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

…, J Wang, AR Bourgoyne, V Knowles…

文献索引：Wu, Chengde; Decker, E. Radford; Blok, Natalie; Bui, Huong; You, Tony J.; Wang, Junmei; Bourgoyne, Andree R.; Knowles, Vippra; Berens, Kurt L.; Holland, George W.; Brock, Tommy A.; Dixon, Richard A. F. Journal of Medicinal Chemistry, 2004 , vol. 47, # 8 p. 1969 - 1986

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被引用次数: 105

摘要

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 ...