847728-90-9Relevant articles and documents
Discovery and characterization of a potent and selective EP4 receptor antagonist
Schiffler, Matthew A.,Chandrasekhar, Srinivasan,Fisher, Matthew J.,Harvey, Anita,Kuklish, Steven L.,Wang, Xu-Shan,Warshawsky, Alan M.,York, Jeremy S.,Yu, Xiao-Peng
, p. 3176 - 3178 (2015/07/08)
Abstract EP4 is a prostaglandin E2 receptor that is a target for potential anti-nociceptive therapy. Described herein is a class of amphoteric EP4 antagonists which reverses PGE2-induced suppression of TNFα prod
PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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, (2013/10/08)
The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(═N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, endometriosis and migraine.
A novel series of potent and selective EP4 receptor ligands: Facile modulation of agonism and antagonism
Boyd, Michael J.,Berthelette, Carl,Chiasson, Jean-Franois,Clark, Patsy,Colucci, John,Denis, Danielle,Han, Yongxin,Lévesque, Jean-Francois,Mathieu, Marie-Claude,Stocco, Rino,Therien, Alex,Rowland, Steve,Wrona, Mark,Xu, Daigen
scheme or table, p. 484 - 487 (2011/02/27)
A novel series of EP4 ligands, based on a benzyl indoline scaffold, has been discovered. It was found that agonism and antagonism in this series can be easily modulated by minor modifications on the benzyl group. The pharmacokinetic, metabolic