A Pharmaceutical Composition of Derivatives of - 1.2 - 1.2 bencisoxasola and bencixotiazola and preparation method thereof

摘要

Disclosed are 1,2-benzisoxazole and 1,2-benzisothiazole derivatives represented by formula I IMAGE (I) wherein X represents oxygen or sulfur; Z rep;esents carbon (CH) so as to complete the imidazol-1-yl ring radical or Z represents nitrogen (N) so as to complete the 1,2,4-triazol-1-yl ring radical; R1 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; R2 represents hydrogen, lower alkenyl, lower alkynyl, aryl-lower alkyl or lower alkyl; or R1 and R2 combined represent lower alkylene; or R1 combined with R5 located on the Z-carbon atom of the imidazolyl radical represents C2-C4-alkylene; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, halogen, trifluoromethyl, cyano, nitro, amino, hydroxy, lower alkanoyloxy, carbocyclic aroyloxy, lower alkoxy, or carbocyclic aryl; or R3 and R4, together when located on adjacent carbon atoms, represent lower alkylenedioxy; or R3 and R4, together when located on the carbon atoms to which attached a benzo-fused or C5-C7-cycloalka-fused ring, respectively; R5 located on carbon represents hydrogen, lower alkyl or hydroxy-lower alkyl; R6 located on carbon represents hydrogen or lower alkyl; or when Z represents carbon, R5 located on the Z-carbon atom combined with R6 located on the adjacent carbon atom represents C3-C5-alkylene; and pharmaceutically acceptable salts thereof; which are active in mammals as anticonvulsant agents.