Discovery of 4-{4-[3-(Pyridin-2-yl)-1 H-pyrazol-4-yl] pyridin-2-yl}-N-(tetrahydro-2 H-pyran-4-yl) benzamide (GW788388): A Potent, Selective, and Orally Active …

…, N Mathews, VL Nguyen, C Bertho-Ruault…

文献索引：Gellibert, Francoise; De Gouville, Anne-Charlotte; Woolven, James; Mathews, Neil; Nguyen, Van-Loc; Bertho-Ruault, Cecile; Patikis, Angela; Grygielko, Eugene T.; Laping, Nicholas J.; Huet, Stephane Journal of Medicinal Chemistry, 2006 , vol. 49, # 7 p. 2210 - 2221

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被引用次数: 61

摘要

Inhibitors of transforming growth factor β (TGF-β) type I receptor (ALK5) offer a novel approach for the treatment of fibrotic diseases such as renal, hepatic, and pulmonary fibrosis. The optimization of a novel phenylpyridine pyrazole series (1a) led to the identification of potent, selective, and orally active ALK5 inhibitors. The cellular potency and pharmacokinetics profiles of these derivatives were improved and several compounds ...