Imidazo [5, 1-f][1, 2, 4] triazin-4 (3H)-ones, a new class of potent PDE 5 inhibitors

…, T Schenke, M Es-Sayed, G Schmidt, T Lampe…

文献索引：Haning, Helmut; Niewoehner, Ulrich; Schenke, Thomas; Es-Sayed, Mazen; Schmidt, Gunter; Lampe, Thomas; Bischoff, Erwin Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 6 p. 865 - 868

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被引用次数: 56

摘要

2-aryl-substituted imidazo [5, 1-f][1, 2, 4] triazin-4 (3H)-ones represent a new class of potent cGMP-PDE 5 inhibitors that prove to be superior to other purine-isosteric inhibitors. Subnanomolar inhibitors of PDE 5 with activity in in vivo models for erectile dysfunction have been identified. BAY 38-9456 (Vardenafil-hydrochloride) has been selected for clinical studies in the indication of erectile dysfunction.