1064195-77-2Relevant academic research and scientific papers
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor
Burch, Jason D.,Farand, Julie,Colucci, John,Sturino, Claudio,Ducharme, Yves,Friesen, Richard W.,Lévesque, Jean-Fran?ois,Gagné, Sébastien,Wrona, Mark,Therien, Alex G.,Mathieu, Marie-Claude,Denis, Danielle,Vigneault, Erika,Xu, Daigen,Clark, Patsy,Rowland, Steve,Han, Yongxin
, p. 1041 - 1046 (2011/03/21)
Two new series of EP4 antagonists based on naphthalene/quinoline scaffolds have been identified as part of our on-going efforts to develop treatments for inflammatory pain. One series contains an acidic sulfonylurea pharmacophore, whereas the other is a neutral amide. Both series show subnanomolar intrinsic binding potency towards the EP4 receptor, and excellent selectivity towards other prostanoid receptors. While the amide series generally displays poor pharmacokinetic parameters, the sulfonylureas exhibit greatly improved profile. MF-592, the optimal compound from the sulfonylurea series, has a desirable overall preclinical profile that suggests it is suitable for further development.
NAPHTHALENE AND QUINOLINE SULFONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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, (2008/12/04)
The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
