3,4-Disubstituted indole acylsulfonamides: A novel series of potent and selective human EP3 receptor antagonists
A series of potent and selective EP3 receptor antagonists are described. Utilizing a pharmacophore model developed for the EP3 receptor, a series of 3,4-disubstituted indoles were shown to be high affinity ligands for this target. These compounds showed high selectivity over IP, FP and other EP receptors and are potent antagonists in functional assays.
Zhou, Nian,Zeller, Wayne,Krohn, Michael,Anderson, Herb,Zhang, Jun,Onua, Emmanuel,Kiselyov, Alex S.,Ramirez, Jose,Halldorsdottir, Gudrun,Andresson, Thorkell,Gurney, Mark E.,Singh, Jasbir
scheme or table
p. 123 - 126
(2009/04/16)
Sulfonamide peri-substituted bicyclics for occlusive artery disease
Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
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Page/Page column 81
(2008/06/13)
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