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- Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).
Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).
Bioorganic & medicinal chemistry letters (2009-09-19)
Christopher J Burns, David G Bourke, Laura Andrau, Xianyong Bu, Susan A Charman, Andrew C Donohue, Emmanuelle Fantino, Michelle Farrugia, John T Feutrill, Max Joffe, Marcel R Kling, Margarita Kurek, Tracy L Nero, Thao Nguyen, James T Palmer, Ian Phillips, David M Shackleford, Harrison Sikanyika, Michelle Styles, Stephen Su, Herbert Treutlein, Jun Zeng, Andrew F Wilks
PMID19762238
摘要
A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported.
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