IMIDAZO[1,2-a]PYRIDINE DERIVATIVES AND THEIR APPLICATION AS POSITIVE ALLOSTERIC MODULATORS OF mGluR2 RECEPTORS Russian patent published in 2013 - IPC C07D471/04 A61K31/437 A61P25/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel imidazo[1,2-a]pyridine derivatives of general formula (I) or to its stereochemical isomeric forms, or to its pharmaceutically acceptable salts, where R¹ represents C_1-6alkyl; C_3-6cycloalkyl; trifluoromethyl; C_1-3alkyl, substituted with trifluoromethyl, C_3-7cycloalkyl, phenyl; phenyl, substituted with 2 substituents, selected from group, consisting of halogeno; R² represents cyano, halogeno or C_1-3alkyl; R³ represents radical of formula (a), or (b), or (d); R⁴ represents hydroxyC_3-6cycloalkyl; pyridinyl, substituted with one C_1-3alkyl group; pyrimidinyl; pyrimidinyl, substituted with two C_1-3alkyl groups; phenyl; phenyl, substituted with 1 or 2 substituents, selected from group, consisting of halogeno, hydroxyC_1-3alkyl, mono- or polyhalogenoC_1-3alkyl, C_1-3alkyloxy and monohalogeno- C_1-3alkyloxy; R⁵ represents hydrogen, fluoro, hydroxyl or monopholinyl; X represents C or N, with R⁵ representing electron pair on N; or R⁴-X-R⁵ represents radical of formula (i), or (j), or (k); n equals 0 or 1' q equals 1 or 2; R⁶ represents C_1-3alkyl; C_3-6cycloalkyl; hydroxyC_2-4alkyl; (C_3-6cycloalkyl)C_1-3alkyl; phenyl; or phenyl, or pyridinyl, substituted with one substituent, selected from group, consisting of halogeno, C_1-3alkyl and (CH₂)_m-CO₂H, where m equals 0; or R⁶ represents cyclic radical of formula (l); where R⁸ represents hydrogen, p equals 2; Z represents O or CR⁹(OH), where R⁹ represents hydrogen or C_1-3alkyl; R⁷ represents hydrogen or halogeno; Y represents covalent bond, O, NH, S, C(OH)(CH₃), -CH₂-O-, -O-CH₂-, CHF or CF₂; or R⁶-Y represents morpholinyl, pyrrolidinyl or piperidinyl, possibly substituted with hydroxyl or hydroxyC_1-3alkyl; and A represents O or NH. Invention also relates to pharmaceutical composition based on formula (I), its application and method of treatment or prevention of central nervous system disorders.

EFFECT: novel imidazo[1,2-a]pyridine derivatives, which possess activity of positive allosteric mGluR2 modulator are obtained.

21 cl, 3 tbl, 22 ex