1642581-63-2Relevant academic research and scientific papers
Design and optimization of a series of 1-sulfonylpyrazolo[4,3-b ]pyridines as selective c-met inhibitors
Ma, Yuchi,Sun, Guangqiang,Chen, Danqi,Peng, Xia,Chen, Yue-Lei,Su, Yi,Ji, Yinchun,Liang, Jin,Wang, Xin,Chen, Lin,Ding, Jian,Xiong, Bing,Ai, Jing,Geng, Meiyu,Shen, Jingkang
, p. 2513 - 2529 (2015)
c-Met has emerged as an attractive target for targeted cancer therapy because of its abnormal activation in many cancer cells. To identify high potent and selective c-Met inhibitors, we started with profiling the potency and in vitro metabolic stability of a reported hit 7. By rational design, a novel sulfonylpyrazolo[4,3-b]pyridine 9 with improved DMPK properties was discovered. Further elaboration of π-π stacking interactions and solvent accessible polar moieties led to a series of highly potent and selective type I c-Met inhibitors. On the basis of in vitro and in vivo pharmacological and pharmacokinetics studies, compound 46 was selected as a preclinical candidate for further anticancer drug development.
FIVE-MEMBER-HETEROCYCLE FUSED PYRIDINE COMPOUNDS, METHOD OF PRODUCING THE SAME, AND USE THEREOF
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Paragraph 0264; 0265; 0266, (2016/06/06)
This invention provides a class of five-member-heterocycle fused pyridine compounds as shown below in Formula (X), pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, a method of producing the same, pharmaceutical compositions containing the compound, and use of the compounds in preparing medicament for preventing and/or treating diseases and tumours associated with abnormal protein tyrosine kinase.
