1218918-62-7Relevant articles and documents
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases
Gallant, Michel,Beaulieu, Christian,Berthelette, Carl,Colucci, John,Crackower, Michael A.,Dalton, Chad,Denis, Danielle,Ducharme, Yves,Friesen, Richard W.,Guay, Daniel,Gervais, Franois G.,Hamel, Martine,Houle, Robert,Krawczyk, Connie M.,Kosjek, Birgit,Lau, Stephen,Leblanc, Yves,Lee, Ernest E.,Levesque, Jean-Franois,Mellon, Christophe,Molinaro, Carmela,Mullet, Wayne,O'Neill, Gary P.,O'Shea, Paul,Sawyer, Nicole,Sillaots, Susan,Simard, Daniel,Slipetz, Deborah,Stocco, Rino,S?rensen, Dan,Truong, Vouy Linh,Wong, Elizabeth,Wu, Jin,Zaghdane, Helmi,Wang, Zhaoyin
, p. 288 - 293 (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.
INDOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
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Page/Page column 17, (2010/04/25)
The compound (+) {7R-[[(4-fluorophenyl)sulfonyl](methyl)ammo]-6,7,8,9-tetrahydropyrido[1,2-a]mdol-10-yl}acetic acid and pharmaceutically acceptable salts thereof are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-meidated diseases such as asthma.