- CHEMOKING RECEPTOR ANTAGONISTS
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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.
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Page/Page column 217
(2013/03/26)
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- Discovery of a 4-Azetidinyl-1-thiazoyl-cyclohexane CCR2 antagonist as a development candidate
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We have discovered a novel series of 4-Azetidinyl-1-Aryl-cyclohexanes as CCR2 antagonists. Divergent SAR studies on hCCR2 and hERG activities led to the discovery of compound 8d, which displayed good hCCR2 binding affinity (IC 50, 37 nM) and po
- Zhang, Xuqing,Hou, Cuifen,Hufnagel, Heather,Singer, Monica,Opas, Evan,McKenney, Sandra,Johnson, Dana,Sui, Zhihua
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p. 1039 - 1044
(2013/02/23)
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- CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I). Wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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Page/Page column 145-146
(2012/01/06)
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- Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist
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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
- 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
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p. 450 - 454
(2011/08/22)
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- 4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANOL ANTAGONISTS OF CCR2
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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).
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Page/Page column 25
(2010/06/19)
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- 4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANE ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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Page/Page column 37-38
(2010/11/03)
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