CYCLIC AMINE DERIVATIVE CONTAINING SUBSTITUTED ALKYL GROUP Russian patent published in 2010 - IPC C07D211/72 C07D401/06 A61K31/445 A61K31/454 A61K31/4545 A61K31/496 A61K31/5377 A61K31/541 A61P7/02 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds having general formula (I) given below, , where R¹ represents a hydrogen atom, C1-C6 alkyl group, C3-C6 cycloalkyl group or C1-C6 alkoxy group; R² is a hydrogen atom or C1-C6 alkyl group; R³ is a substituted C1-C6 alkyl group {said substitute is a heterocyclyl group or heterocyclyl group substituted with 1-5 substitutes selected from <a group of substitutes α> (said heterocyclyl groups can be substituted with 1-4 oxo groups); a heteroaryl group or a heteroaryl group substituted with 1-5 substitutes selected from <a group of substitutes α>; or a substitute selected from <a group of substitutes β>}, or a heterocyclyl group or a heterocyclyl group substituted with 1-5 substitutes selected from <a group of substitutes α> (said heterocyclyl groups can be substituted with 1-4 oxo groups); where the heteroaryl group is a 5- or 6-member aromatic heterocyclic group containing at least one nitrogen atom, and the heterocyclyl group is a partially or completely reduced 5- or 6-member heterocyclic group containing 1-3 sulphur atoms, oxygen atoms and/or nitrogen atoms; X¹, X², X³, X⁴ and X⁵ each independently represents a hydrogen atom or a halogen atom; n equals 1, < group of substitutes α> is a carboxy group, C2-C7 alkoxycarbonyl group, carbamoyl group, hydroxyl group, C1-C6 alkyl group, C2-C7 alkanoyl group, C2-C7 alkylcarbamoyl group, di(C1-C6 alkyl)carbamoyl group or a group of formula R⁴-CO-CR⁵R⁶-(CH₂)_m-, where R⁴ represents a hydroxyl group or a C1-C6 alkoxy group; R⁵ and R⁶ are identical or different and each represents a hydrogen atom or a C1-C6 alkyl group; and m equals an integer ranging from 0 to 5; and <group of substitutes β> is represents a carboxy group, C2-C7alkoxycarbonyl group, carbamoyl group, cyano group, hydroxyl group, C1-C6 alkoxy group, C2-C7 alkylcarbamoyl group, di(C1-C6 alkyl)carbamoyl group and a group of formula R⁹-CO-(CH₂)_k-N(R¹⁰)- {where R⁹ represents a hydroxyl group or C1-C6 alkoxy group; R¹⁰ represents a hydrogen atom or C1-C6 alkyl group; and k equals an integer from 0 to 5}, to pharmacologically acceptable salts thereof and to C1-C6 alkanoyl derivatives. The invention also relates to a pharmaceutical composition, to use as well as to a method of preventing or therapy for diseases related to thrombosis or embolus formation.

EFFECT: obtaining novel biologically active compounds having inhibitory activity towards thrombocyte aggregation.

24 cl, 118 ex, 8 tbl