659731-59-6Relevant academic research and scientific papers
Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists
Stec, Markian M.,Bo, Yunxin,Chakrabarti, Partha P.,Liao, Lillian,Ncube, Mqhele,Tamayo, Nuria,Tamir, Rami,Gavva, Narender R.,Treanor, James J.S.,Norman, Mark H.
scheme or table, p. 5118 - 5122 (2009/05/07)
Clinical candidate AMG 517 (1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor solubility. Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists
Tamayo, Nuria,Liao, Hongyu,Stec, Markian M.,Wang, Xianghong,Chakrabarti, Partha,Retz, Dan,Doherty, Elizabeth M.,Surapaneni, Sekhar,Tamir, Rami,Bannon, Anthony W.,Gavva, Narender R.,Norman, Mark H.
, p. 2744 - 2757 (2008/12/22)
Transient receptor potential vanilloid 1 (TRPV1) channel antagonists may have clinical utility for the treatment of chronic nociceptive and neuropathic pain. We recently advanced a TRPV1 antagonist, 3 (AMG 517), into clinical trials as a new therapy for t
