or a covalent bond; Y₃ represents a hydrogen atom or (C₁-C₆)alkyl radical, optionally substituted with one or more identical or different halogen radicals; R_N represents a hydrogen atom or (C₁-C₆)alkyl radical; Z₃ represents a radical with a given formula (see below); Z'₃ represents a phenyl radical, optionally substituted with one ore more identical or different substitutes, chosen from -(CH₂)_P"-V'₃-Y'₃; V'₃ represents -O-; Y'₃ represents a hydrogen atom or (C₁-C₆)alkyl radical; Z"₃ represents a hydrogen atom or -(CH₂)q-A"₃ radical; A"₃ represents (C₁-C₆)alkyl, phenyl or thienyl radical; alkyl or phenyl radical can be optionally substituted with one or more identical or different substitutes, chosen from halogen and -V"₃-Y"₃; V"₃ represents -O-, -C(O)-, -C(O)-O- or a covalent bond; Y"₃ represents a hydrogen atom or (C₁-C₆)alkyl radical; p is an integer from 0 to 6; p' and p" independently represent an integer from 0 to 1; q is an integer from 0 to 2; R₄ represents a radical with formula -(CH₂)_S-R'₄; R'₄ represents a 5-7- member heterocycloalkyl, containing at least one nitrogen atom and optionally substituted with (C₁-C₆)alkyl; or a radical with formula -NW₄W'₄; W₄ represents a hydrogen atom; W'₄ represents a hydrogen atom; s is an integer from 0 to 6; in racemic or enantiomeric form or any combination of the said forms, or its pharmaceutically acceptable salt. The invention also relates to a method of obtaining a compound in paragraph 1, a pharmaceutical composition based on the said compound and its use in making a medicinal agent.

5-sulphanyl-4h-1,2,4-triazole derivative and their use as medicinal agents / 2367655

New 5-sulphanyl-4H-1,2,4-triazole derivatives of general formula I (meaning of radicals R₁-R₃ are indicated in the description of the invention), methods of their preparation by liquid-phase parallel synthesis and pharmaceutical composition are claimed.

Nitrogen-containing heterocyclic derivatives and medicaments thereof as active ingredient / 2366655

Present invention refers to the new compounds of formula (I): whereat R¹ is -SO₂NR¹⁰²R¹⁰³, -NR¹⁰¹SO₂R¹⁰⁴ or -COOR¹⁰⁵ whereat R¹⁰¹ is hydrogen atom, R¹⁰² and R¹⁰³ each independently represents hydrogen atom or C1-4 alkyl, R¹⁰⁴ is C1-4 alkyl and R¹⁰⁵ is hydrogen atom or C1-4 alkyl ; X is bond, -CH₂- or -O-; Y is -CH₂-; ring A and ring B, which are same or different, each independently is benzene, pyridine, pyrazol or piperidine which can have the following substituents: C1-4 alkyl or halogen; ring D is piperidine; R² is whereat the arrow shows the position of the bond with the ring D; R⁵¹ is (1) hydrogen atom a, (2) C1-6alkyl, which can have the following substituents: (a) hydroxy, (b) methoxy, (c) cyano, (d) carboxy, (e) halogen, (f) methyl sulphonylamino, (g) C3-8cycloalkyl or phenyl, which can have the following substituents: methyl, halogen, hydroxy or methoxy, (h) thienyl, pyrazolyl, tetrahydropyranyl, thiazolyl, isooxalyl, imidazolyl, tetraazolyl, pyridyl, pyrimidinyl which can have the following substituents: methyl, trifluoromethyl or hydroxy, (3) C2-10alkenyl, (4) C2-10alkynyl, (5) phenyl which can have the following substituents: C1-4alkyl or halogen, or (6) pyridine or tetrahydropyran; R⁵² is (1) hydrogen atom a, (2) C1-6alkyl which can have the following substituents: (a) hydroxy, (b) methoxy, (c) carboxy, (d) C3-8cycloalkyl, (e) phenyl or (f) oxo, (3) C3-8cycloalkyl or phenyl which can have the following substituents: C1-4alkyl, hydroxy, cyano, oxo, carbamoyl, N-methyl aminocarbonyl, carboxy, halogen, methoxy, trifluoromethoxy, methythio, methylsulphonyl, acetylamino, dimethylamino, acetyl, tetraazolyl, trifluoromethyl or methylsulphonylamino (4) C3-10cycloalkenyl, (5) adamantyl, (6) thienyl, pyrazolyl, tetrahydropyranyl, isoxaazolyl, isothiazolyl, thiadiazolyl, piperidinyl, pyridyl, pyrimidinyl, pyridazinyl, quinolyl, indolyl, benzothiazolyl, benzoisothiazolyl, benzotriazolyl, dioxaindanyl, benzodioxaindanyl which can have the following substituents: C1-4alkyl, hydroxy, oxo, halogen, azido or trifluoromethyl or (7) benzyloxy groups; and R⁵³ is hydrogen atom or C1-6alkyl; to its salts or its solvates. The invention refers also to the regulator CCR5, to the agent of prevention and/or treatment of HIV infection, immunological or inflammatory diseases, to the pharmaceutical composition, to the medicinal preparation, to the method of disease treatment or prevention as well as to the application of compound as in claim 1.

