ACETYLENE DERIVATIVES, METHOD OF THEIR OBTANING, PHARMACEUTICAL COMPOSITION BASED ON THEM AND THEIR USE AS ANTAGONISTS OF METABOTHROPIC GLUTAMATE RECEPTORS (MGLUR5) Russian patent published in 2008 - IPC C07C233/23 C07C271/12 C07C271/24 C07D209/32 C07D209/44 A61K31/164 A61K31/27 A61K31/4035 A61K31/404 

FIELD: chemistry.

SUBSTANCE: described are compounds of formula I in form of free base or acid-additive salt, method of their obtaining, pharmaceutical composition based on them and their application s antagonists of metabotropic glutamate receptors (mGluR5). The invention can be applied in the treatment of the illnesses connected with the disorder of glutamatic signal transfer and the disorder of nervous system partially or completety mediate mGluR5. In general formula T represents 0 or 1, A represents hydroxy, X represents hydrogen, Y represents hydrogen or A forms simple bond with X or Y; ring methylene group directly bound with CH(X)-, can be dimethylated; R₀ represents hydrogen, C₁-C₄alkyl, C₁-C₄alkoxy, halogen, cyano, and R represents -COR₃, -COOR₃ or -SO₂R₆,where R₃ represents C₁-C₄alkyl, C₃-C₇cycloakyl, and R₆ represents C₁-C₄alkyl, C₃-C₇cycloakyl, or R represents -C(O)R₃, where R₃ represents furanyl, trifluoromethyl, pyridinyl, morpholinyl or methylpiperasinyl; or -C(O)OR₃, where R₃ represents tetrahydrofuranyl, R' represents hydrogen, C₁-C₄alkyl or 4-methoxybenzyl, and R" represents hydrogen or C₁-C₄alkyl, or R' and R" together form group -CH₂-(CH₂)_p-, where p represents 0, 1 or 2, one of symbols n and p does not represent 0, on condition that R₀ does not represent hydrogen, trifluoromethyl and methoxy, when m represents 1, n represents 0, A represents hydroxy, X and Y both represent hydrogen, R represents COOEt and R' and R" together form group -(CH₂)₂-.

EFFECT: efficient application of compounds for treatment of diseases caused by disturbance of transduction of glutamatergic signal and diseases of nervous system.

8 cl, 11 ex