1008529-50-7Relevant academic research and scientific papers
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
Synthesis of a TRPV1 receptor antagonist
Yu, Su,Haight, Anthony,Kotecki, Brian,Wang, Lei,Lukin, Kirill,Hill, David R.
experimental part, p. 9539 - 9542 (2010/03/03)
(Chemical Equation Presented) A five-step synthesis of a TRPV1 receptor antagonist 1 is described. The key step involves a novel palladium-catalyzed amidation reaction of 4-chloro-1-methylindazole 8 with the benzyl urea 9 to form the unsymmetrically subst
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.
INDAZOLE DERIVATIVES THAT INHIBIT TRPV1 AND USES THEREOF
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Page/Page column 26-27, (2008/06/13)
Compounds of formula (I) wherein R3, R7, R9 and L are defined in the description are TRPV1 antagonists that exhibit low inhibitory activity against CYP3A4. Compositions comprising such compounds and methods for treating co