Heterocyclic inhibitors of hh-sygnal cascade, based on them medicinal compositions and method of treating diseases induced by abbarant activity of hh-signal system / 2364597

Claimed invention relates to novel derivatives of 2,6-dihydro-7H- pyrazolo[3,4-d]pyradazin-7-one, 1,4-dihydropyrazolo[3,4-b]thiazin-5(6H)-one; N-acylated 4-imidazo[1,2-a]pyridin-2-yl- and 4-imidazo[1,2-a]pyrimidin-2-yl- anilines; amides of [(4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]pyperidin-4-carboxylic acid; amides of 2-(4-carbamoylpyperidin-1-yl)isonicotinic acid; amides of N-sulfonyl-1,2,3,4-tetrahydrochinolin-6-carboxylic acid; as well as to N-acylated 3-azolyl derivatives of 2-amino-4,5,6,7-tetrahydtithieno[2,3-c]pyridine possessing properties of Hh-signal cascade inhibitors.

Antiaggregatory and stress limiting agent / 2375071

Invention refers to chemical-pharmaceutical industry, namely to development of an antiaggregatory and stress-limiting agent as a reactant containing ecdysteroids-containing substance in the form of mixed 20-hydrohyecdysone in amount 75% and more, and 25S-inokosteron in amount 10% and more. The reactant is recovered from herb of Serratula sort of Asteraceae family, preferentially leaves collected during vegetation, mass budding or beginning of blossoming.

FIELD: medicine.

SUBSTANCE: there are presented compounds of formula I wherein W, R, R¹, R², R³, R⁴, R⁵, R⁶ and R⁷ have values specified in cl. 1 of the patent claim, and to method for making these compounds, a based medicinal agent used for treating conditions affected by inhibition, regulation and/or modulation of mitotic motor protein Eg5, to a mixture and application of said compounds for making the medicinal agent.

EFFECT: there are produced and described new compounds which can find application in treating tumours.

40 cl, 654 ex, 3 tbl, 25 dwg

The text descriptions are given in facsimile form.

