John Michael Janusz

Selective Kv1.5 Blockers: Development of (R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl)-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a Potential Treatment for Atrial Arrhythmia

Atrial fibrillation is the most prevalent form of cardiac arrhythmia. Current treatments extend the atrial effective refractory period by nonselective blockade of cardiac ion channels. An alternative approach selectively targeting the Kv1.5 ion channel offers the opportunity for therapeutic benefit with decreased risk of adverse cardiovascular events. KVI-020 (4g) successfully demonstrated antiarrhythmic efficacy in a canine arrhythmia model, and these findings support its utility as an antiarrhythmic agent.

Solid-phase synthesis of 3-aminohydantoin, dihydrouracil, thiohydantoin and dihydrothiouracil derivatives

Abstract An efficient and convenient route to 3-aminohydantoins and dihydrouracils using solid-phase chemistry has been developed. This methodology has the advantage of generality and diversity over solution-phase chemistry for the preparation of 3-aminohydantoins and dihydrouracils.

An efficient one-pot synthesis of 3-aminohydantoin and 3-aminodihydrouracil derivatives

Abstract An efficient one-pot synthesis of 3-aminohydantoin and 3-aminodihydrouracil derivatives is described. This methodology provides a simple, straightforward and versatile synthetic route to these interesting classes of heterocycles.