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    Galanthamine derivatives as acetylcholinesterase inhibitors
    1.
    发明授权
    Galanthamine derivatives as acetylcholinesterase inhibitors 失效
    Galanthamine衍生物作为乙酰胆碱酯酶抑制剂

    公开(公告)号：US06323195B1

    公开(公告)日：2001-11-27

    申请号：US08137440

    申请日：1993-10-15

    申请人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    发明人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    IPC分类号： C07D49106

    CPC分类号： C07D491/10 ,  C07D491/06

    摘要： This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is hydrogen, (C3-C12)alkenylcarbonyloxy, (C3-C12)cycloalkylcarbonyloxy, (C3-C12)cycloalkyl(C1-C12)alkylcarbonyloxy, oxygen containing heterocycloxy, oxygen containing heterocyclylcarbonyloxy, sulfur containing heterocyclyloxy, sulfur containing heterocyclylcarbonyloxy, nitrogen containing hetercyclyloxy, nitrogen containing heterocyclylcarbonyloxy, haloalkylsulfonyloxy, (C1-C6)alkylsilyloxy; R3 is hydrogen, halo or (C1-C4)alkyl; R4 is hydrogen or (C1-C6)alkyl; with the proviso that R1 and R2 are not both hydrogen when R3 and R4 are hydrogen; all geometric, and optical stereoisomers thereof, or a pharmaceutically acceptable addition salt thereof; 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.

    摘要翻译： 本申请涉及式（Ⅳ）的化合物是氢，（C1-C12烷基羰基，（C1-C12）烷氧基羰基，单（C1-C12）烷基氨基羰基或二（C1-C12）烷基氨基羰基; R2是氢，（C3-C12）烯基羰氧基 ，（C 3 -C 12）环烷基羰基氧基，（C 3 -C 12）环烷基（C 1 -C 12）烷基羰基氧基，含氧杂环氧基，含氧杂环基羰基氧基，含硫杂环基氧基，含硫杂环基羰基氧基，含氮杂环氧基，含氮杂环基羰基氧基，卤代烷基磺酰氧基，（C1- C6）烷基甲硅烷氧基; R3是氢，卤素或（C1-C4）烷基; R4是氢或（C1-C6）烷基;条件是当R3和R4是氢时，R1和R2不都是氢; 其光学立体异构体或其药学上可接受的加成盐;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，含有该组合物的药物组合物 制备和使用该化合物的方法和方法。

    Galanthamine derivatives as acetylcholinesterase inhibitors
    2.
    发明授权
    Galanthamine derivatives as acetylcholinesterase inhibitors 失效
    Galanthamine衍生物作为乙酰胆碱酯酶抑制剂

    公开(公告)号：US06316439B1

    公开(公告)日：2001-11-13

    申请号：US08137444

    申请日：1993-10-15

    申请人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    发明人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    IPC分类号： C07D49106

    CPC分类号： C07D491/10

    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.

    摘要翻译： 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。

    Galanthamine derivatives as acetylcholinesterase inhibitors
    3.
    发明授权
    Galanthamine derivatives as acetylcholinesterase inhibitors 失效
    Galanthamine衍生物作为乙酰胆碱酯酶抑制剂

    公开(公告)号：US06323196B1

    公开(公告)日：2001-11-27

    申请号：US08137443

    申请日：1993-10-15

    申请人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    发明人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    IPC分类号： C07D49106

    CPC分类号： C07D491/10

    摘要： This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is mono(C1-C18)alkylaminocarbonyloxy, di(C1-C8)alkylaminocarbonyloxy, or aryl(C1-C4)alkylaminocarbonyloxy; R3 is hydrogen or halo; or a pharmaceutically acceptable acid addition salt thereof, 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.

    摘要翻译： 本申请涉及式（Ⅳ）化合物，其中R1为氢，（C1-C12）烷基羰基，（C1-C12）烷氧基羰基，单（C1-C12）烷基氨基羰基或二（C1-C12）烷基氨基羰基; R2为单（C1-C18 ）烷基氨基羰基氧基，二（C1-C8）烷基氨基羰基氧基或芳基（C1-C4）烷基氨基羰基氧基; R3是氢或卤素; 或其药学上可接受的酸加成盐，所述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，含有该化合物的药物组合物以及制备和使用该化合物的方法。