Chinese Academy of Sciences

University of Michigan

The University of Texas System

Auckland Uniservices Limited

Saint Louis University

Jinan University

Shanghai Haihe Pharmaceutical Co., Ltd.

Guangzhou Institute of Biomedicine and Health

Guangzhou Eggbio Co., Ltd.

Shenzhen Newdel Biotech Co., Ltd.

Guangzhou Healthquest Pharma Co., Ltd.

Healthquest Pharma Inc.

Haihe Biopharma Co., Ltd.

Ke Ding

Zhengchao Tu

Shaomeng Wang

Guoping Wang

Xiaomei Ren

Zaneta Nikolovska-Coleska

Su Qiu

Dongguang Qin

Sanjeev Kumar

Xiaoyun Lu

Zhang Zhang

Yipin Lu

Meiyu Geng

Dongmei Zhang

Jing Min Xu

Jian Ding

Yi Chen

Rolf A Brekken

Jeffrey Bruce Smaill

Jie Wang

Jing Ai

Adam Vorn Patterson

Swarnalatha Akuratiya Gamage

Peng Li

Xia Peng

Marvin Jay Meyers

Amir Ashoorzadeh

Christopher Paul Guise

Xiaoping Chen

Duanqing Pei

Yanmei Zhang

Micky D Tortorella

Yican Wang

Yinchun Ji

Hua Xie

Li Tan

Zhenwei Li

Christopher John Squire

Yang Dai

Feng Jin

Matthew Roy Bull

Zhen Wang

Kristina Y Aguilera

Kun Luo

Zhimin Zhang

Shuang Jiang

Tianyu Zhang

Zuqin Wang

Xun He

Tian Wu

Junting Wan

Yuanyuan Cao

Shengjiang He

Shingpan Chan

Jinxi Liao

Panyu Chen

Maria Rosaria Abbattista

Donglin Gao

Chiwai Wong

Lijie Peng

Zhanfang Kang

Xi Zhou

Shuang Xiang

Jian Tang

Xia Tang

Shuihua Zhang

Xiantao Zhang

Angus Cheverton Grey

Deping Wang

Mengjie Shen

Xueqiang Li

Yubing Feng

Wei Ye

The present disclosure relates to Alkynylphenylbenzamide compounds and the applications thereof. The said Alkynylphenylbenzamide compounds have the structure shown in Formula (I). The compounds can be used as protein kinase inhibitors, which can effectively inhibit the activity of TRK protein kinase and the proliferation, migration and invasion of various tumor cells. At the same time, it has the characteristics of good pharmacokinetics and low toxicity.

Alkynylphenylbenzamide compounds and applications thereof

Fibroblast Growth Factor Receptor kinase inhibitors and prodrugs thereof of Formula (I) and their use for the treatment of hyper-proliferative diseases such as retinopathy, psoriasis, rheumatoid arthritis, osteoarthritis, septic arthritis, tumour metastasis, periodontal disease, corral ulceration, proteinuria, coronary thrombosis from atherosclerotic plaque, aneurismal aorta, dystrophobic epidermolysis bullosa, degenerative cartilage loss following traumatic joint injury, osteopenias mediated by MMP activity, tempero mandibular joint disease, and demyelating disease of the nervous system.

FGFR kinase inhibitors and pharmaceutical uses

Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.

Substituted quinolone derivatives, or pharmaceutically acceptable salts or stereoisomers thereof, and pharmaceutical compositions and use thereof

Compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in effectively inhibiting the enzymatic activity of discoidin domain receptor 1 and can be used as new therapeutic agents for preventing and treating e.g. inflammation, liver fibrosis, kidney fibrosis, lung fibrosis, skin scar, atherosclerosis, and cancer. The compound of formula I is: wherein the variables are as defined herein. 

Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof

Disclosed in the disclosure are a pyrazolo [1,5-a] pyrideine compound with structural features as shown in formula (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug molecule thereof and a use thereof. Such compounds have a good in vitro antituberculosis activity, and the minimal inhibitory concentration (MIC) of the compounds is lower than 0.1 &#x3bc;g/mL and partially achieves 0.01 &#x3bc;g/mL, and have a very strong inhibiting effect on clinically selected multi-drug resistant tuberculosis (MDR-TB) strains. In an in vivo experiment, the pyrazolo[1,5-a] pyrideine compounds of the present disclosure can effectively scavenge the infectious dose of H37Ra in a mouse body at 20 mg/kg/d does, thereby being a new type of antituberculosis compound. 

Pyrazolo[1,5-A]pyridine compounds and use thereof

Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R, R, R, R, R, X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics. 

2-aminopyrimidine compound and pharmaceutical composition and use thereof

The present invention discloses coupling compounds of a structure as shown in Formula I, II or III formed by connecting NSAID anti-inflammatory and analgesic drugs and EGFR inhibitors by ester bonds or pharmaceutically acceptable salts or stereoisomers thereof or prodrug molecules thereof: 

Coupling compounds of NSAID anti-inflammatory and analgesic drugs and EGFR kinase inhibitors, synthesis methods and applications thereof

The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.

Compositions and methods for the treatment of malaria

The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).

Small molecule inhibitors of MDM2 and the uses thereof

The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description. 

Compounds of estrogen-related receptor modulators and the uses thereof

The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec. 

Heterocyclic alkynyl benzene compounds and medical compositions and uses thereof

Process for the preparation of small molecule inhibitors of MDM2 and intermediates used therein

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Guangzhou, China

Ke Ding