PYRIDINE AND PYRIMIDINE DERIVATIVES AS mGluR2 ANTAGONISTS Russian patent published in 2012 - IPC C07D213/34 C07D401/04 C07D401/10 C07D401/14 C07D403/04 C07D403/14 C07D413/04 C07D413/14 C07D233/96 C07D409/10 C07D409/14 C07D407/04 A61K31/505 A61K31/506 A61K31/44 A61P25/18 A61P25/28 A61P25/20 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: this invention relates to new compounds with formula (I) possessing the properties of mGLuR2 antagonists, to their obtainment methods, their application for production of medicines for prevention and treatment of disorders wherein mGLuR2 plays the activation role (in particular - central nervous system disorders). In formula (I) either any of X and Y represents N while the other represents CH or each of X and Y represents N; A represents aryl representing phenyl or 5- or 6-membered heteroaryl containing in the cycle 1-3 atoms selected from among nitrogen, oxygen or sulphur, the heteroaryl selected from among amidazolyl, [1,2,4] oxadiazolyl, pyrrolyl, 1H-pyrazolyl, pyridinyl, [1,2,4] triazolyl, tiazolyl and pyrimidinyl, each of them substitutable by C_1-6-alkyl; B represents H, cyano or represents a possibly substituted aryl selected from among phenyl or possibly substituted by 5- or 6-membered heteroaryl containing in the cycle 1-3 atoms selected from among nitrogen, oxygen or sulphur where the substitutes are selected from the group consisting of nitro, C_1-6-alkyl, possibly substituted hydroxy, NR^aR^b where R^a and R^b independently represent H, C_1-6-alkyl etc. R¹ represents H, a halogen atom, C_1-6-alkyl, possibly substituted hydroxy, C_1-6-alcoxy, C_1-6-halogenoalkyl, C_3-6-cycloalkyl represents H cyano, a halogen atom, C_1-6-halogenoalkyl, C_1-6-alcoxy, C_1-6-halogenoalcoxi-, C_1-6-alkyl or C_3-6-cycloalkyl R³ represents a halogen atom, H, C_1-6-alcoxy, C_1-6-halogenoalkyl, C_1-6-alkyl, C_3-6-cycloalkyl, C_1-6-halogenoalcoxy R⁴ reprsents H or halogeno.

EFFECT: creation of new compounds of formula (I) possessing mGLuR2 antagonist properties.

104 cl, 465 ex