659731-60-9Relevant academic research and scientific papers
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
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
