PIPERIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS

摘要

The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C₁-C₄ alkylamino, or together form a group that contains one or more heteroatoms, and that taken together with one or more: (a) hydrogen atoms; (b) carbon atoms; (c) -CH- groups; (d) -CH₂- groups; or (e) additional heteroatoms of the same or different type; or any combination thereof, form a 4-7 membered homocyclic or heterocyclic ring, wherein the homocyclic or heterocyclic ring may combine with the phenyl group to form a bicyclic ring, and wherein the homocyclic or heterocyclic ring or the bicyclic ring may contain one or more oxo, thioxo, amino, mercapto, trifluoromethyl, C₁-C₄ alkyl, -S or -SH groups; W: is -CO-, -CH₂- or -CH₂-(C₁-C₄ alkyl)-; X: is -CO-; Y: is -O-, C₁-C₄ alkylene, C₁-C₄ alkynylene, cycloalkylene, aminocarbonyl, -NH-, -N(C₁-C₄ alkyl)-, -C₁-C₄ alkylene-N(C₁-C₄ alkyl)-, -CH₂O-, -CH(OH)- or -OCH₂-; Z: is hydrogen, halogen, nitro, amino, C₁-C₄ alkyl, C₁-C₄ alkoxy, cyano, trifluoromethyl, hydroxyl or carboxyl; R¹ and R²: are hydrogen, or together form a C₁-C₃ bridge; and n and m: independently are 0-3, wherein n and m cannot each be 0; or an optical antipode, racemate or pharmaceutically-acceptable salt thereof. The carboxylic acid amide derivatives of formula (I) are highly effective and selective antagonists of the NMDA receptor.