2. Academic Validation
  3. Discovery and optimization of CRTH2 and DP dual antagonists

Discovery and optimization of CRTH2 and DP dual antagonists

  • Bioorg Med Chem Lett. 2009 Nov 15;19(22):6419-23. doi: 10.1016/j.bmcl.2009.09.052.
Jiwen Liu 1,  Zice Fu,  Yingcai Wang,  Mike Schmitt,  Alan Huang,  Derek Marshall,  George Tonn,  Lisa Seitz,  Tim Sullivan,  H Lucy Tang,  Tassie Collins,  Julio Medina
Affiliations

Affiliation

  • 1 Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jiwenl@amgen.com
PMID: 19804971 DOI: 10.1016/j.bmcl.2009.09.052
Abstract

A series of phenylacetic acid derivatives was discovered as CRTH2 antagonists. Modification of the series led to compounds that are also antagonists of DP. Since activation of CRTH2 and DP are believed to play key roles in mediating responses of asthma and other immune diseases, this series was optimized to increase the dual antagonistic activities and improve pharmacokinetic properties. These efforts led to selection of AMG 009 as a clinical candidate.

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