2. Academic Validation
  3. Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases

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

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):288-93. doi: 10.1016/j.bmcl.2010.11.015.
Michel Gallant 1,  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
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Kirkland, Québec, Canada. [email protected]
PMID: 21106375 DOI: 10.1016/j.bmcl.2010.11.015
Abstract

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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