Pyrazolopyrimidinone derivatives conjugated to thiophene moieties or benzo Ýfused¨ 5-membered heterocycles for erectile dysfunction

摘要

There is disclosed a genus of substituted pyrazolopyrimidinones characterized, in part, by multiply substituted thiophene moieties and, in part, a genus of substituted bicyclic heteroaryl appendages. The compounds are potent inhibitors of phosphodiesterases, particularly cyclic guanosine 3',5'-monophosphate (cGMP) phosphodiesterase (PDE) activity (aka cGMP-PDE) and are useful for a variety of cardiovascular disorders relating to vascular patency, such as erectile dysfunction. Specifically, a selected set of [benzo]-fused heterocycles includes benzofuran, benzoazole, benzo[d]isoxazole, their 2,3-dihydro analogs, and benzo-1,3-dioxole moieties.