167414-75-7Relevant articles and documents
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels
Qu, Chunrong,Ding, Mingmin,Zhu, Yingmin,Lu, Yungang,Du, Juan,Miller, Melissa,Tian, Jinbin,Zhu, Jinmei,Xu, Jian,Wen, Meng,Er-Bu,Wang, Jule,Xiao, Yuling,Wu, Meng,McManus, Owen B.,Li, Min,Wu, Jilin,Luo, Huai-Rong,Cao, Zhengyu,Shen, Bing,Wang, Hongbo,Zhu, Michael X.,Hong, Xuechuan
, p. 4680 - 4692 (2017/06/13)
Transient receptor potential canonical 3/6/7 (TRPC3/6/7) are highly homologous receptor-operated nonselective cation channels. Despite their physiological significance, very few selective and potent agonists are available for functional examination of these channels. Using a cell-based high throughput screening approach, a lead compound with the pyrazolopyrimidine skeleton was identified as a TRPC6 agonist. Synthetic schemes for the lead and its analogues were established, and structural-activity relationship studies were carried out. A series of potent and direct agonists of TRPC3/6/7 channels were identified, and among them, 4m-4p have a potency order of TRPC3 > C7 > C6, with 4n being the most potent with an EC50 of 20 nM on TRPC3. Importantly, these compounds exhibited no stimulatory activity on related TRP channels. The potent and selective compounds described here should be suitable for evaluation of the roles of TRPC channels in the physiology and pathogenesis of diseases, including glomerulosclerosis and cancer.
TYROSINE KINASE INHIBITORS
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, (2012/12/13)
The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by
PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS
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Page 33, (2008/06/13)
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.