申请人:Marion Merrell Dow Inc.
公开号:US05036107A1
公开(公告)日:1991-07-30
1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one. The compounds are highly specific M.sub.1 -AChR antagonists with relatively prolonged duration of activity. They are particularly useful in the treatment of neurogenic bladder disorders and may be administered orally or parenterally in conventional formulations containing optional conventional additives such as binders, surfactants, emulsifiers, flavorants, preservatives and the like.
1-苯基-7-取代庚-5-炔-2-酮在1-位置取代有C.sub.1到C.sub.7烷基,C.sub.3到C.sub.6环烷基,芳基,杂芳基或杂环烷基基团,并在7-位置取代有氨基,二烷基氨基,哌啶基,吡咯基或六氢吲哚基的化合物被披露,除了1-位置的苯基外还可能有一个或两个取代基,并且苯基上也可能有一个对氟取代基。首选化合物是1-环己基-1-苯基-1-羟基-7-二甲基氨基庚-5-炔-2-酮,1-环丁基-1-苯基-1-羟基-7-二甲基氨基庚-5-炔-2-酮和1-环-1-苯基-1-羟基-7-乙基氨基庚-5-炔-2-酮。这些化合物是高度特异的M.sub.1 -AChR拮抗剂,具有相对较长的活性持续时间。它们在神经源性膀胱疾病的治疗中特别有用,可以口服或经肠道给药,含有可选的传统添加剂,如粘合剂,表面活性剂,乳化剂,调味剂,防腐剂等的传统配方。