Chinese Academy of Sciences

Shanghai Puyi Chemical Co., Ltd.

Shanghai Theorion Pharmaceutical Co., Ltd.

Yangming Zhang

Fajun Nan

Jian Ding

Jia Tao Li

Yubo Zhou

Min Li

Xin Xie

Jianping Zuo

Mingbo Su

Haiyan Xu

Zhaobing Gao

Haining Hu

Wei Tang

Fei Chen

Linghua Meng

Min Gu

Chaojun Gong

Xiaoping Pi

Huanan Liu

Sheng Liu

Yi Chen

Meiyu Geng

Ying Xiong

Xiaowei Zhang

Anhui Gao

Siwei Wang

Yang Zhan

Boliang Li

Xichan Hu

Hui Chai

Pingzheng Zhou

Shixian Wang

Linqian Yu

Na Yang

Shimeng Guo

Chenlu Zhang

Jia Li

Cen Xie

Disclosed are a pentacyclic triterpene compound as shown in general formula (I) and a preparation method therefor. The compound has an effective antagonistic effect on FXR receptors. 

Pentacyclic triterpene compound and preparation method therefor, and pharmaceutical composition and use thereof

The invention describes an aryl-2,2'-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2&#x2032;-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs. 

Aryl-2,2'-tandem bisthiazole compound and preparation method and use thereof

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window. 

KCNQ potassium channel agonist, and preparation method therefor and use thereof

The present invention relates to a series of analogs of natural product Pyripyropene A represented by general formula I and a preparation method and use thereof. More particularly, the present invention relates to analogs of the natural product Pyripyropene A, a preparation method and use thereof as the acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors for the treatment of cardiovascular diseases such as atherosclerosis and the like. 

Tricyclic analogues, preparation method and uses thereof

KCNQ potassium channel agonists, method of preparation and method of use thereof

The present invention relates to a thiazole-based compound, a preparation method therefor, and a use thereof. More specifically, the present invention relates to a 2,2'-bis-thiazole-based compound, a preparation method therefor, and a use of 2,2&#x2032;-bis-thiazole-based compound a histone deacetylase inhibitor in the preparation of an antitumor medicament, a medicament for treating autoimmune diseases, a medicament for treating type II diabetes mellitus and complication thereof, or a medicament for treating neurodegenerative diseases. 

2,2'-tandem dithiazole compound, preparation method therefor, and use thereof

The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration. 

Compound as KCNQ potassium channel agonist, preparation method therefor and use thereof

The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase. 

Thiazole compounds, methods for preparation and use thereof

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

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Shanghai, China

Yangming Zhang