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

  • J Med Chem. 2014 Sep 25;57(18):7550-64. doi: 10.1021/jm5003167.
Joseph B Santella 3rd  1 ,  Daniel S Gardner ,  John V Duncia ,  Hong Wu ,  Murali Dhar ,  Cullen 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 J Watson ,  Guchen Yang ,  Anne V Rose ,  Rodney D Vickery ,  Janet Caceres-Cortes ,  Christian Caporuscio ,  Daniel M Camac ,  Javed A Khan ,  Yongmi An ,  William R Foster ,  Paul Davies ,  John Hynes Jr
Affiliations
  • 1. Bristol Myers Squibb Company , P.O. Box 4000, Princeton, New Jersey 08543-4000, United States.
PMID: 25101488 DOI: 10.1021/jm5003167
Abstract

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.

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