Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists

  • Bioorg Med Chem Lett. 2012 Feb 15;22(4):1686-9. doi: 10.1016/j.bmcl.2011.12.107.
Jiwen Jim Liu  1 ,  Yingcai Wang ,  Michael G Johnson ,  An-Rong Li ,  Wang Shen ,  Xuemei Wang ,  Yongli Su ,  Matthew Brown ,  Bettina Van Lengerich ,  Erika Rickel ,  Tod Martin ,  Alison Budelsky ,  Lisa Seitz ,  Jay Danao ,  H Lucy Tang ,  Tassie Collins ,  Julio C Medina
Affiliations
  • 1. Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. [email protected]
PMID: 22264478 DOI: 10.1016/j.bmcl.2011.12.107
Abstract

Our first generation CRTH2 and DP dual antagonists, represented by AMG 009, are more potent toward the CRTH2 receptor than to the DP receptor. Here we report our efforts in the discovery of CRTH2 and DP dual antagonists with more balanced potencies to both receptors, such as compound 15.