NOVEL PYRROLIDINE-3, 4-DICARBOXAMIDE DRIVATIVES Russian patent published in 2010 - IPC C07D207/16 C07D401/12 C07D401/14 C07D403/12 C07D409/14 C07D417/12 A61K31/541 A61P7/02 

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrrolidine-3,4-dicarboxamide derivatives of formula (I): , where: X is N or C-R⁶; R¹ is C_1-7alkyl, C_3-10cycloalkyl, C_3-10cycloalkyl-C_1-7alkyl, fluoro-C_1-7alkyl, hydroxy-C_1-7alkyl, CN-C_1-7alkyl, R¹⁰C(O), R¹⁰OC(O)-, N(R¹¹,R¹²)C(O)-; R¹⁰OC(O)C_1-7alkyl, N(R¹¹,R¹²)C(O)-C_1-7alkyl, R¹⁰SO₂, R¹⁰-SO₂-C_1-7alkyl, N(R¹¹, R¹²)-SO₂, N(R¹¹,R¹²)-SO₂-C_1-7alkyl, aryl-C_1-7alkyl, 5-member monocyclic heteroaryl containing a nitrogen atom, where the ring carbon atom can be substituted with a carbonyl group, heteroaryl-C1-7alkyl, where the term "heteroaryl" represents an aromatic -member monocyclic ring with 1 S atom or a 6-member monocyclic ring with 1 N atom, C_1-7alkoxy-C_1-7alkyl, C_1-7alkoxycarbonyl-C_3-10cycloalkyl-C_1-7alkyl or halogen substituted 4-member heterocyclyl-C_1-7alkyl with one O atom; R² is H, C_1-7alkyl; R³ is aryl, aryl-C_1-7alkyl, heteroaryl, heteroaryl-C_1-7alkyl, where the term "heteroaryl" represents a 5-member monocyclic ring with 1 S atom, a 6-member monocyclic ring with 1 or 2 N atoms, 9-, 10-member bicyclic system with 1 or 2 N atoms in one ring; R⁴ is H, C_1-7alkyl, OH; R⁵, R⁶, R⁷, R⁸ are independently selected from a group consisting of H, halogen, C_1-7alkyl, C_1-7alkoxy, flouro-C_1-7alkyl, fluoro-C_1-7alkyloxy; R⁹ is aryl, heterocyclyl, heteroaryl, heterocyclyl-C(O)-; R¹⁰ is H, C_1-7alkyl, C_3-10cycloalkyl, C_3-10cycloalkyl-C_1-7alkyl, fluro-C_1-7alkyl, heteroaryl, heteroaryl-C_1-7alkyl, where the term "heteroaryl" represents a 5-member monocyclic ring with 4 N atoms, a 5-member heterocyclyl with 1 N atom; R¹¹, R¹² are independently selected from a group consisting of H, C_1-7alkyl, C_3-10cycloalkyl, C_3-10cycloalkyl-C_1-7 alkyl; and pharmaceutically acceptable salts thereof; where the term "aryl" represents a phenyl group which can be optionally substituted with 1 to 5 substitutes which are independently selected from a group consisting of the following: halogen, CF₃, NH₂, C_1-7alkylsulphonyl, C_1-7alkoxy, fluoro-C_1-7alkyl, fluoro-C_1-7 alkoxy; the term "heterocyclyl" represents a nonaromatic monocyclic 5-, 6-member heterocyclic group with 1, 2 N atoms, or with 1 N atom and 1 O atom, where the heterocyclyl group can be substituted as indicated with respect to the term "aryl", and one carbon atom of the ring system of the heterocyclyl group can be substituted with a carbonyl group; the term "heteraryl" represents an aromatic 5- or 6-member monocyclic ring system which can have 1, 2, 3 N atoms, or 1 N atom and 1 S atom, where the heteroaryl group can be substituted as indicated with respect to the term "aryl", and one carbon atom of the ring system of the heteroaryl group can be substituted with a carbonyl group. Formula I compounds have inhibitory activity towards coagulation factor Xa.

EFFECT: possibility of using said compounds in a pharmaceutical composition and for preparing a medicinal agent.

27 cl, 90 ex