Chinese Academy of Sciences

Shanghai Fochon Pharmaceutical Co., Ltd.

Shanghai Haihe Pharmaceutical Co., Ltd.

Tongji University

Jinan University

Haihe Biopharma Co., Ltd.

Jing Ai

Hongbin Liu

Meiyu Geng

Jian Ding

Xia Peng

Weibo Wang

Xingdong Zhao

Haohan Tan

Ling Chen

Weipeng Zhang

Qiang Tian

Jian Li

Yang Liu

Wei Zhang

Zhang Zhang

Dongmei Zhang

Xin Wang

Yinchun Ji

Min Huang

Lei Liu

Jia Tao Li

Qi Rong Wang

Yi Chen

Hualiang Jiang

Tao Tao

Kaixian Chen

Lei Jiang

Jingkang Shen

Ke Ding

Tao Meng

Zhengchao Tu

Ao Zhang

Lanping Ma

Zilan Song

Youhong Hu

Xiaoyun Lu

Li Tan

Xiaomei Ren

Jianhua Cao

Bing Xiong

Yi Zang

Li Xing

Yu Zhou

Xun Huang

Hexiang Yan

Wenhu Duan

Hong Liu

Shuping Li

Limin Zeng

Danqi Chen

Kunlun Xin

Qian Tan

Yang Dai

Yaqiu Long

Hefeng Zhang

Feifei Fang

Wangting Gu

Kui Zhang

Wenming Ren

Xiaocong Guan

Lang Wang

Zhongliang Xu

Chuantao Zha

Ying Dong

Yuelei Chen

Donglin Gao

Shingpan Chan

Yuchi Ma

Qi Wang

Provided are a class of fused-cyclic pyrazolone formamide compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided is a compound having the structure as shown in formula (I) (with each group defined in the description). The compound can be used as an AXL inhibitor in the preparation of a pharmaceutical composition for treating tumors.

Fused-cyclic pyrazolone formamide compound and preparation method therefor, pharmaceutical composition and use thereof

A compound having Axl and c-Met kinase inhibitory activity, a preparation method therefor and an application thereof are provided. Specifically, provided herein are a compound having the structure represented by formula (I), a preparation method therefor and an application thereof in the preparation of a medication for the treatment and/or prevention of tumor-associated diseases and/or kinase-related diseases.

Compound having Axl and c-Met kinase inhibitory activity, preparation thereof and application thereof

Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.

Substituted amino six-membered nitric heterocyclic ring compound and preparation and use thereof

The present disclosure relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present disclosure are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumors and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present disclosure are a preparation method for the compound shown in formula I, and a use thereof. 

Fused ring pyrimidine amino compound and preparation method, pharmaceutical composition, and use thereof

The present invention relates to a method for acquiring the water leakage amount of a leakage area in a water distribution system. In the method, a hydraulic model is coupled with monitored data, and the water leakage amounts of different areas in the water distribution system are obtained through inversion by optimizing the spatial distribution of water leakage amounts. In addition to the coupling of the hydraulic model with the monitored data, virtual sectorization and pipe leakage risk assessment are used. By using a minimum difference between a simulated value and a monitored value at a pressure measurement point as a target, the water leakage amounts of different areas in the water distribution system are calculated by an optimization algorithm. Compared with the prior art, the present invention actualizes the effective identification of leakage areas in a water distribution system with a high leakage rate (i.e., with many leakage points).

Method for acquiring water leakage amount of leakage area in water distribution system

An o-aminoheteroaryl alkynyl-containing compound has a structure represented by formula (I), and the compound of formula (I) has advantages of a high FGFR and RET double target inhibitory activity and a relatively low KDR activity, and the compound of formula (I) exhibits a strong inhibitory activity in a human lung cancer cell line NCI-H1581 and a gastric cancer cell line SNU16 as well as an RET-dependent sensitive cell line BaF3-CCDC6-Ret and a mutant thereof. Pharmacokinetic data shows that the o-aminoheteroaryl alkynyl-containing compound has druggability, and exhibits significant relevant inhibition of the growth of related tumors in a long-term animal model of drug efficacy and results in favorable animal condition at effective doses. 

O-aminoheteroaryl alkynyl-containing compound, preparation method therefor, and use thereof

The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase. 

Pyrido-azaheterecydic compound and preparation method and use 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

The present invention provides an indazole compound as a FGFR kinase inhibitor, preparation and use thereof. Specifically, the present invention provides a compound represented by formula (I), wherein the definitions of each group are described in the specification. The compound of the present invention has good FGFR kinase-inhibiting activity, and can be used in preparing a series of medicines for treating FGFR kinase activity related diseases. 

Indazole compounds as FGFR kinase inhibitor, preparation and use thereof

A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerizing factor activity inhibitors and actin-aggregation inhibitors.

Sulfated polygulonic acid polysaccharide or pharmaceutical salt thereof, preparation method therefor and use thereof

Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.

Certain protein kinase inhibitors

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Shanghai, China

Jing Ai