847728-90-9Relevant academic research and scientific papers
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
PHENOXYETHYL PIPERIDINE COMPOUNDS
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Page/Page column 9, (2014/01/17)
The present invention provides a compound of the Formula II: Formula II wherein X is: R1 is H, -CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined toge
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.
PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Page/Page column 36, (2012/06/30)
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 convalently 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 artrhritis, 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
Ortho substituted aryl or heteroaryl amide compounds
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Page/Page column 20, (2008/06/13)
This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: Z represents a hydrogen atom or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or th
SUBSTITUTED METHYL ARYL OR HETEROARYL AMIDE COMPOUNDS
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Page/Page column 33, (2008/06/13)
This invention provides a compound of the formula (I), wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 in
PHENYL OR PYRIDYL AMIDE COMPOUNDS AS PROSTAGLANDIN E2 ANTAGONISTS
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Page/Page column 65, (2015/03/06)
This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 independently represent a hydrogen atom or the li
COMBINATIONS COMPRISING ALPHA-2-DELTA LIGANDS
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Page/Page column 108-109; 173; 215-216, (2008/06/13)
The instant invention relates to a combination of an EP4-receptor antagonist and an alpha-2-delta ligand, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly inflammatory,
