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
  • 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.