1. The compounds of formula I

the which
W represents CH or N,
R¹, R², R³independently from each other, represent H, A, aryl, heteroaryl, Hal, -(CY₂)_n-SA, -(CY₂)_n-SCF₃, -(CY₂)_n-SCN, -(CY₂)_n-CF₃, -(CY₂)_n-F₃cycloalkyl, -S₃, -SCN, -CF₃, -F₃, -OA, -(CY₂)_n-OH, -(CY₂)_n-CO₂R, -(CY₂)_n-CN, -(CY₂)_n-Hal, -(CY₂)_n-NR₂, (CY₂)_n-OA, (CY₂)_n-OCOA, -SCF₃, (CY₂)_n-CONR₂, -(CY₂)_n-NHCOA, -(CY₂)_n-NHSO₂A, SF₅Si(CH₃)₃WITH-(SU₂)_n-CH₃, -(SU₂)_n-N-pyrrolidone, CH(CH₂)_nNRCOOR, CHNRCOOR, NCO, CH(CH₂)_nCOOR, NCOOR, CH(CH₂)_nOH, N(CH₂)_nOH, CHNH₂CH(CH₂)_nNR₂CH(CH₂)_nNR₂C(OH)R, CHNCOR, CH(CH₂)_n-aryl, CH(CH₂)_n-heteroaryl, CH(CH₂)_nR¹N(CH₂)_nCOOR, CH(CH₂)_nX(CH₂)_n-aryl, CH(CH₂)_nX(CH₂)_n-heteroaryl, N(CH₂)_nCONR₂, XCONR(CH₂)_nNR₂, N[(CH₂)_nXCOOR]CO(CH₂)_n-aryl, N[(CH₂)_nR] (CH₂)_n-aryl, N[(CH₂)_nXR]CO(CH₂)_nX-aryl, N[(CH₂)_nXR]SO₂(CH₂)_n-aryl, N[(CH₂)_n NRCOOR]CO(CH₂)_n-aryl, N[(CH₂)_nNR₂]CO(CH₂)_n-aryl, N[(CH₂)_nNR₂]CO(CH₂)_nNR-aryl, N[(CH₂)_nNR₂]SO₂(CH₂)_n-aryl, N[(CH₂)_nXR]CO(CH₂)_n-heteroaryl, N[(CH₂)_nXR]CO(CH₂)_nX-heteroaryl, N[(CH₂)_nXR]SO₂(CH₂)_n-heteroaryl, N[(CH₂)_nNRCOOR]CO(CH₂)_n-heteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_n-heteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_nNR-heteroaryl, N[(CH₂)_nNR₂]SO₂(CH₂)_n-heteroaryl, O(CH₂)_nNR₂X(CH₂)_nNR₂, NCO(CH₂)_nNR₂, R¹and R²together represent a-N-C(CF₃)=N-, -N CR=N-, -N-N-N-,
Y represents H, A, Hal,
And represents an alkyl or cycloalkyl, in which one or more H atoms may be replaced by Hal,
Hal represents F, Cl, Br or I,
R represents H or A, in the case genialnyh radicals R together also -(CH₂)₅-, -(CH₂)₄- or -(CH₂)₂-X-(CH₂)₂or -(CH₂)₂-Z-(CH₂)_n,
R⁴, R⁵independently from each other, represent H or unsubstituted or mono - or poly-OR-NO₂-, Hal-, CF₃-, F₃-, CN-, NR₂- or SR-, aryl - or hetaerae the aryl-substituted N-pyrrolidinyl radical, -X-(CH₂)₂OR, -X-(CH₂)_nCH₃, -X-(CH₂)₂NR₂, R¹, S-aryl, O-aryl, CH₂Si(CH₃)₃or together are-X - (CR₂)₂-, -S-(CR₂)₃-, -S-(SNSN₂OR)(CH₂)₂-, -X-(CHCH₂NR₂)(CH₂)₂-, -X - (CH₂)₂NR₂, -(CR₂)₃-, -(CR₂)₄-, -CR=CR-CR=CR-, -XCHQ(CR₂)₂-, -XCHQCR₂-R-N-(C=X)-N-R-XC[(CH₂)_nOR]₂CH₂CH₂-,
X represents O, S or NR,
Q represents CH₂l, Cho, COR^aCH₂R^aCH₂OCOR^aCH₂NCOR¹CH₂N(R¹)₂CH₂OR¹CH₂OCON(R¹)₂CH₂OCOOR¹CH₂NHCON(R¹)₂CH₂NHCOOR¹,
R^arepresents a

