Discovery, Modeling, and Human Pharmacokinetics of N-(2-Acetyl-4, 6-dimethylphenyl)-3-(3, 4-dimethylisoxazol-5-ylsulfamoyl) thiophene-2-carboxamide (TBC3711), …

…, GW Holland, TA Brock, RAF Dixon

Index: Wu; Decker; Blok; Li; Bourgoyne; Bui; Keller; Knowles; Stavros; Holland; Brock; Dixon Journal of Medicinal Chemistry, 2001 , vol. 44, # 8 p. 1211 - 1216

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Citation Number: 105

Abstract

Sitaxsentan (1)(Wu et al. J. Med. Chem. 1997, 40, 1690) is our first endothelin antagonist being evaluated in clinical trials. It has demonstrated biological effects in an acute hemodynamic study in CHF (Givertz et al. Circulation 2000, 101, 2922), an open-label 20- patient pulmonary hypertension trial (Barst et al. Chest 2002, 121, 1860-1868), and a 31- patient trial in essential hypertension (Calhoun et al. AHA Scientific Sessions 2000). In a ...