Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain

  • Bioorg Med Chem Lett. 2010 Jun 15;20(12):3760-3. doi: 10.1016/j.bmcl.2010.04.065.
John Colucci  1 ,  Michael Boyd ,  Carl Berthelette ,  Jean-Francois Chiasson ,  Zhaoyin Wang ,  Yves Ducharme ,  Rick Friesen ,  Mark Wrona ,  Jean-Francois Levesque ,  Danielle Denis ,  Marie-Claude Mathieu ,  Rino Stocco ,  Alex G Therien ,  Patsy Clarke ,  Steve Rowland ,  Daigen Xu ,  Yongxin Han
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Frosst Canada Ltd, Kirkland, Quebec, Canada.
PMID: 20471829 DOI: 10.1016/j.bmcl.2010.04.065
Abstract

The discovery of a highly potent and selective EP(4) antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and unprecedented in vivo potency in the rat AIA model.

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