Shanghai Institute of Pharmaceutical Industry

Nhwa Pharma. Corporation

Jiangsu Hengyi Pharmaceutical Co., Ltd.

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

Sinopharm A-think Pharmaceutical Co., Ltd.

Sinopharm A-think Medical and Pharmaceutical Research & Development (beijing) Co., Ltd.

Cspc Zhonggi Pharmaceutical Technology (shijiazhuang) Co. Ltd.

Shanhai Institute of Pharmaceutical Industry

Shanghai Zhongze Therapeutics, Co. Ltd.

Cspc Zhongqi Pharmaceutical Technology Co., Ltd.

Jianqi Li

Guan Zhong Wang

Guisen Zhang

Wangping Cai

Xiangqing Xu

Yongyong Zheng

Liying Huang

Kai Gao

Xiaowen Chen

Qingwei Zhang

Yali Li

Shicheng Liu

Yanqin Ma

Xiangping Yang

Zhijie Weng

Lin Guo

Na Lv

Chunnian Zhang

Fang Liu

Yuan Yuan Zhang

Juan Feng

Minquan Yu

Song Zhao

Hua Jin

Shaoping Peng

Xican Tang

Junwei Xu

Shixia Zhou

Chengjin Shi

Xia Ge

Linjie Zhang

Guoyuan Hu

Yang Min

Yangli Qi

Ruixiang Yuan

Qiang Pu

Wenxin Dong

Shuming Hu

Wenhua Ji

Yumei Wang

Peng Xie

Yunfeng Liao

Jiajing Wang

Zhidan Jia

Ning Cui

Zhilong Ma

Guan Wang

Disclosed in the present invention are a pyridinyl morpholine compound, a preparation method therefor, and an application thereof. The present invention provides a pyridinyl morpholine compound as represented by formula I, a pharmaceutically acceptable salt thereof or a hydrate of the pharmaceutically acceptable salt thereof. The compound can be used as an antagonist for one or more of D, Dor 5-HT, and is used for preparing a drug for treating schizophrenia.

Pyridinyl morpholine compound, preparation method therefor, and application thereof

Disclosed are benzoisothiazole compounds and a use in the preparation of anti-schizophrenia drugs. The benzoisothiazole compounds of the present invention not only have strong affinity for dopamine Dreceptor, 5-HTreceptor and 5-HTreceptor, but also can observably improve the symptoms of schizophrenia relevant to apomorphine model and MK-801 model mice, with oral absorption being good, safety being high and side-effect being less, and having developmental value as new anti-neurotic disease drugs. The present invention is the compounds having a structure of general formula (I), or geometric isomers, free alkalies, salts, hydrates or solvates thereof. 

Benzoisothiazole compounds and methods of treating schizophrenia

Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesic drugs, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytrptamine, and also are novel antidepressants regulating 5-hydroxytrptamine. This class of compounds also has less toxic and side effects and a higher safety range. The 3-cyanoanilinoalkylarylpiperazine derivative is a compound shown as formula (III) or free base or salt thereof: 

3-cyanoanilinoalkylarylpiperazine derivative and use thereof in preparing drugs

Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumors, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof. 

Histone deacetylase inhibitor of benzamides and use thereof

The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic. 

4-aminoquinazoline derivatives and uses thereof

Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al. 

Aralkyl diamine derivatives and uses thereof as antidepressants

The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation. The histone deacetylase inhibitors are the compounds represented by the following formula or salts thereof: 

Histone deacetylase inhibitors and uses thereof

The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein Cand Crepresent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R, R, Rand Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.

Substituted phenylpiperazinyl aralkylalcohol derivatives, pharmaceutical compositions containing such derivatives and uses thereof

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 present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula. 

Aralkyl substituted piperidine or piperazine derivatives and their use for treating schizophrenia

The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereof. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like. The derivative is a compound having the following general formula or its salt: 

Aralkyl alcohol pyridine derivative compounds and the use thereof as medicaments for treating depression

The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects. 

Aralkyl piperidine derivatives and their uses as antalgic or ataractic agent

The use of aryl piperazines of formula (I) in manufacturing a medicament for treating acute pain, neuropathic pain or receptive nociceptive pain in mammals including human beings is disclosed. 

Use of aryl piperazine derivatives in manufacturing medicants for treating pain

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

Aryl alkanol piperazine derivatives of the formula and pharmaceutical compositions comprising the same. Also disclosed are methods for treating depression using the pharmaceutical composition. Compounds of the invention have excellent dual inhibitory actions to the uptake of the mono-amines neurotransmitter, good antidepressant activities and minor side effects.

Aralkyl-alcohol peiperazine derivatives and their uses as antidepressant

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Shanghai, China

Jianqi Li