946594-19-0Relevant articles and documents
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis
Santella, Joseph B.,Gardner, Daniel S.,Duncia, John V.,Wu, Hong,Dhar, Murali,Cavallaro, Cullen,Tebben, Andrew J.,Carter, Percy H.,Barrish, Joel C.,Yarde, Melissa,Briceno, Stephanie W.,Cvijic, Mary Ellen,Grafstrom, R. Robert,Liu, Richard,Patel, Sima R.,Watson, Andrew J.,Yang, Guchen,Rose, Anne V.,Vickery, Rodney D.,Caceres-Cortes, Janet,Caporuscio, Christian,Camac, Daniel M.,Khan, Javed A.,An, Yongmi,Foster, William R.,Davies, Paul,Hynes, John
, p. 7550 - 7564 (2015/02/18)
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.
The discovery of BMS-457, a potent and selective CCR1 antagonist
Gardner, Daniel S.,Santella III, Joseph B.,Duncia, John V.,Carter, Percy H.,Dhar, T.G.Murali,Wu, Hong,Guo, Weiwei,Cavallaro, Cullen,Van Kirk, Katy,Yarde, Melissa,Briceno, Stephanie W.,Robert Grafstrom,Liu, Richard,Patel, Sima R.,Tebben, Andrew J.,Camac, Dan,Khan, Javed,Watson, Andrew,Yang, Guchen,Rose, Anne,Foster, William R.,Cvijic, Mary Ellen,Davies, Paul,Hynes Jr., John
, p. 3833 - 3840 (2013/07/25)
A series of compounds which exhibited good human CCR1 binding and functional potency was modified resulting in the discovery of a novel series of high affinity, functionally potent antagonists of the CCR1 receptor. Issues of PXR activity, ion-channel pote