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    THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF
    3.
    发明公开
    THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF 有权
    1-BUTYL-2-HYDROXARARKYL-PIPERAZIN-DERIVATE UND IHRE VERWENDUNG ALS ANTIDEPRESSIVA

    公开(公告)号：EP2351746A1

    公开(公告)日：2011-08-03

    申请号：EP09818779.2

    申请日：2009-09-29

    申请人： CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. ,  Shanghai Institute of Pharmaceutical Industry

    发明人： LI, Jianqi ,  LV, Na ,  JIN, Hua ,  WENG, Zhijie ,  ZHENG, Yongyong

    IPC分类号： C07D295/084 ,  A61K31/495 ,  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，神经毒性降低和副反应较少; 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靠性。 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：