QUINAZOLINE DERIVATIVES FOR SLOWING DOWN GROWTH OF CANCER CELLS AND METHOD OF OBTAINING THEM Russian patent published in 2009 - IPC C07D239/94 C07D401/12 C07D401/14 A61K31/517 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to quinazolene derivatives of formula (I) and pharmaceutically acceptable salts of salt for slowing down cancer cells growth, as well as to method of obtaining compound and pharmaceutical composition based on them. Compounds can be applied for treatment of cancer diseases in which growth of cancer cells is induced by epithelial growth factor. In general formula (I) R¹ represents hydrogen, C_1-6alkyl, C_3-7cycloalkyl, C_2-6alkenyl, C_2-6alkynyl, C_1-6alkoxy, C_1-6alkylamino, C_1-6dialkylamino, C_1-6alkyltio, 2-((Nmethyl-(2-hydroxyethyl)amino)mathyl)vinyl, phenoxy, phenyl, dimethylaminoethoxymethyl, methoxyethoxymethyl, 4-methylpiperazinylmethyl, ethoxycarbonyl, benzamino, cyclopentenyl, 2-(4-methylpiperazinylmethyl)vinyl, methanesulphonylethylaminomethyl, methoxyethylaminomethyl, 2-(methanesulphonylethylaminomethyl)vinyl or 5-member heteroaryl, containing 1-2 heteroatoms selected from N, O or S, which are optionally substituted with X; R² represents hydrogen or C_1-6alkyl; R³ represents C_1-6alkyl or C_1-6dialkylamino C_1-6alkyl; Y represents -(CR¹¹R¹²)-, phenyl or 5-member heteroaryl, containing one sulphur atom, R¹¹ and R¹², each independently represent hydrogen, halogen, hydroxy, carboxyC_1-3alkyl, C_1-6alkyl, C_1-6alkoxy, C_1-6alkyltio, C_1-6alkylsulphinyl, C_1-6alkylsulphonyl, C_1-6alkanoyl, C_1-6alkoxycarbonyl, phenyl; optionally are condensed with each other with formation of 3-member non-aromatic ring, or R¹¹ or R¹² can be condensed with R² with formation together with carbon and nitrogen, to which they are bonded, of 4-6-member non-aromatic ring, optionally containing additional sulphur heteroatom; R⁴ represents hydrogen, halogen, C_1-6alkoxy, ethylsulphanyl, cyclopropylmethoxy, cyclopentyloxy, or C_1-6alkylamino, optionally substituted with R¹³, where R¹³ represents halogen, trifuoromethyl, C_1-6alkoxy, 4-methylpiperidinylmethoxy, N,N-dimethylamino or 6-member heteroaryl, containing 1-2 heteroatoms selected from N and O; R⁵ represents hydrohen or C_1-3alkyl; R⁶ represents R¹⁴, phenyl, 1-phenylethyl, 3-ethenylphenyl, 1-penta-2,4-dienyl-1N-indasol-5-yl, imidasol or 9-member heteroaryl, containing 1-2 nitrogen atoms, optionally substituted with substituent R¹⁵, where R¹⁴ and R¹⁵, each independently represent hydrogen, halogen, C_1-6alkyl, or phenyl, benzyl, 10-member heteroarylC_1-6alkyl, containing one nitrogen atom, benzyloxy, 6-member heteroarylC_1-6alkoxy, containing one nitrogen atom, 6-member heteroaryloxy, containing one nitrogen atom, phenylcarbamoyl, optionally substituted with R¹⁶, where R¹⁶ represents halogen, nitro, C_1-6alkyl, or C_1-6alkoxy; n equals integer number within the range from 1 to 4; p equals 0 or 1; X represents halogen, nitro, cyano, trifluoromethyl, C_1-6alkyl, C_1-6alkoxy, C_1-6dialkylamino, C_1-6alkylsulphinyl, C_1-6alkylsulphonyl, C_1-6alkyloxycarbonyl, C_1-6alkanoyl, phenyl or 5-6-member heteroaryl, containing 1-2 heteroatoms selected from N and O; where heteroaryl represents heteroaromatic or non-aromatic group.

EFFECT: obtaining quinazoline derivatives and pharmaceutically acceptable salts of salts for slowing down growth of cancer cells.

11 cl, 7 dwg, 5 tbl, 225 ex