915192-29-9Relevant academic research and scientific papers
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP4 receptor
Burch, Jason D.,Belley, Michel,Fortin, Rejean,Deschenes, Denis,Girard, Mario,Colucci, John,Farand, Julie,Therien, Alex G.,Mathieu, Marie-Claude,Denis, Danielle,Vigneault, Erika,Levesque, Jean-Francois,Gagne, Sebastien,Wrona, Mark,Xu, Daigen,Clark, Patsy,Rowland, Steve,Han, Yongxin
, p. 2048 - 2054 (2008/12/20)
A new series of EP4 antagonists based on a quinoline acylsulfonamide scaffold have been identified as part of our on-going efforts to develop treatments for chronic inflammation. These compounds show subnanomolar intrinsic binding potency towar
QUINOLINE DERIVATIVES AS EP4 ANTAGONISTS
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Page/Page column 18; 22, (2008/06/13)
The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom., a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.
