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Discovery of AMG 853, a CRTH2 and DP Dual Antagonist #MMPMID24900313
Liu J; Li AR; Wang Y; Johnson MG; Su Y; Shen W; Wang X; Lively S; Brown M; Lai S; Gonzalez Lopez De Turiso F; Xu Q; Van Lengerich B; Schmitt M; Fu Z; Sun Y; Lawlis S; Seitz L; Danao J; Wait J; Ye Q; Tang HL; Grillo M; Collins TL; Sullivan TJ; Medina JC
ACS Med Chem Lett 2011[May]; 2 (5): 326-30 PMID24900313show ga
Prostaglandin D2 (PGD2) plays a key role in mediating allergic reactions seen in asthma, allergic rhinitis, and atopic dermatitis. PGD2 exerts its activity through two G protein-coupled receptors (GPCRs), prostanoid D receptor (DP or DP1), and chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2 or DP2). We report the optimization of a series of phenylacetic acid derivatives in an effort to improve the dual activity of AMG 009 against DP and CRTH2. These efforts led to the discovery of AMG 853 (2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenyl sulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid), which is being evaluated in human clinical trials for asthma.