申请人:ASTELLAS PHARMA INC
公开号:WO2006033446A1
公开(公告)日:2006-03-30
The present invention relates to a compound of the formula [I]: wherein (a), in which -Y-, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20 R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, -Z-R9 or (b), in which -Z- is -0-, -S-, R9 -SO- or -SO2-, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R10, in which -D- is -CONHSO2- or -S02NHCO-, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.
本发明涉及一种具有以下结构的化合物[I]:其中(a)中的-Y-,R4,R5和R6分别如描述中定义,等等,R1为氢,卤素,低烷基,羟基等,R2为氢,低烷基或羟基(低)烷基,R3为氢或氨基保护基,R7为氢,低烷基,环(低)烷基,低R9烯基,-Z-R9或(b),其中-Z-为-0-,-S-,R9-SO-或-SO2-,每个R9独立地为氢,低烷基,环(低)烷基等,R8为-D-E-R10,其中-D-为-CONHSO2-或-S02NHCO-,E为键或低烷基,R10为卤素,氰基,羧基等,或其前药或盐。本发明的化合物[I]及其药学上可接受的盐对于预防和/或治疗溃疡,过度活跃的膀胱等疾病是有用的。