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

Michel Gallant,Christian Beaulieu,Carl Berthelette,John Colucci,Michael A. Crackower,Chad Dalton,Danielle Denis,Yves Ducharme,Richard Friesen,Daniel Guay,Francois Gervais,Martine Hamel,Robert Houle,Connie M. Krawczyk,Birgit Kosjek,Stephen Lau,Yves Leblanc,Ernest E. Lee,Jean François Lévesque,Christophe Mellon,Carmela Molinaro,Wayne Mullet,Gary O’Neill,Paul D. 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

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

2011

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.

Keywords:

Antagonist
Immunology
Biochemistry
Pharmacology
Chemistry
In vitro
Prostaglandin D2
Respiratory system
metabolic profile
crth2 antagonist
Pharmacokinetics

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