Chinese Academy of Sciences

Ningbo Ziyuan Pharmaceuticals Inc.

Shanghai Lead Discovery Pharmaceuticals Limited Company

Shanghai Pharmaceutical (Group) Co., Ltd.

Jiangsu Zuoyou Medicine Co., Ltd.

Jianping Zuo

Wei Tang

Fajun Nan

Yangming Zhang

Min Gu

Yu Zhang

Jian Ding

Ying Nan Li

Haijun Chen

Youhong Hu

Jing Lan Chen

Yu Chen Zhou

Hong Tao Liu

Hualiang Jiang

Fei Ye

Li Yang

Kaixian Chen

Fan Zhang

Jingkang Shen

Tao Sun

Ying Li

Jianhua Shen

Linghua Meng

Jianxin Zhang

Yi Sui

Dong Lu

Xu Shen

Bing Xiong

Xiaomin Luo

Yu Zhou

Bo Chao

Fenghua Zhu

Lili Chen

Ru Ling Zhou

Shijun He

Peilan He

Guifeng Wang

Zhongshun Yang

Junxia Wang

Xiankun Tong

Limin Zeng

Feifei Liu

Wenlong Wang

Donglu Bai

Yiming Yang

Haibin Luo

Ping Li

Chunlan Feng

Zemin Lin

Dewen Li

Chongsheng Yuan

Feihong Ji

Linqian Yu

Na Yang

Yunzhe Zhang

Wenliang Zhou

Wuhong Chen

Jinming Wu

Chunshan Gui

Yifu Yang

Xianhan Zhuang

Xuchang He

Yuanchao Li

Yuxi Yan

Xiaoqian Yang

Zhong Shun Yang

Provided in the present invention is a use of methyl 4-[9-(6-aminopuryl)]-2(s)-hydroxybutyrate in the preparation of a medicament for treating psoriasis and vitiligo. More specifically, the present invention uses mice whose psoriasis is induced by an imiquimod cream to observe a changing condition in skin lesions on the psoriasis-like mice, according to a psoriasis skin lesion area of the mice and grading standards for disease severity; the present invention also observes a proportion of lymphocytes in the spleens and cytokines in skin lesion tissues of the mice. A good therapeutic effect may be obtained by treating typical cases of vitiligo with an ointment of methyl 4-[9-(6-aminopuryl)]-2(s)-hydroxybutyrate. Results show that methyl 4-[9-(6-aminopuryl)]-2(s)-hydroxybutyrate used in the present invention has a good therapeutic effect on psoriasis and vitiligo, as well as a favorable prospect in clinical application.

Application of methyl 4-[9-(6-aminopuryl)]-2(s)-hydroxybutyrate in preparation of medicament for treating psoriasis and vitiligo

Provided are a phthalazinone compound, method for preparation thereof, pharmaceutical composition thereof, and a use thereof; the structure of said phthalazinone compound is as represented by formula I; the compound of said formula I is targeted to a viral nucleocapsid; it can inhibit the replication of a virus by means of interference of the viral nucleocapsid, has a potent activity for inhibiting HBV DNA replication and a good liver targeting, can stably exist and enrich in the liver, and is a new and effective anti-HBV inhibitor. 

Phthalazinone compound, method for preparation thereof, pharmaceutical composition thereof, and use thereof

Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection. 

Use of a quinazoline compound in preparing a medicament against flaviviridae virus

The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on. 

Heterocyclic non-nucleoside compounds, their preparation, pharmaceutical composition and their use as antiviral agents

Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl. 

Rapamycin carbonic ester analogues, pharmaceutical compositions, preparations and uses thereof

The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2',2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability. 

2',2-bisthiazole non-nucleoside compounds, preparation methods, pharmaceutical compositions and uses as hepatitis virus inhibitors thereof

The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product. Comparing with the prior preparation methods, the present method has advantages in low cost, mild conditions, high retention of the chiral center during the reaction, high productivity, great improvement in the quality and yield of the product and great decrease in cost, and thus is suitable for the production on a large scale.

Method for preparing 4-(6-amino-purin-9-YL)-2(S)-hydroxy-butyric acid methyl ester

Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation. 

Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions and the use thereof

The invention provides a type of artemisinin derivatives having following structure I, its preparation method and use, as well as a pharmaceutical composition containing such artemisinin derivatives and its use. The arteminsinin derivatives of the present invention and their pharmaceutical composition containing the artemisinin derivatives. have immunosuppressive activities and can be used more safely. The composition which comprises the artemisinin derivatives can be formulated into long-term dosage forms such as tablet, pellet and the like, and have wider productive and use value. 

Artemisinin (qinghaosu) derivatives, their preparation methods and their use, and pharmaceutical compositions containing the same

The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared.

Bisheterocycle tandem compounds useful as antiviral agents, the uses thereof and the compositions comprising such compounds

The present invention discloses 3D-structure of SARS-CoV Viral 3CL Protease obtained through molecular simulation. The 3D-structure is used as a drug target for screening the existing medical database CMC (Comprehensive Medicinal Chemistry, MDL Information System, Inc.), and a group of compounds which have the activity of inhibiting SARS-CoV virus 3CL Protease are found. Cinanserin was tested at molecular and viral levels, and it was found to be able to inhibit the SARS-CoV viral 3CL protease and SARS-CoV viruses. Cinanserin analogs were synthesized and tested at molecular and viral levels, they were found to be able to inhibit the SARS-CoV virus 3CL Protease and SARS-CoV viruses, and may be used for treating and/or preventing SARS-CoV virus infection.

3D-structure model of SARS coronavirus 3CL protease and anti-SARS drugs

Triptolide derivatives of Formula (I), their pharmaceutically acceptable salts and optical isomers, Formula (I):  wherein, C5 and C6 are connect with each other by a C-C single bond or double bond; when C5 and C6 are connected with C-C single bond, X and Y represent independently hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula &#x2014;OCOR, &#x2014;OSOOR or &#x2014;OPO(OH), each of which is attached to C5 and C6, R represents &#x2014;(CH)nCONa, &#x2014;(CO)nCOK, or &#x2014;(CH)nCH, wherein n=1-6; Z represents hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula -OCOR, -OSOOR or &#x2014;OPO(OH)2, each of which is linked at C14-position, R represents &#x2014;(CH2)nCO2Na, &#x2014;(CO2)nCO2K, or &#x2014;(CH)nCH, wherein n=1-6; wherein, the'______' linked with X, Y, and Z represents the stereochemistry orientations '' or &#x201c;&#x201d; , but X and Y cannot both be hydrogen atom at the same time, methods for preparing the triptolides and their use as antiphiogistic agent, immunosuppressive agent or therapeutic agent for other related diseases.

Triptolide derivatives and their uses

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Shanghai, China

Jianping Zuo