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    1,7-substituted heptyn-2-ones and use
    2.
    发明授权
    1,7-substituted heptyn-2-ones and use 失效
    使用1,7-取代庚炔-2-酮

    公开(公告)号：US5036107A

    公开(公告)日：1991-07-30

    申请号：US437165

    申请日：1989-11-16

    申请人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  Daniel W. McPherson ,  Ciro J. Spagnuolo ,  Kenneth J. Natalie, Jr.

    发明人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  Daniel W. McPherson ,  Ciro J. Spagnuolo ,  Kenneth J. Natalie, Jr.

    IPC分类号： C07D295/104

    CPC分类号： C07D295/104 ,  Y10S514/906 ,  Y10S514/929 ,  Y10S514/93 ,  Y10S514/935

    摘要： 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.

    摘要翻译： 被1-取代的C1-C7烷基，C3至C6环烷基，芳基，杂芳基或杂环烷基取代的1-苯基-7-取代的庚-5-炔-2-酮和一个氨基，二烷基氨基，哌啶基 ，公开了7-位上的吡咯烷基或六氢氮杂基，除了在1-位上的苯基之外，还可以具有一个或两个取代基，并且在苯基上也可以具有对氟取代基。 优选的化合物是1-环己基-1-苯基-1-羟基-7-二甲基氨基庚基-5-炔-2-酮，1-环丁基-1-苯基-1-羟基-7-二甲基氨基庚基-5-炔-2 - 酮和1-环-1-苯基-1-羟基-7-乙基氨基庚-5-酮-2-酮。 这些化合物是具有较长活性持续时间的高度特异性的M1-AChR拮抗剂。 它们在治疗神经性膀胱疾病中特别有用，并且可以在含有任选的常规添加剂如粘合剂，表面活性剂，乳化剂，调味剂，防腐剂等的常规制剂中口服或肠胃外给药。