1287693-27-9Relevant academic research and scientific papers
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist
Zheng, Changsheng,Cao, Ganfeng,Xia, Michael,Feng, Hao,Glenn, Joseph,Anand, Rajan,Zhang, Ke,Huang, Taisheng,Wang, Anlai,Kong, Ling,Li, Mei,Galya, Laurine,Hughes, Robert O.,Devraj, Rajesh,Morton, Phillip A.,Rogier, D. Joseph,Covington, Maryanne,Baribaud, Fred,Shin, Niu,Scherle, Peggy,Diamond, Sharon,Yeleswaram, Swamy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian,Xue, Chu-Biao
, p. 1442 - 1446 (2011/04/22)
We report the discovery of a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4- (trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl] -3-methoxytetrahydro-2H-pyran-4-amine (19). After evaluation in 28-day toxicology studies, compound 19 (INCB10820/PF-4178903) was selected as a clinical candidate.
