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Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases

✍ Scribed by Michel Gallant; Christian Beaulieu; Carl Berthelette; John Colucci; Michael A. Crackower; Chad Dalton; Danielle Denis; Yves Ducharme; Richard W. Friesen; Daniel Guay; François G. Gervais; Martine Hamel; Robert Houle; Connie M. Krawczyk; Birgit Kosjek; Stephen Lau; Yves Leblanc; Ernest E. Lee; Jean-François Levesque; Christophe Mellon; Carmela Molinaro; Wayne Mullet; Gary P. O’Neill; Paul O’Shea; Nicole Sawyer; Susan Sillaots; Daniel Simard; Deborah Slipetz; Rino Stocco; Dan Sørensen; Vouy Linh Truong; Elizabeth Wong; Jin Wu; Helmi Zaghdane; Zhaoyin Wang

Book ID: 104005096
Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 567 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.11.015

No coin nor oath required. For personal study only.

✦ Synopsis

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 metabolic profile of MK-7246 is disclosed.

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