Chinese Academy of Sciences

Jinan University

Shanghai Haihe Pharmaceutical Co., Ltd.

Guangzhou Eggbio Co., Ltd.

Shenzhen Newdel Biotech Co., Ltd.

Haihe Biopharma Co., Ltd.

Xiaoyun Lu

Ke Ding

Zhang Zhang

Dongmei Zhang

Jian Ding

Zhengchao Tu

Meiyu Geng

Jie Wang

Jing Ai

Xia Peng

Yinchun Ji

Xiaomei Ren

Li Tan

Zhenwei Li

Feng Jin

Yang Dai

Zhimin Zhang

Tian Wu

Zuqin Wang

Junting Wan

Xun He

Yuanyuan Cao

Shengjiang He

Shingpan Chan

Donglin Gao

Huifeng Jiang

Lina Lu

Shuang Xiang

Xiantao Zhang

Xia Tang

Shuihua Zhang

Sheng Yang

Jian Tang

Junran Gou

Yiqun Yang

Tianyu Zhang

Yuwan Liu

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

An enzyme synthesizes hydroxyl acetaldehyde and/or 1,3-dihydroxyacetone by catalyzing formaldehyde. Site-directed mutation of benzoylformate decarboxylase (BFD) creates a mutant of the enzyme, which can polymerize the formaldehyde, A phosphoketalose (F/XPK) generates acetyl phosphoric acid from the hydroxyl acetaldehyde or 1,3-dihydroxyacetone (DHA). Combination with phosphotransacetylase (Pta) provides a route from the formaldehyde to acetyl coenzyme A in three steps.

Enzyme for synthesizing hydroxyl acetaldehyde and/or 1,3-dihydroxyacetone by catalyzing formaldehyde, and applications thereof

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

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

Growing community of inventors

Guangdong, China

Xiaoyun Lu