Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

Joseph B. Santella,Daniel S. Gardner,John V. Duncia,Hong Wu,Murali Dhar,Cullen L. Cavallaro,Andrew J. Tebben,Percy H. Carter,Joel C. Barrish,Melissa Yarde,Stephanie W. Briceno,Mary Ellen Cvijic,R. Robert Grafstrom,Richard Liu,Sima R. Patel,Andrew Watson,Guchen Yang,Anne Rose,Rodney Vickery,Janet Caceres Cortes,Christian Caporuscio,Daniel M. Camac,Javed Khan,Yongmi An,William R. Foster,Paul A. Davies,John Hynes

Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

2014

High-affinity, functionally potent, urea-based antagonists of CCR1 have been discovered. Modulation of PXR transactivation has revealed the selective and orally bioavailable CCR1 antagonist BMS-817399 (29), which entered clinical trials for the treatment of rheumatoid arthritis.

Keywords:

Transactivation
Pregnane X receptor
CCR1
Rheumatoid arthritis
Endocrinology
Pharmacology
Internal medicine
Chemistry
Clinical trial
Antagonist

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