PYRAZOLE-PYRIMIDINE DERIVATIVES AS mGluR2 ANTAGONISTS Russian patent published in 2010 - IPC C07D487/04 A61K31/519 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrazole-pyrimidine derivatives having metabotropic glutamate receptor (mGluR2) antagonist properties and having formula (1): , where A is selected from a group consisting of: R^a is H, halogen or C_1-6-alkyl; R¹ is II, halogen, C_1-6-alkoxy, C_1-6-alkyl, C_1-6-haloalkyl, C_1-6-haloalkoxy; R² is a halogen, C_1-6-haloalkyl; R³ is NR^bR^c, where R^b and R^c are independently selected from a group consisting of H and C_1-6-alkyl which is possibly substituted with one or more substitutes selected from a group consisting of hydroxy and -NR^b'R^c', where R^b' and R^c' are independently selected from a group consisting of H and C_1-6-alkyl; or R^b and R^c together with the nitrogen atom to which they are bonded form a possibly substituted heterocyclic group containing 5-6 ring atoms, possibly containing an additional N heteroatom, where the substitutes are selected from a group consisting of hydroxy and C_1-6-alkyl, R⁴ is C_1-6-haloalkyl or C_3-4-cycloalkyl; as well as to pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition and use of the compounds in preparing a medicinal agent for treating or preventing diseases and conditions in which mGluR2 activation plays a role.

EFFECT: improved properties of compounds.

10 cl, 2 dwg, 1 tbl, 129 ex