IMIDAZOL-4-YLETHYNYL PYRIDINE DERIVATIVES, METHOD OF THEIR OBTAINING (VERSIONS) AND APPLICATION AS ANXIOLYTIC, PHARMACEUTICAL COMPOSITION AND METHOD OF TREATMENT OF DISORDERS MEDIATED BY RECEPTOR mGLuR5 Russian patent published in 2008 - IPC C07D401/06 C07D401/14 C07D413/14 C07D417/14 A61K31/4178 A61K31/4439 A61P25/00 

FIELD: chemistry.

SUBSTANCE: claimed invention relates to derivatives of 4-[1-arylimidazol-4-yl ethynyl]-2-alkylpyridine and 4-[1-heteroarylimidazol-4-yl ethynyl]-2-alkylpyridine of general formula I having general formula I in which R¹ stands for C₁-C₆alkyl; R² stands for C₁-C₆alkyl or C₃-C₁₂cycloalkyl; R³ stands for aryl or heteroaryl, where aryl or heteroaryl are unsubstituted or contain substituents, selected from group, including halogen, C₁-C₆alkyl, S-C₁-C₆alkyl, C₁-C₆alkylhlogen, C₁-C₆alkoxygroup, halogen- C₁-C₆lkoxygroup, C₃-C₁₂cycloalkyl, C₂-C₁₁heterocycloakyl, C₁-C₆alkylminogroup,di- C₁-C₆alkylaminogroup, C₁-C₆alkoxyaminogroup, (C₁-C₆ alkoxy) C₁-C₆alkylaminogroup, C₃-C₁₂cycloalkylaminogroup, benzylaminogroup and cyanogroup, where said "aryl" represents phenyl, and said " heteroaryl" represents aromatic 5- or 6- member ring or one or more condensed rings, containing one or more heteroatoms, selected from group, which includes nitrogen, oxygen and sulfur; and R⁴ stands for hydrogen, C(O)H or CH₂R⁵ , where R stands for hydrogen or its pharmaceutically acceptable salt. Invention also relates to method of obtaining compounds of general formula I, their application as anxiolytic, to based on them pharmaceutical composition and method of treatment or prevention of disorders, fully or partly mediated by metabotropic glutamate receptor of subtype 5.

EFFECT: obtaining novel heterocyclic compounds possessing useful biological properties.

15 cl, 18 ex