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Bioorg Med Chem Lett. 2011 Jan 1;21(1):288-93. doi: 10.1016/j.bmcl.2010.11.015. Epub 2010 Nov 5.

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

Author information

1
Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Kirkland, Québec, Canada. michel_gallant@videotron.ca

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.

PMID:
21106375
DOI:
10.1016/j.bmcl.2010.11.015
[Indexed for MEDLINE]

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