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    Method for treating depression with thioxanthen-9-one derivatives
    4.
    发明授权
    Method for treating depression with thioxanthen-9-one derivatives 失效
    用噻吨-9-酮衍生物治疗抑郁症的方法

    公开(公告)号：US4737514A

    公开(公告)日：1988-04-12

    申请号：US817752

    申请日：1986-01-02

    申请人： Morton Harfenist ,  Charles T. Joyner ,  Darryl J. Heuser

    发明人： Morton Harfenist ,  Charles T. Joyner ,  Darryl J. Heuser

    IPC分类号： C07D335/16 ,  C07D409/04 ,  A61K31/38 ,  A61K31/535

    CPC分类号： C07D409/04 ,  C07D335/16

    摘要： Compounds of formula (I) ##STR1## wherein n is 0, 1 or 2;one or R.sup.1 and R.sup.2 is hydrogen and the other is selected from carbamoyl, N-C.sub.1-4 alkylcarbamoyl, N,N-di-C.sub.1-4 alkylcarbamoyl, carbamimidoyl, N.sup.1 -C.sub.1-4 alkylcarbamimidoyl, N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1 -C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl and imidazolin-2-yl (optionally substituted by one or more C.sub.1-4 alkyl groups); andR.sup.3 is selected from hydrogen, saturated and unsaturated aliphatic hydocarbon moieties containing from 1 to 4 carbon atoms, groups OR.sup.4 (where R.sup.4 is selected from hydrogen and saturated and unsaturated aliphatic hydrocarbon moieties containing from 1 to 4 carbon atoms), halo, groups of formula--NR.sup.5 R.sup.6 (where R.sup.5 and R.sup.6 are independently selected from hydrogen, C.sub.1-4 alkyl and hydroxy C.sub.1-4 alkyl, provided that the total number of carbon atoms in R.sup.5 and R.sup.6 does not exceed 4), amino C.sub.1-4 alkylamino and morpholino,provided that when n is 2 and R.sup.2 is hydrogen, thenR.sup.1 is not carbamoyl when R.sup.3 is hydrogen or methyl; andR.sup.1 is not N-methylcarbamoyl when R.sup.3 is hydrogen; and physiologically acceptable salts thereof, and their pro-drugs and metabolites are inhibitors of monoamine oxidase-A and are useful in the prophylaxis and treatment of mental disorders such as depression.

    摘要翻译： 式（I）化合物其中n为0,1或2; 一个或R 1和R 2是氢，另一个选自氨基甲酰基，N-C 1-4烷基氨基甲酰基，N，N-二-C 1-4烷基氨基甲酰基，氨基甲脒基，N 1 -C 1-4烷基甲脒基，N 2 -C 1-4烷基甲脒基， 1-4烷基-N 2 -C 1-4烷基甲脒基，N 1，N 1 - 二-C 1-4烷基甲脒基，N 1，N 1 - 二-C 1-4烷基-N 2 -C 1-4烷基甲脒基和咪唑啉-2-基（任选地被一个或多个 C 1-4烷基）; 并且R 3选自氢，饱和和不饱和的含有1至4个碳原子的脂族烃部分，OR 4基团（其中R 4选自氢和含有1至4个碳原子的饱和和不饱和脂族烃部分），卤素， 式-NR5R6（其中R5和R6独立地选自氢，C1-4烷基和羟基C1-4烷基，条件是R5和R6中的碳原子总数不超过4），氨基C 1-4烷基氨基和吗啉代 条件是当n为2且R 2为氢时，则当R 3为氢或甲基时，R 1不为氨基甲酰基; 当R 3是氢时，R 1不是N-甲基氨基甲酰基; 及其生理上可接受的盐，其前药和代谢物是单胺氧化酶-A的抑制剂，可用于预防和治疗精神障碍如抑郁症。

    Use of nitrogen heterocyclic compounds
    5.
    发明授权
    Use of nitrogen heterocyclic compounds 失效
    使用氮杂环化合物

    公开(公告)号：US4616032A

    公开(公告)日：1986-10-07

    申请号：US688704

    申请日：1985-01-04

    申请人： Morton Harfenist

    发明人： Morton Harfenist

    IPC分类号： C07D335/16 ,  C07D409/04 ,  A61K31/385

    CPC分类号： C07D409/04 ,  C07D335/16

    摘要： A method of inhibiting monoamine oxidase-A in a mammal such as man, comprising administration to said mammal of an effective amount of a compound of formula (I') or a physiologically acceptable salt, or a pro-drug or metabolite thereof.In formula (I') ##STR1## n is 0, 1 or 2; one of R.sup.1 and R.sup.2 is hydrogen and the other is a tetrazol-5-yl group optionally substituted by one or more C.sub.1-4 alkyl groups; andR.sup.3 is selected from hydrogen, saturated and unsaturated aliphatic hydrocarbon moieties containing from 1 to 4 carbon atoms, groups OR.sup.4 (where R.sup.4 is selected from hydrogen and saturated and unsaturated aliphatic hydrocarbon moieties containing from 1 to 4 carbon atoms), halo, groups of formula --NR.sup.5 R.sup.6 (where R.sup.5 and R.sup.6 are independently selected from hydrogen C.sub.1-4 alkyl and hydroxy C.sub.1-4 alkyl, provided that the total number of carbona atoms in R.sup.5 and R.sup.6 does not exceed 4), amino C.sub.1-4 alkylamino and morpholino.The compounds of formula (I') and their physiologically acceptable salts are thus used in methods of prophylaxis and treatment of mental disorders such as depression.

    摘要翻译： 一种抑制哺乳动物（例如人）中的单胺氧化酶-A的方法，包括向所述哺乳动物施用有效量的式（I'）化合物或其生理学上可接受的盐或其前体药物或代谢物。 在式（I'）中，图像（I'）n为0,1或2; R1和R2之一是氢，另一个是任选被一个或多个C 1-4烷基取代的四唑-5-基; 并且R 3选自含有1至4个碳原子的氢，饱和和不饱和脂族烃部分，OR 4基团（其中R 4选自氢和含有1至4个碳原子的饱和和不饱和脂族烃部分），卤素， 式-NR5R6（其中R5和R6独立地选自氢C1-4烷基和羟基C1-4烷基，条件是R5和R6中的碳原子总数不超过4），氨基C 1-4烷基氨基和吗啉代。 因此，式（I'）化合物及其生理上可接受的盐用于预防和治疗精神障碍如抑郁症的方法中。