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Discovery of MK-3697: A selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia

โœ Scribed by Roecker, Anthony J.; Reger, Thomas S.; Mattern, M. Christa; Mercer, Swati P.; Bergman, Jeffrey M.; Schreier, John D.; Cube, Rowena V.; Cox, Christopher D.; Li, Dansu; Lemaire, Wei; Bruno, Joseph G.; Harrell, C. Meacham; Garson, Susan L.; Gotter, Anthony L.; Fox, Steven V.; Stevens, Joanne; Tannenbaum, Pamela L.; Prueksaritanont, Thomayant; Cabalu, Tamara D.; Cui, Donghui; Stellabott, Joyce; Hartman, George D.; Young, Steven D.; Winrow, Christopher J.; Renger, John J.; Coleman, Paul J.


Book ID
127318198
Publisher
Elsevier Science
Year
2014
Tongue
English
Weight
503 KB
Volume
24
Category
Article
ISSN
0960-894X

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Discovery of MK-7246, a selective CRTH2
โœ Michel Gallant; Christian Beaulieu; Carl Berthelette; John Colucci; Michael A. C ๐Ÿ“‚ Article ๐Ÿ“… 2011 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 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