Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-((trans-4-hydroxycyclohexyl)amino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl) pyrido(3,4-b)pyrazin-2(1H)-one.

摘要

We describe efforts to improve the pharmacokinetic profile of the aminopyridopyrazinone class of PDE5 inhibitors. These efforts led to the discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl) pyrido[3,4-b]pyrazin-2(1H)-one, a potent and selective inhibitor of PDE5 with an excellent PK profile.