NOVEL VINYLOGENIC ACID DERIVATIVES Russian patent published in 2011 - IPC C07D403/06 C07D405/06 C07D209/14 C07D401/06 C07D487/08 C07D419/14 A61K31/4045 A61K31/4439 A61K31/4178 A61P37/00 A61P11/06 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I)

, where A denotes -CH₂-, -O- or -NR'-, in which R' denotes hydrogen or C₁-₆alkyl, or R' and R⁴ form C₂-₅alkylene; R¹ denotes hydrogen, amine group, C₁-₆alkyl, hydroxy group, -NR'R", (C₀-₆alkylene)-NR'R", where R' and R" are independently selected from a group comprising hydrogen, C₁-₆alkyl, heteroalkyl, formyl, C_1-6alkylcarbonyl, arylcarbonyl optionally substituted with halogenalkyl, C_1-6alkylsulphonyl, arylsulphonyl or -(C_0-6alkylene)-OR', where R' denotes hydrogen, C_1-6alkyl, formyl or C_1-6alkylcarbonyl; R² , R² and R² independently denote hydrogen, halogen, C_1-6alkyl or C_1-6alkoxy group; R³ denotes hydrogen, C_1-6alkyl, aryl-C_1-6alkyl, aryl optionally substituted with halogen, or heteroaryl, where the heteroaryl is a monocyclic or bicyclic ring containing 5-6 ring atoms and at least one aromatic ring containing one or three ring heteroatoms selected fron N, O and S, where the remaining ring atoms are carbon atoms, and the bonding site of the heteroaryl radical must be on the aromatic ring; R⁴ denotes hydrogen, C_1-6alkyl, aryl, C_3-7cycloalkyl-C_1-6alkyl, aryl-C_1-6alkyl; R⁵ denotes hydrogen or C_1-6alkyl; or R⁴ and R⁵ together with the carbon atom to which they are bonded, form an optionally substituted C_3-7cycloalkyl ring; R⁶ denotes hydrogen or C_1-6alkyl; and pharmaceutically acceptable salts thereof, where the term "aryl" denotes phenyl or naphthyl. The invention also relates to a pharmaceutical composition based on compounds of formula I and having a inhibitory activity towards chymase.

EFFECT: novel compounds which can inhibit chymase are obtained and can be used as medicinal agents.

22 cl, 79 ex, 1 tbl