2. Academic Validation
  3. Discovery of TRPV1 antagonist ABT-116

Discovery of TRPV1 antagonist ABT-116

  • Bioorg Med Chem Lett. 2010 Jun 1;20(11):3291-4. doi: 10.1016/j.bmcl.2010.04.047.
Brian S Brown 1,  Ryan Keddy,  Richard J Perner,  Stanley DiDomenico,  John R Koenig,  Tammie K Jinkerson,  Steven M Hannick,  Heath A McDonald,  Bruce R Bianchi,  Prisca Honore,  Pamela S Puttfarcken,  Robert B Moreland,  Kennan C Marsh,  Connie R Faltynek,  Chih-Hung Lee
Affiliations

Affiliation

  • 1 Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Dept R4PM, AP10-207, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA. [email protected]
PMID: 20457518 DOI: 10.1016/j.bmcl.2010.04.047
Abstract

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 properties for advancement to clinical development for pain management.

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