QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS OF VESSEL ENDOTHELIUM GROWTH FACTOR Russian patent published in 2003 - IPC

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of quinazoline of the formula (I) where Z means -O-, -NH- or S-; m is a whole number from 1 to 5 under condition that when Z means -NH- then m is a whole number from 3 to 5; R¹ means hydrogen atom, C_1-3-alkoxy- group; R² means hydrogen atom; R³ means hydroxy-group, halogen atom, C_1-3-alkyl, C_1-3-alkoxy-, C_1-3-alkanoylhydroxy-, trifluoromethyl- or cyano-group; X¹ means -O-, -NR⁷, -NR⁸CO- where each of R⁷, R⁸ means hydrogen atom, C_1-3-alkyl; R⁴ is taken among one of seven groups enumerated in claim 1 of the invention claim excepting for 4-(3,4,5-trimethoxyphenoxy)-6,7-dimethoxyquinazoline, 4-(3- methoxyphenylthio)-6,7-dimethoxyquinazoline, 4-(3-chlorophenyl-thio)-6,7-dimethoxyquinazoline, 4- (3-chlorophenoxy)-6,7-dimethoxy- -quinazoline and 4-(3,4,5-trimethoxyanilino)-6,7- dimethoxyquinazoline or their salts. Invention proposes also 5 methods of synthesis of the above described compounds. Compounds of the formula (I) exhibit antiangiogenic and/or reducing effect on vessels permeability in warm-blooded animals and they are designated for using as drugs with indicated effect. Invention relates also to pharmaceutical composition comprising the above described compounds and method of inhibition of angiogenesis and/or reducing vessel permeability in warm-blooded animals needing such treatment. EFFECT: valuable medicinal properties of compounds. 21 cl, 1 tbl, 37 ex