1000416-51-2Relevant articles and documents
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility
Wang, Xianghong,Chakrabarti, Partha P.,Ognyanov, Vassil I.,Pettus, Liping H.,Tamir, Rami,Tan, Helming,Tang, Phi,Treanor, James J.S.,Gavva, Narender R.,Norman, Mark H.
, p. 6539 - 6545 (2008/09/20)
A series of trisubstituted pyrimidines were synthesized to improve aqueous solubility of our first TRPV1 clinical candidate (1; AMG 517), while maintaining potent TRPV1 inhibitory activity. Structure-activity and structure-solubility studies led to the id