BICYCLIC PYRROLE DERIVATIVES Russian patent published in 2010 - IPC C07D487/04 C07D401/04 A61K31/519 A61K31/5377 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula : in which R¹ represents a hydrogen atom or alkyl optionally substituted with (1) aralkyloxy group, (2) aroyl, (3) isoquinolinyl or (4) aryl, optionally substituted with an alkoxy group; the solid line and the dashed line between A¹ and A² represent a double bond (A¹=A²) or a single bond (A¹-A²); A¹ is a group of formula C(R⁴), and A² is a nitrogen atom when the solid line and the dashed line between A¹ and A² represents a double bond (A¹=A²); A¹ is a group of formula C=O, and A² is a group of formula N(R⁵) when the solid line or the dashed line between A¹ and A² represent a single bond (A¹-A²); R² represents alkyl optionally substituted with a cyano group, aryl optionally substituted with an alkoxy group, aralkyl optionally substituted with a halogen atom, a cyano group, an alkoxy group, an alkyl or carbamoyl or alkynyl; R³ represents a hydrogen atom, a halogen atom, cyano, formyl, carboxyl, alkyl optionally substituted with (1) amino group optionally substituted with alkyl, or (2) alkoxy group, aryl optionally substituted with an alkoxy group, tetrazolyl, alkylcarbonyl, cycloalkylcarbonyl, heteroarylcarbonyl, where heteroaryl is a 4-6-member monocyclic radical containing 1-2 heteroatoms selected from a nitrogen atom or oxygen atom, alkoxycarbonyl, carbamoyl optionally substituted with alkyl, cycloalkyl or cycloalkylalkyl, hydroxyl, alkoxy group or a group of formula: -Rd-C(O)O-Re, where Rd represents a single bond, and Re represents a group of formula: -CH(R^4a)OC(O)R^4b, where R^4a represents alkyl or R^4b represents cycloalkyloxy or aryloxy; R represents a hydrogen atom, hydroxyl, cyano, alkyl, carbamoyl, carboxyl, aryloxy optionally substituted with an alkoxy group or carbamoyl, alkylsulfonyl, alkylcarbonyl or alkoxycarbonyl; R⁵ represents a hydrogen atom or alkyl; -Y represents a group of formula (A) given below: in which m1 equals 2, and R⁶ is absent, or to pharmaceutically acceptable salts of the said compounds. The invention also relates to compounds of formula (VI), to pharmaceutical compositions, to a dipeptidyl peptidase IV inhibitor, as well as to use of the said compounds.

EFFECT: obtaining novel biologically active compounds with dipeptidyl peptidase IV inhibition properties.

20 cl, 76 ex, 1 tbl