OR other₂, NR₂, NR(CH₂)_n-the reel, NR(CH₂)_nOR, COOR, N-pyrrolidinyl radical, OCOR, NR(CH₂)_nNR₂, N[(CH₂)_nNR₂]CO(CH₂)_n-aryl, N[(CH₂)_nNHCOOR]CO-aryl, R¹N[CH₂(CH₂)_nOR]₂, NR(CH₂)_nNCOOR, X(CH₂)_nX(CH₂)_nXR, NR(CH₂)_nX(CH₂)_nOH, NR(CH₂)_nO(CH₂)_nOH, (CH₂)_nCOOR, O(CO)NR(CH₂)_nOR, O(CO)(CH₂)_nNR₂, NR(CH₂)_nNR₂, N[(CH₂)_nNR₂]CO(CH₂)_n-aryl, N[(CH₂)_nXR]CO(CH₂)_n-aryl, N[(CH₂)_nR] (CH₂)_n-heteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_n-heteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_nR¹N(R)(CH₂)_nN(R)COOR, XCOO(CH₂)_nNR₂, OSO₂A, OSO₂CF₃, OSO₂Ar, OCONR₂, OCH₂(CH₂)_nNR₂,
Z represents CH₂X, CHCONH₂CH(CH₂)_nNRCOOR, CHNRCOOR, NCO, CH(CH₂)_nCOOR, NCOOR, CH(CH₂)_nOH, N(CH₂)_nOH, CHNH₂CH(CH₂)_nNR₂CH(CH₂)_nNR₂C(OH)R, CHNCOR, CH(CH₂)_n-aryl, CH(CH₂)_n-heteroaryl, CH(CH₂)_nR¹N(CH₂)_nCOOR, CH(CH₂)_nX(CH₂)_n-aryl, CH(CH₂)_nX(CH₂)_n-heteroaryl, N(CH₂)_nCONR ₂, XCONR(CH₂)_nNR₂, N[(CH₂)_nR] (CH₂)_n-aryl, N[(CH₂)_nR] (CH₂)_n-aryl, N[(CH₂)_nR] (CH₂)_nX-aryl, N[(CH₂)_nXR]SO₂(CH₂)_n-aryl, N[(CH₂)_nNRCOOR]CO(CH₂)_n-aryl, N[(CH₂)_nNR₂]CO(CH₂)_n-aryl, N[(CH₂)_nNR₂]CO(CH₂)_nNR-aryl, N[(CH₂)_nNR₂]SO₂(CH₂)_n-aryl, N[(CH₂)_nXR]CO(CH₂)_n-heteroaryl, N[(CH₂)_nXR]CO(CH₂)_nX-heteroaryl, N[(CH₂)_nXR]SO₂(CH₂)_n-heteroaryl, N[(CH₂)_nNRCOOR]CO(CH₂)_n-heteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_n-heteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_nNR-heteroaryl, N[(CH₂)_nNR₂]SO₂(CH₂)_n-heteroaryl, O(CH₂)_nNR₂X(CH₂)_nNR₂, NCO(CH₂)_nNR₂,
R⁶represents aryl or heteroaryl, each of which is unsubstituted or mono - or polyamidine the aryl or heteroaryl, each of which can be substituted by the groups Hal, NO₂CN, A, OR, OCOR, COR, NR₂, CF₃, F₃, Och(CF₃)₂or groups Hal, NO₂, CN, OR, A, -(CY₂)_n-OR, -OCOR, -(CY₂)_n-CO₂R, -(CY₂)_{n/sub> -CN, -NCOR, -COR or -(CY₂)_n-NR₂,

R⁷represents (C=O)-R, (C=O)-NR₂(C=O)-OR, H or A,

m represents 0, 1 or 2 and

n represents 0, 1, 2, 3, 4, 5, 6 or 7, and their pharmaceutically acceptable derivative, solvate, tautomers, salts and stereoisomers, including mixtures thereof in all ratios, except

