2. Academic Validation
  3. Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis

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

Affiliation

  • 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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