Adenosine A1 modulators: a patent update (2008 to present)

Introduction: In 2008, we published our review titled 'Therapeutic potential of A1 adenosine receptor ligands - a survey of recent patent literature' that reported the compounds active on A1 adenosine receptors (ARs) and the applications of A1 AR ligands patented in the period 2005 - 2008. Areas covered: This article is a discussion of the patents about the same subjects, issued in the period 2008 to present. It is organized similarly to the first one, with a section about new compounds, subdivided on the basis of their functional activity (agonists, antagonists and allosteric modulators) and a section regarding new therapeutic applications. Expert opinion: The main novelty is represented by the patenting of A1 AR ligands with dual selectivity which may show, in some conditions, better efficacy and fewer side effects. Moreover, while the way to arrive into the market appears full of obstacles for selective A1 ligands that need systemic administration for long-term therapy, better chances are foreseen in applications requiring topical administration.