Patent RU-2362773-C2 (RU)
Title: Quinazoline derivatives for slowing down growth of cancer cells and method of obtaining them
Inventor: KHAM JANG DZIN
IPC: C07D401/14
Filed: 2005-12-20
Granted: 2009-07-27
Abstract: 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)   R 1  represents hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 alkoxy, C 1-6 alkylamino, C 1-6 dialkylamino, C 1-6 alkyltio, 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; R 2  represents hydrogen or C 1-6 alkyl; R 3  represents C 1-6 alkyl or C 1-6 dialkylamino C 1-6 alkyl; Y represents -(CR 11 R 12 )-, phenyl or 5-member heteroaryl, containing one sulphur atom, R 11  and R 12 , each independently represent hydrogen, halogen, hydroxy, carboxyC 1-3 alkyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkyltio, C 1-6 alkylsulphinyl, C 1-6 alkylsulphonyl, C 1-6 alkanoyl, C 1-6 alkoxycarbonyl, phenyl; optionally are condensed with each other with formation of 3-member non-aromatic ring, or R 11  or R 12  can be condensed with R 2  with formation together with carbon and nitrogen, to which they are bonded, of 4-6-member non-aromatic ring, optionally containing additional sulphur heteroatom; R 4  represents hydrogen, halogen, C 1-6 alkoxy, ethylsulphanyl, cyclopropylmethoxy, cyclopentyloxy, or C 1-6 alkylamino, optionally substituted with R 13 , where R 13  represents halogen, trifuoromethyl, C 1-6 alkoxy, 4-methylpiperidinylmethoxy, N,N-dimethylamino or 6-member heteroaryl, containing 1-2 heteroatoms selected from N and O; R 5  represents hydrohen or C 1-3 alkyl; R 6  represents R 14 , 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 R 15 , where R 14  and R 15 , each independently represent hydrogen, halogen, C 1-6 alkyl, or phenyl, benzyl, 10-member heteroarylC 1-6 alkyl, containing one nitrogen atom, benzyloxy, 6-member heteroarylC 1-6 alkoxy, containing one nitrogen atom, 6-member heteroaryloxy, containing one nitrogen atom, phenylcarbamoyl, optionally substituted with R 16 , where R 16  represents halogen, nitro, C 1-6 alkyl, or C 1-6 alkoxy; n equals integer number within the range from 1 to 4; p equals 0 or 1; X represents halogen, nitro, cyano, trifluoromethyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 dialkylamino, C 1-6 alkylsulphinyl, C 1-6 alkylsulphonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkanoyl, 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