Chinese Academy of Sciences

University of Texas System

Auckland Uniservices Limited

Jinan University

Shanghai Haihe Pharmaceutical Co., Ltd.

Guangzhou Institute of Biomedicine and Health

Guangzhou Eggbio Co., Ltd.

Shenzhen Newdel Biotech Co., Ltd.

Haihe Biopharma Co., Ltd.

Zhengchao Tu

Ke Ding

Xiaomei Ren

John Jeffrey Talley

Xin Lu

Yan Chen

Xiaorong Liu

Yanmei Zhang

Micky D Tortorella

Jianqi Liu

Yican Wang

Xiaoyun Lu

Mark G Obukowicz

Meiyu Geng

Zhang Zhang

Dongmei Zhang

Jian Ding

Yi Chen

Rolf A Brekken

Jeffrey Bruce Smaill

Jie Wang

Adam Vorn Patterson

Jing Ai

Swarnalatha Akuratiya Gamage

Xia Peng

Amir Ashoorzadeh

Christopher Paul Guise

Yinchun Ji

Hua Xie

Li Tan

Zhenwei Li

Zhen Wang

Yang Dai

Feng Jin

Christopher John Squire

Matthew Roy Bull

Angus Cheverton Grey

Kristina Y Aguilera

Xueqiang Li

Jian Tang

Tianyu Zhang

Xiantao Zhang

Tian Wu

Shuang Jiang

Junting Wan

Yuanyuan Cao

Shengjiang He

Shingpan Chan

Shuang Xiang

Zhimin Zhang

Xia Tang

Donglin Gao

Zuqin Wang

Shuihua Zhang

Xun He

Maria Rosaria Abbattista

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 deuterated benzopyran compounds having structure features as shown in Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or prodrug molecules thereof. With excellent anti-inflammatory and analgesic effects and the capability to inhibit growth of tumor cells, such compounds are novel COX-2 selective inhibitors. The compounds and pharmaceutically acceptable salts thereof disclosed by the present application can be applied in preparing anti-inflammatory and analgesic drugs and drugs for treating or preventing tumors. 

Deuterated benzopyran compounds and the use in the treatment of pain and inflammation

Deuterated benzopyran compounds and application thereof

Growing community of inventors

Guangdong, China

Zhengchao Tu