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    Benzothiophene alkanol piperazine derivatives and their use as antidepressant
    1.
    发明授权
    Benzothiophene alkanol piperazine derivatives and their use as antidepressant 失效
    苯并噻吩烷醇哌嗪衍生物及其用作抗抑郁药

    公开(公告)号：US08680097B2

    公开(公告)日：2014-03-25

    申请号：US13001998

    申请日：2009-06-30

    申请人： Jianqi Li ,  Kai Gao ,  Na Lv

    发明人： Jianqi Li ,  Kai Gao ,  Na Lv

    IPC分类号： A61K31/496 ,  A61K31/5377 ,  C07D333/58 ,  C07D409/12 ,  C07D413/12

    CPC分类号： C07D409/06 ,  C07D409/14

    摘要： The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.

    摘要翻译： 本发明公开了苯并噻吩烷醇哌嗪衍生物及其作为抗抑郁药的用途。 本发明公开了对5-HT，NA和DA的再摄取具有三重抑制作用的所述苯并噻吩烷醇哌嗪衍生物。 与迄今为止具有单一目标的临床使用的抗抑郁药相比， 本发明的所述苯并噻吩烷醇哌嗪衍生物可能具有更广泛的适应范围和对神经系统的毒副作用较小的临床用途的抗抑郁药，目前为止具有双重目标，例如文拉法辛和度洛西汀。 苯并噻吩烷醇哌嗪衍生物是具有下式的化合物或其药学上可接受的盐，其中Ar1，R1-R4，X，Y，m和n具有与权利要求1中所定义的相同的定义。

    BENZOTHIOPHENE ALKANOL PIPERAZINE DERIVATIVES AND THEIR USE AS ANTIDEPRESSANT
    2.
    发明申请
    BENZOTHIOPHENE ALKANOL PIPERAZINE DERIVATIVES AND THEIR USE AS ANTIDEPRESSANT 失效
    苯并噻唑烷醇衍生物及其用作抗生素

    公开(公告)号：US20110118263A1

    公开(公告)日：2011-05-19

    申请号：US13001998

    申请日：2009-06-30

    申请人： Jianqi Li ,  Kai Gao ,  Na Lv

    发明人： Jianqi Li ,  Kai Gao ,  Na Lv

    IPC分类号： A61K31/5377 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  A61K31/497 ,  A61P25/24

    CPC分类号： C07D409/06 ,  C07D409/14

    摘要： The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.

    摘要翻译： 本发明公开了苯并噻吩烷醇哌嗪衍生物及其作为抗抑郁药的用途。 本发明公开了对5-HT，NA和DA的再摄取具有三重抑制作用的所述苯并噻吩烷醇哌嗪衍生物。 与迄今为止具有单一目标的临床使用的抗抑郁药相比， 本发明的所述苯并噻吩烷醇哌嗪衍生物可能具有更广泛的适应范围和对神经系统的毒副作用较小的临床用途的抗抑郁药，目前为止具有双重目标，例如文拉法辛和度洛西汀。 苯并噻吩烷醇哌嗪衍生物是具有下式的化合物或其药学上可接受的盐，其中Ar1，R1-R4，X，Y，m和n具有与权利要求1中所定义的相同的定义。

    1-butyl-2-hydroxyaralkyl piperazine derivatives and the uses as anti-depression medicine thereof
    3.
    发明授权
    1-butyl-2-hydroxyaralkyl piperazine derivatives and the uses as anti-depression medicine thereof 有权
    1-丁基-2-羟基烷基哌嗪衍生物及其作为抗抑郁药的用途

    公开(公告)号：US08252796B2

    公开(公告)日：2012-08-28

    申请号：US13122691

    申请日：2009-09-29

    申请人： Jianqi Li ,  Na Lv ,  Hua Jin ,  Zhijie Weng ,  Yongyong Zheng

    发明人： Jianqi Li ,  Na Lv ,  Hua Jin ,  Zhijie Weng ,  Yongyong Zheng

    IPC分类号： A61K31/495 ,  C07D241/04

    CPC分类号： A61K31/495 ,  C07D295/088 ,  C07D295/092

    摘要： The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art. The 1-butyl-2-hydroxyl aralkyl piperazine derivative is the free alkali or its salt of a compound of formula below:

    摘要翻译： 本发明公开了1-丁基-2-羟基芳烷基哌嗪衍生物及其作为抗抑郁药的用途。 本发明的衍生物对5-HT，NA和DA的再摄取具有三重抑制作用，并且可以通过口服给药，注射等途径以组合物的形式施用于有需要的患者。 与临床目前使用的双抗抑郁药（如文拉法辛）相比，所述衍生物可能具有更强的抗抑郁作用，适应症广，发病更快，神经毒性和副反应降低; 与现有技术中公开的芳基链烷醇哌嗪衍生物及其旋光异构体相比，所述衍生物具有更强的抗抑郁活性，更低的毒性，更高的生物利用度，更长的半衰期和更好的药物可用性。 1-丁基-2-羟基芳烷基哌嗪衍生物是下式化合物的游离碱或其盐：

    THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF
    4.
    发明申请
    THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF 有权
    1-丁基-2-羟基甲基哌嗪衍生物及其作为抗抑郁药物的用途

    公开(公告)号：US20110183996A1

    公开(公告)日：2011-07-28

    申请号：US13122691

    申请日：2009-09-29

    申请人： Jianqi Li ,  Na Lv ,  Hua Jin ,  Zhijie Weng ,  Yongyong Zheng

    发明人： Jianqi Li ,  Na Lv ,  Hua Jin ,  Zhijie Weng ,  Yongyong Zheng

    IPC分类号： A61K31/495 ,  C07D295/096 ,  A61P25/24

    CPC分类号： A61K31/495 ,  C07D295/088 ,  C07D295/092

    摘要： The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art. The 1-butyl-2-hydroxyl aralkyl piperazine derivative is the free alkali or its salt of a compound of formula below:

    摘要翻译： 本发明公开了1-丁基-2-羟基芳烷基哌嗪衍生物及其作为抗抑郁药的用途。 本发明的衍生物对5-HT，NA和DA的再摄取具有三重抑制作用，并且可以通过口服给药，注射等途径以组合物的形式施用于有需要的患者。 与临床目前使用的双抗抑郁药（如文拉法辛）相比，所述衍生物可能具有更强的抗抑郁作用，适应症广，发病更快，神经毒性和副反应降低; 与现有技术中公开的芳基链烷醇哌嗪衍生物及其旋光异构体相比，所述衍生物具有更强的抗抑郁活性，更低的毒性，更高的生物利用度，更长的半衰期和更好的药物可用性。 1-丁基-2-羟基芳烷基哌嗪衍生物是下式化合物的游离碱或其盐：