申请人:NIPPON SHINYAKU COMPANY, LIMITED
公开号:EP0781766A1
公开(公告)日:1997-07-02
A pharmaceutical composition comprising a compound of the following general formula [I] or its salt.
wherein R1 represents aryl or a heteroaromatic group.
R2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino, or phenyl. R3 and R4 independently represent hydrogen or alkyl or R3 and R4 taken together with the adjacent N atom represent a 5- through 7-membered cyclic amino group. A represents C2-10 alkylene. W represents O, S, or (CH)n (where CH may be substituted by alkyl; n is an integer of 0, 1 or 2). X, Y, and Z may be the same or different and each represents CH (which may be substituted by alkyl), or N. Provided, however, that the case in which X, Y, and Z concurrently represent CH is excluded.
The compound of the invention has excellent neuronal death inhibitory activity and is useful as a therapeutic drug for cerebrovascular diseases.
一种药物组合物,包含下式通式[I]的化合物或其盐。
其中 R1 代表芳基或杂芳基。
R2 代表氢、烷基、烯基、环烷基、环烷基烷基、羟基烷基、卤代烷基、烷氧基、烷硫基、氨基、单烷基氨基、二烷基氨基或苯基。R3 和 R4 独立地代表氢或烷基,或 R3 和 R4 与相邻的 N 原子一起代表 5 至 7 元环状氨基。A 代表 C2-10 亚烷基。W 代表 O、S 或 (CH)n(其中 CH 可被烷基取代;n 为 0、1 或 2 的整数)。X、Y 和 Z 可以相同或不同,各自代表 CH(可被烷基取代)或 N,但不包括 X、Y 和 Z 同时代表 CH 的情况。
本发明化合物具有优异的神经元死亡抑制活性,可作为脑血管疾病的治疗药物。