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

  • Bioorg Med Chem Lett. 2002 Mar 25;12(6):865-8. doi: 10.1016/s0960-894x(02)00030-6.
Helmut Haning  1 ,  Ulrich Niewöhner ,  Thomas Schenke ,  Mazen Es-Sayed ,  Gunter Schmidt ,  Thomas Lampe ,  Erwin Bischoff
Affiliations
  • 1. Department of Medicinal Chemistry, BAYER AG, Business Group Pharma, D-42096, Wuppertal, Germany. [email protected]
PMID: 11958981 DOI: 10.1016/s0960-894x(02)00030-6
Abstract

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.

Products