1008529-50-7Relevant articles and documents
Discovery of TRPV1 antagonist ABT-116
Brown, Brian S.,Keddy, Ryan,Perner, Richard J.,DiDomenico, Stanley,Koenig, John R.,Jinkerson, Tammie K.,Hannick, Steven M.,McDonald, Heath A.,Bianchi, Bruce R.,Honore, Prisca,Puttfarcken, Pamela S.,Moreland, Robert B.,Marsh, Kennan C.,Faltynek, Connie R.,Lee, Chih-Hung
scheme or table, p. 3291 - 3294 (2010/08/07)
The synthesis and SAR of a series of indazole TRPV1 antagonists leading to the discovery of 21 (ABT-116) is described. Biological studies demonstrated potent in vitro and in vivo activity for 21, as well as suitable physicochemical and pharmacokinetic pro
METHODS FOR MAKING CENTRAL NERVOUS SYSTEM AGENTS THAT ARE TRPV1 ANTAGONISTS
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Page/Page column 41-42, (2009/10/22)
The invention discloses compounds of formula ( II ): and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.