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

…, E Rickel, T Martin, A Budelsky, L Seitz, J Danao…

Index: Liu, Jiwen; Wang, Yingcai; Johnson, Michael G.; Li, An-Rong; Shen, Wang; Wang, Xuemei; Su, Yongli; Brown, Matthew; Lengerich, Bettina Van; Rickel, Erika; Martin, Tod; Budelsky, Alison; Seitz, Lisa; Danao, Jay; Tang, H. Lucy; Collins, Tassie; Medina, Julio C. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1686 - 1689

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Citation Number: 4

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.