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Discovery of a New Class of Potent, Selective, and Orally Bioavailable CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases #

✍ Scribed by Crosignani, Stefano; Page, Patrick; Missotten, Marc; Colovray, Véronique; Cleva, Christophe; Arrighi, Jean-François; Atherall, John; Macritchie, Jackie; Martin, Thierry; Humbert, Yves; Gaudet, Marilène; Pupowicz, Doris; Maio, Maurizio; Pittet, Pierre-André; Golzio, Lucia; Giachetti, Claudio; Rocha, Cynthia; Bernardinelli, Gérald; Filinchuk, Yaroslav; Scheer, Alexander; Schwarz, Matthias K.; Chollet, André


Book ID
121363802
Publisher
American Chemical Society
Year
2008
Tongue
English
Weight
717 KB
Volume
51
Category
Article
ISSN
0022-2623

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Discovery of MK-7246, a selective CRTH2
✍ Michel Gallant; Christian Beaulieu; Carl Berthelette; John Colucci; Michael A. C 📂 Article 📅 2011 🏛 Elsevier Science 🌐 English ⚖ 567 KB

In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences enabling the preparation of this novel class of CRTH2 antagonist are reported. Finally, the pharmacokinetic and metaboli