Shanghai Institute of Pharmaceutical Industry

Cspc Zhongqi Pharmaceutical Technology (shijiazhuang) Co., Ltd.

Cspc Zhonggi Pharmaceutical Technology (shijiazhuang) Co. Ltd.

Cspc Zhongqi Pharmaceutical Technology Co., Ltd.

Na Lv

Jianqi Li

Yongyong Zheng

Hua Jin

Kai Gao

Zhijie Weng

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, R-R, X, Y, m and n have the same definition as defined in claim. 

Benzothiophene alkanol piperazine derivatives and their use as antidepressant

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: 

1-butyl-2-hydroxyaralkyl piperazine derivatives and the uses as anti-depression medicine thereof

Growing community of inventors

Shanghai, China

Na Lv