1621680-76-9Relevant academic research and scientific papers
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile
Blanco, Maria-Jesus,Vetman, Tatiana,Chandrasekhar, Srinivasan,Fisher, Matthew J.,Harvey, Anita,Chambers, Mark,Lin, Chaohua,Mudra, Daniel,Oskins, Jennifer,Wang, Xu-Shan,Yu, Xiao-Peng,Warshawsky, Alan M.
, p. 931 - 935 (2016)
Two new series of EP4 antagonists containing a 3-methylaryl-2-carbonyl core have been identified. One series has a 3-substituted-phenyl core, while the other one incorporates a 3-substituted pyridine. Both series led to compounds with potent activity in functional and human whole blood (hWB) assays. In the pyridine series, compound 7a was found to be a highly potent and selective EP4 antagonist, with suitable rat and dog pharmacokinetic profiles.
DIMETHYLBENZOIC ACID COMPOUNDS
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Page/Page column 15; 16, (2015/07/07)
The present invention provides a compound of the Formula I: wherein A is: and W, Y, X, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, for use as an inhibitor of the EP4 receptor.
Substituted benzamides with activity towards EP4 receptors
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Paragraph 0124-0125, (2014/08/20)
The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.
SUBSTITUTED BENZAMIDES WITH ACTIVITY TOWARDS EP4 RECEPTORS
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Page/Page column 45; 46, (2014/08/20)
The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.
