151276-15-2Relevant articles and documents
CXCR3 RECEPTOR AGONISTS
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Paragraph 333, (2018/03/25)
Compounds are provided having the structure of the following Formula I: where R, R1, R2, R3a and R3b are as defined herein. Pharmaceutical compositions comprising such compounds, as well as methods related to their manufacture and use, are also provided.
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors
Zhang, Peilong,Dong, Jiaqiang,Zhong, Boyu,Zhang, Deyi,Jin, Can,Meng, Xuejing,Sun, Desheng,Xu, Xiangyuan,Zhou, Yong,Liang, Zhi,Ji, Minghua,Li, Hailong,Xu, Tao,Song, Guowei,Zhang, Ling,Chen, Gang,Yuan, Hongbin,Shih, Joe,Zhang, Ruihao,Hou, Guojun,Jin, Ying,Yang, Qiong
, p. 3738 - 3743 (2015/08/06)
Abstract A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure-activity relationship of the left side-chain on phenyl substitutions were explored which delivered many potent ALK inhibitors. Among them, 29a showed favorable pharmacokinetic profiles in rats and dogs together with significant antitumor efficacy in EML4-ALK fusion xenograft model. Graphical abstract
