872592-39-7Relevant 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
scheme or table, 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.
3-AMINOCYCLOPENTANECARBOXAMIDES AS MODULATORS OF CHEMOKINE RECEPTORS
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Page/Page column 23, (2008/06/13)
The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
