TETRAHYDROIMIDAZO[1,5-a]PYRAZINE DERIVATIVES, METHOD FOR PREPARING AND USING THEM IN MEDICINE Russian patent published in 2013 - IPC C07D487/04 A61K31/4985 A61K31/5377 A61P3/04 A61P3/10 A61P5/48 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to tetrahydroimidazo[1,5-a]pyrazine derivatives of formula I or to their pharmaceutically acceptable salts (I), wherein: Ar represents phenyl, wherein phenyl is additionally substituted by 1-3 substitutes independently specified in halogen; R¹ represents trifluoromethyl; R² is specified in a group consisting of hydrohyl, alkyl having 1 to 4 carbon atoms, alkoxyl having having 1 to 4 carbon atoms, cycloalkyl representing a 5-6-member monocyclic ring group consisting of carbon completely, and -NR⁴R⁵, wherein each alkoxyl is optionally substituted by one group specified in a group consisting of phenyl and -OC(O)OR⁸; R³ is specified in a group consisting of a hydrogen atom and alkyl having 1 to 4 carbon atoms; each of R⁴ and R⁵ is independently specified is a group consisting of a hydrogen atom, alkyl having 1 to 4 carbon atoms, cycloalkyl representing a 3-8-member monocyclic ring group consisting of carbon completely, phenyl and pyridinyl, wherein each alkyl or phenyl is optionally substituted by one or more group specified in a group consisting of halogen, a cyano group, -SO₂R⁷, -NR⁴R⁵ and -C(=O)OCH₃; or R⁴ and R⁵ together with an atom, whereto attached form a 5-6-member heterocycle wherein the 5-6-member heterocycle optionally contains one or more N, O or S atom, and each 5-6-member heterocycle is optionally substituted by one or more groups consisting of halogen, hydroxyl, an amino group, alkyl having 1 to 4 carbon atoms, hydroxyalkyl 1 to 4 carbon atoms, -SO₂R⁷, -C(O)NR⁴R⁵, -C(O)R⁷, =O; R⁷ represents alkyl 1 to 4 carbon atoms; and R⁸ is specified in a group consisting of alkyl 1 to 4 carbon atoms, and cycloalkyl representing a 5-6-member monocyclic ring group consisting of carbon completely. The invention also refers to methods for preparing them, a pharmaceutical composition having dipeptidyl peptidase IV inhibitory activity and containing said derivatives.

EFFECT: there are produced new compounds and composition on their basis which can find application in medicine for treating type 2 diabetes mellitus or hyperglycemia.

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