QUINAZOLINONES INHIBITING FARNESYLTRANSFERASE ACTIVITY Russian patent published in 2003 - IPC

FIELD: organic chemistry, biochemistry. SUBSTANCE: invention proposes derivatives of quinazolinone of the general formula (I) and their pharmaceutically acceptable acid-additive salts and stereochemical isomeric forms where dotted line is optionally linkage; X is oxygen atom; R¹ and R² each means independently hydrogen or halogen atom; R³ and R⁴ each means independently hydrogen or halogen atom; R⁵ means hydrogen, halogen atom or radical of the formula -O-R¹⁰ (a-1) or N-R¹¹R¹² (a-3) where R¹⁰, R¹¹, R¹² are hydrogen atom; R⁶ means radical of the formula (b-1) or (b-2) where R¹⁶ is hydrogen atom or phenyl; R¹⁷ is hydrogen atom or C_1-6-alkyl; R⁷ is hydrogen atom or C_1-6-alkyl under condition that dotted line is not a linkage; R⁸ is hydrogen atom, C_1-6-alkyl or Het¹CH₂; R⁹ is hydrogen atom; is pyridinyl. Compounds of the general formula (I) show inhibitory effect on farnesyltransferase activity and can be used for preparing medicinal agents inhibiting proliferative diseases. Invention relates also to pharmaceutical composition based on compounds of the general formula (I) eliciting inhibitory effect on farnesyltransferase activity, to method for preparing this composition, to intermediate derivatives of quinazolinone of the general formula (IX) and their acid-additive salts or stereochemical isomeric forms where n = 2 or 3 and R¹, R², R³, R⁴, R⁹, mean values indicated above, to method for preparing some compounds of the general formula (I) where R⁶ is radical of the formula (b-2) and to method for preparing intermediate derivatives of quinazolinone of the general formula (IX) and their acid-additive salts or stereochemical isomeric forms. EFFECT: improved preparing method of compounds and composition, valuable medicinal and biochemical properties. 10 cl, 4 tbl, 15 ex