Therapeutic potential of A₁ adenosine receptor ligands: a survey of recent patent literature

Abstract

Background: In recent years, a number of companies, universities and other institutions have invested in research on new molecules acting as agonists, antagonists and enhancers on A₁ adenosine receptors (ARs) and in the evaluation of their new therapeutic applications. Objective: To review recent patenting activity on this topic. Methods: The first part of this article describes the compounds patented, subdivided by functional activity, and the second part the most relevant therapeutic applications or new uses for A₁ AR ligands, with a focus on compounds in or soon to be in clinical trials. Conclusion: Although a number of potential therapeutic applications are proposed in the recent literature, at present, in the authors' opinion, very few A₁ ligands are close to coming on the market, probably due to limited selectivity towards the target tissue or organ.

Keywords::

• A₁ adenosine receptor
• agonists
• antagonists
• asthma
• bone loss
• cardiac arrhythmia
• cardioprotection
• CNS disorders
• diabetes
• enhancers
• insulin resistance
• kidney protection
• obesity
• pain
• partial agonists
• sepsis