5-Phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

7-Chloro-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

9-Chloro-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

7-Methyl-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

5-Phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline-7-ol,

9-Methoxy-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

10-Chloro-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

9,10-Dichloro-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

8-Chloro-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

8,9-Dichloro-5-phenyl-3,4,4A,5,6,10b-hexahydro-2H-Piran[3,2-C]quinoline,

4-Phenyl-2,3,3A,4,5,9b-hexahydrofuro [3,2-C]quinoline,

8-Methoxy-4-phenyl-2,3,3A,4,5,9b-hexahydrofuro [3,2-C]quinoline,

6-Methyl-4-phenyl-2,3,3A,4,5,9b-hexahydrofuro [3,2-C]quinoline,

4-Phenyl-2,3,3A,4,5,9b-hexahydrofuro [3,2-C]quinoline-6-ol,

8-Chloro-4-phenyl-2,3,3A,4,5,9b-hexahydrofuro [3,2-C]quinoline,

8-Nitro-4-phenyl-2,3,3A,4,5,9b-hexahydrofuro [3,2-C]quinoline,

1-(2-Phenyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-it,

3,3-Dimethyl-2-phenyl-1,2,3,4-then it is carbonated is rhinolin,

4-Benzyloxy-3,3-dimethyl-2-phenyl-1,2,3,4-tetrahydroquinoline,

4-Methoxy-2-phenyl-1,2,3,4-tetrahydroquinoline,

2-(4-Forfinal)-4-methoxy-1,2,3,4-tetrahydroquinoline,

2-Furan-2-yl-4-methoxy-1,2,3,4-tetrahydroquinoline,

1-(3-Pentyl-2-p-tolyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-it,

and

1-(1-Methyl-2-phenyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-it.}

2. Compounds according to claim 1, in which
R¹represents A, CF₃, F₃, SA, SCN, CH₂CN, -OOA, Hal, SCF₃, tert-butyl, -CH(CH₃)CH₂CH₃, isopropyl, ethyl or methyl.

3. Compounds according to claim 1, in which
R²represents F or N.

4. Compounds according to claim 1, in which R³represents F or N.

5. Compounds according to claim 1, in which
R⁴preferably represents one of the following groups, if R⁵is a N:
or
X and R take values specified in claim 1.

6. Compounds according to claim 1, in which R⁵represents N.

7. Compounds according to claim 1, in which
R⁵together with R⁴takes one of the following values:
,,,,or,
in which
X, R and R^atake the values specified is paragraph 1.

8. Compounds according to claim 1, in which
R⁶represents phenyl, 2-, 3 - or 4-pyridyl, pyrimidyl, furyl or thienyl, each of which is unsubstituted or mono - or polyamidine groups Hal, CN, NO₂HE, CF₃, Och(CF₃)₂OSON₃or A.

9. Compounds according to claim 1, in which
R⁶represents one of the following groups:
,,,,,
,,,,,,
,,,,,
,,,,
,,,,.

10. Compounds according to claim 1, in which R⁷represents N.

11. Compounds according to claim 1 sub-formulae IA-ID:

in which
R, R¹ , R², R³, R⁴, R⁵, R⁶, R⁷and X take the values specified in paragraph 1
and
R⁸represents N, CH₂Or, or CH₂NR₂.

12. Compounds according to claim 1 sub-formulas a and b:

in which R¹, R², R³, R⁴, R⁵, R⁶, R⁷take the values specified in claim 1, and their racemate or other mixtures of enantiomers.

13. Compounds of the sub-formulae I1-A:

14. Method of producing compounds of the formula I according to claims 1 to 13, and their pharmaceutically acceptable derivatives, salts, solvate, tautomers and stereoisomers, wherein the compound of formula II

in which
R¹, R²and R³take the values specified in claim 1, is introduced into reaction with the compound of the formula III

in which
R⁶takes the values specified in claim 1,
and
with the compound of the formula IV, its isomer with a double bond (E isomer) or mixtures thereof

in which
R⁴and R⁵take the values specified in claim 1,
and, if necessary, the radical R⁷that represents N, turn in the radical R⁷that takes a value different from N, and/or, if necessary,
the base or acid of the formula I is converted into one of its salts.

15. The method according to 14, characterized in that the reaction is performed in the presence of a proton acid or a Lewis acid.

16. The method according to 14, characterized in that the reaction is performed in the presence of triperoxonane acid, hexafluoroisopropanol, bismuth (III) chloride, ytterbium (III) triflate, scandium (III) triflate or cerium (IV) ammonium nitrate.

17. Medicines, art is meant to treat diseases, which may affect the inhibition, regulation and/or modulation of the mitotic motor protein Eg5, comprising at least one compound of formula I according to claims 1 to 13 and/or its pharmaceutically acceptable derivative, salt, solvate, tautomers and stereoisomers, including mixtures thereof in all ratios, and optionally excipients and/or auxiliary substances.

18. A mixture containing one or more compounds of formula I and a certain amount of one or more compounds of the formula V, analogues and/or their metabolites

in which
Y' and Z' each, independently of one another represents O or N, R⁹and R¹⁰each, independently of one another, represent H, HE, halogen, OC_1-10-alkyl, F₃, NO₂or NH₂n is an integer between 2 and 6 inclusive, and R⁸and R¹¹each, independently of one another, is meta - or para-position and is selected from the group:

and

19. The mixture p, which used the compound of formula V is a pentamidine or its salts.

20. The use of compounds according to claims 1 to 13, and their pharmaceutically acceptable derivatives, sole is, the solvate, tautomers and stereoisomers, including mixtures thereof in all ratios, or a mixture p, for preparing a medicinal product for the treatment of diseases which can be influenced by the inhibition, regulation and/or modulation of the mitotic motor protein Eg5.

