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

Abstract

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.

Keywords::

• A1 adenosine receptor
• A1 adenosine receptor agonists
• A1 adenosine receptor antagonists
• A1 adenosine receptor modulators
• blood–brain barrier permeability
• glaucoma
• hearing loss
• heart failure
• heart protection
• liver fibrosis
• liver steatosis
• metabolic disorders
• movement disorders
• neurodegenerative disorders
• pain
• partial agonists
• sepsis

Notes

This box summarizes key points contained in the article.