申请人:Li Jianqi
公开号:US20110118263A1
公开(公告)日:2011-05-19
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 Ar
1
, R
1
-R
4
, X, Y, m and n have the same definition as defined in claim
1.
该发明披露了苯并噻吩烷醇哌嗪衍生物及其作为抗抑郁药物的用途。该发明揭示了所述苯并噻吩烷醇哌嗪衍生物对5-HT、NA和DA的再摄取具有三重抑制效应。与迄今为止具有单一靶点的临床使用抗抑郁药物(如去甲丙胺和氟西汀)以及迄今为止具有双重靶点的临床使用抗抑郁药物(如文拉法辛和度洛西汀)相比,本发明的苯并噻吩烷醇哌嗪衍生物可能具有更广泛的适应症范围,对神经系统的毒性和副作用更少。苯并噻吩烷醇哌嗪衍生物是具有以下结构式或其药用盐的化合物,其中Ar1、R1-R4、X、Y、m和n的定义与权利要求1中定义的相同。