1006037-08-6Relevant articles and documents
Scalable synthesis of a prostaglandin EP4 receptor antagonist
Gauvreau, Danny,Dolman, Sarah J.,Hughes, Greg,Oshea, Paul D.,Davies, Ian W.
supporting information; experimental part, p. 4078 - 4085 (2010/08/22)
The evolution of scalable, economically viable synthetic approaches to the potent and selective prostaglandin EP4 antagonist 1 is presented. The chromatography-free synthesis of multikilogram quantities of 1 using a seven-step sequence (six in the longest
The discovery of 4-{l-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]- 3thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin e2 subtype 4 receptor antagonist
Blouin, Marc,Han, Yongxin,Burch, Jason,Farand, Julie,Mellon, Christophe,Gaudreault, Mireille,Wrona, Mark,Lévesque, Jean-Fran?ois,Denis, Danielle,Mathieu, Marie-Claude,Stocco, Rino,Vigneault, Erika,Therien, Alex,Clark, Patsy,Rowland, Steve,Xu, Daigen,o'Neill, Gary,Ducharme, Yves,Friesen, Rick
experimental part, p. 2227 - 2238 (2010/08/21)
The discovery of highly potent and selective second generation EP4 antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. It also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.
PROCESS FOR MAKING THIOPHENE CARBOXAMIDE DERIVATIVE
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Page/Page column 13; 19-21, (2009/04/25)
The invention encompasses a process for making a thiophene carboxamide derivative, which is an EP4 antagonist useful for treating pain and inflammation.
THIOPHENECARBOXAMIDE DERIVATIVES AS EP4 RECEPTOR LIGANDS
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Page/Page column 76-78, (2008/06/13)
The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoi
