DERIVATIVES OF 4-(SUBSTITUTED PHENYLAMINO)-QUINAZOLINE OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHOD OF INHIBITION OF RECEPTOR TYROSINE KINASE AND PHARMACEUTICAL COMPOSITION Russian patent published in 2001 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention proposes derivatives of 4-(substituted phenylamino)- -quinazoline of the formula (I) where m = 1 or 2; n = 1 or 2; each R¹ is taken independently among the group including halogen atom, cyano-group, hydroxy-group, R⁵, nitro-group, amino-group, trifluoromethyl, C(= O)O R⁵, R⁵O optionally substituted with halogen atom, hydroxy-group, (1-4)C-alkoxygroup, acetoxy-group, (1-4)C-alkylpiperazinyl, morpholinyl, imidazolyl, 4-oxopyridyl or S(1-3)C-alkyl optionally substituted with carboxy-group, SO₂R⁵, SR⁵ optionally substituted with cyano-group, (1-4)C-alkyl, S(1-4)C-alkyl or 4-cyanophenyl group, toluenesulfonylamino-group, NHSO₂R⁵, benzylsulfanyl or phenylsulfanyl optionally substituted with 1-2 halogen atoms, phenoxy-group optionally substituted with 1-2 substitutes taken among halogen atom, (1-4)C-alkyl, (1-4)C-alkoxy-group, methanesulfonyl, methanesulfanyl and halogenphenylsulfanyl, allylsulfanyl, vinylhydroxy-group, guanidino-group and phthalimido-(1-4)C-alkylsulfonylamino-group; or two fragments R¹ taken in common in positions 6 and 7 of quinazoline form methylenedioxy-group and where alkyl groups and alkyl fragments of indicated alkoxy-groups can be a direct chain and can be a branched chain if they consist of at least three carbon atoms; R² means hydrogen atom; each R³ group is taken independently among hydrogen atom, halogen atom and (1-4)C-alkyl; R⁴ means azido-group or (2-4)C-alkynyl where indicated alkynyl is optionally substituted with hydroxy-group, amino- group or aminomethyl group; R⁵ means (1-4)C-alkyl, or their pharmaceutically acceptable salts. Indicated compounds inhibit activity of receptor tyrosine kinase and can be used in treatment of patients with hyperproliferative diseases, for example, malignant tumors in mammals. Also, invention proposes method of inhibition of activity of receptor tyrosine kinase and pharmaceutical composition eliciting antiproliferative activity. EFFECT: improved method of inhibition of tyrosine kinase activity, valuable pharmacological and medicinal properties of compounds. 10 cl, 2 tbl, 105 ex