708273-57-8Relevant articles and documents
CHEMOKING RECEPTOR ANTAGONISTS
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Page/Page column 217, (2013/03/26)
Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist
Xue, Chu-Biao,Feng, Hao,Cao, Ganfeng,Huang, Taisheng,Glenn, Joseph,Anand, Rajan,Meloni, David,Zhang, Ke,Kong, Lingquan,Wang, Anlai,Zhang, Yingxin,Zheng, Changsheng,Xia, Michael,Chen, Lihua,Tanaka, Hiroyuki,Han, Qi,Robinson,Modi, Dilip,Storace, Lou,Shao, Lixin,Sharief, Vaqar,Li, Mei,Galya, Laurine G.,Covington, Maryanne,Scherle, Peggy,Diamond, Sharon,Emm, Tom,Yeleswaram, Swamy,Contel, Nancy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian
supporting information; experimental part, p. 450 - 454 (2011/08/22)
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC 50 of 4.7 nM in antagonism of c
4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANOL ANTAGONISTS OF CCR2
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Page/Page column 25, (2010/06/19)
The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).