21. The use of compounds according to claims 1 to 13 or a mixture p, for preparing a medicinal product for the treatment and prevention of neoplastic diseases.

22. Use item 21, in which neoplastic disease associated with a tumor from the group of tumours of the squamous epithelium, the bladder, stomach, kidney, head and neck, esophagus, cervix, thyroid, intestine, liver, brain, prostate, urogenital tract, lymphatic system, stomach, larynx and/or lung.

23. The application of article 22, in which the tumor is selected from the group which includes monocytic leukaemia, lung adenocarcinoma, small cell lung carcinoma, pancreatic cancer, glioblastomas and carcinoma of the breast and carcinoma of the intestine.

24. Use item 21, in which tumour disease that must be treated is a tumor of the blood and immune system.

25. The application of paragraph 24, in which the tumour originates from the group, which includes acute melodicheskoe leukemia, chronic melodicheskoe leukemia, acute lymphatic leukaemia and/or XP is technical lymphatic leukemia.

26. The use of compounds according to claims 1 to 13 and/or their physiologically acceptable salts and solvate for the preparation of drugs for the treatment of tumors in combination with a therapeutically effective amount of one or more compounds of the formula V, analogues and/or their metabolites

in which
Y' and Z' each, independently of one another represents O or N, R⁹and R¹⁰each, independently of one another, represent H, HE, halogen, OS_1-10alkyl, F₃, NO₂or NH₂n is an integer between 2 and 6 inclusive, and R⁸and R¹¹each is, independently from each other, preferably in meta - or para-position and is selected from the group:

and

where
the compounds of formula I and the compounds of formula V, analogues and/or their metabolites are administered simultaneously or within 14 days of one another in amounts which are sufficient to inhibit the growth of cancer or other hyperproliferative cells.

27. Use p, where the connection of the formula V represents pentamidine or its salts.

28. The use of compounds of the formula I according to the claim 1 to 13 and/or their physiologically acceptable derivatives, salts and solvate for the preparation of drugs for the treatment of tumours, where a therapeutically effective amount of the compounds of formula I are used in combination with radiotherapy and a compound from the group which includes: 1) an estrogen receptor modulator, 2) modulator androgenous receptor, 3) modulator retinoid receptor, 4) cytotoxic agent, 5) antiproliferative agent, 6) inhibitor phenyl-protein transferase, 7) an inhibitor of HMG-CoA reductase inhibitor, 8) an inhibitor of HIV protease, 9) reverse transcriptase inhibitor and 10) other inhibitors of angiogenesis.

29. The compounds of formula I,

in which Q represents CH₂R^aand R^atakes one of the following values: other₂, NR₂, NR(CH₂)_naryl, NR(CH₂)_nOR, COOR, N-pyrrolidinyl radical, OCOR, NR(CH₂)_nNR₂, N[(CH₂)_nNR₂]CO(CH₂)_naryl, N[(CH₂)_nNHCOOR]Soarin, R¹N[CH₂(CH₂)_nOR]₂, NR(CH₂)_nNCOOR, X(CH₂)_nX(CH₂)_nXR, NR(CH₂)_nX(CH₂)_nOH, NR(CH₂)_nO(CH₂)_nOH, (CH₂)_nCOOR, O(CO)NR(CH₂)_nOR, O(CO)(CH₂)_nNR₂, NR(CH₂)_nNR₂, N[(CH₂)_nNR₂]CO(CH₂)_naryl, N[(CH₂)_nXR]CO(CH₂)_nthe reel, N[(CH₂)_nR] (CH₂)_nheteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_nheteroaryl, N[(CH₂)_nNR₂]CO(CH₂)_nR¹N(R)(CH₂)_nN(R)COOR, XCOO(CH₂)_nNR₂, OSO₂A, OSO₂CF₃, OSO₂Ar, OCONR₂or OCH₂(CH₂)_nNR.

30. The compound of the formula

and its pharmaceutically acceptable derivative, solvate, tautomers, salts and stereoisomers, including mixtures thereof in any ratio.