Intermediates for spiro[2H-1,4-benzodioxepin-3(5H)4'piperidine] compounds
    31.
    发明授权
    Intermediates for spiro[2H-1,4-benzodioxepin-3(5H)4'piperidine] compounds 失效
    螺[2H-1,4-苯并二氧杂环庚烯-3(5H)4'-哌啶]化合物的中间体

    公开(公告)号:US4577026A

    公开(公告)日:1986-03-18

    申请号:US630134

    申请日:1984-07-12

    IPC分类号: C07D211/48 C07D491/10

    CPC分类号: C07D491/10 C07D211/48

    摘要: Spiro[2H-1,4-benzodioxepin-3(5H)4'-piperidine and -3-pyrrolidine] compounds of the formula ##STR1## where the substituents are as defined herein, are useful in the treatment of hypertension in mammals. Such compounds, their use as antihypertensive agents, pharmaceutical compositions containing the compounds, intermediates and processes for preparing the compounds are provided.

    摘要翻译: 具有本文定义的取代基的式[IMAGE]的螺[2H-1,4-苯并二氧杂环庚烷-3(5H)4'-哌啶和-3-吡咯烷]化合物可用于治疗哺乳动物的高血压。 提供这样的化合物,它们作为抗高血压药的用途,含有化合物的药物组合物,中间体和制备化合物的方法。

    Galanthamine derivatives as acetylcholinesterase inhibitors
    38.
    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

    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。