Galanthamine derivatives as acetylcholinesterase inhibitors

发明授权

US06316439B1 Galanthamine derivatives as acetylcholinesterase inhibitors 失效

标题翻译： Galanthamine衍生物作为乙酰胆碱酯酶抑制剂

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专利标题： Galanthamine derivatives as acetylcholinesterase inhibitors
专利标题（中）： Galanthamine衍生物作为乙酰胆碱酯酶抑制剂
申请号： US08137444

申请日： 1993-10-15
公开(公告)号： US06316439B1

公开(公告)日： 2001-11-13
发明人: Raymond W. Kosley, Jr. , Larry Davis , Veronica Taberna
申请人： Raymond W. Kosley, Jr. , Larry Davis , Veronica Taberna
主分类号： C07D49106
IPC分类号： C07D49106

Galanthamine derivatives as acetylcholinesterase inhibitors

摘要：

This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, aryl(C1-C12)alkylaminocarbonyl, mono(C1-C18)alkylaminocarbonyl or di(C1-C8)alkylaminocarbonyl; R2 is (C1-C12)alkylcarbonyloxy, aryl(C1-C4)alkylcarbonyloxy, (C1-C12)alkoxycarbonyloxy, arylcarbonyloxy, hydroxy, (C1-C6)alkoxycarbonyl(C1-C6)alkoxy or hydroxy(C1-C10)alkoxy; R3 is hydrogen or halo; and pharmaceutically acceptable addition salts; with the proviso that when R2 is hydroxy, R1 and R3 are not both hydrogen or when R2 is hydroxy and R3 is hydrogen, R1 is not methylcarbonyl; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.

摘要（中）：

本申请涉及式（Ⅳ）化合物，其中R1是氢，（C1-C12）烷基羰基，（C1-C12）烷氧基羰基，芳基（C1-C12）烷基氨基羰基，单（C1-C18）烷基氨基羰基或二（C1-C8）烷基氨基羰基; R2是（C1-C12）烷基羰基氧基，芳基（C1-C4）烷基羰基氧基，（C1-C12）烷氧基羰氧基，芳基羰基氧基，羟基，（C1-C6）烷氧羰基（C1-C6）烷氧基或羟基（C1-C10）是氢或卤素; 和药学上可接受的加成盐; 条件是当R 2是羟基时，R 1和R 3不是氢或当R 2是羟基且R 3是氢时，R 1不是甲基羰基;这些化合物可用于治疗以胆碱能功能降低为特征的记忆功能障碍，含有化合物的制备和使用方法。

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