DERIVATIVES OF QUINAZOLINE, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION COMPRISING THEREOF AND METHOD OF ACHIEVEMENT OF ANTI-ANGIOGENIC EFFECT AND/OR EFFECT OF DECREASE OF VASCULAR PENETRATION WITH THEIR USING Russian patent published in 2002 - IPC

Abstract RU 2194701 C2

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to derivatives of quinazoline of the formula (I) where Y1 means O-, -S-, -NR5-CO where R5 means hydrogen atom; R1 means hydrogen atom or C1-3- alkoxy-group; R2 means hydrogen atom; m means a whole number from 1 to 5; R3 means hydroxy- group, halogen atom, C1-3-alkyl, C1-3-alkoxy-group, C1-3-alkanoylhydroxy-group or cyano-group; R4 means one of five groups that is optionally substituted pyridone, phenyl or aromatic heterocyclic group with 1-3 heteroatoms taken among O, N and S or it comprises such group and their salts. Invention relates also to methods of their synthesis and pharmaceutical compositions containing compound of the formula (I) or its pharmaceutically acceptable salt as active component. Compounds of the formula (I) and their pharmaceutically acceptable salts inhibit effects of VEGF that is useful for treatment of many diseases including cancer and rheumatic arthritis. Invention relates also to method of achievement of anti-angiogenic effect and/or effect of decrease of vascular penetration in warm- blooded animal involving administration to indicated animal the effective amount of compound of the formula (I) or its pharmaceutically acceptable salt. EFFECT: improved method of synthesis, valuable medicinal properties of compounds. 19 cl

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RU 2 194 701 C2

Authors

Lomann Zhan-Zhak Marsel'

Ehnneken Loran Fransua Andre

Tomas Ehndrju Piter

Dates

2002-12-20Published

1996-12-13Filed