A patent review of adenosine A2B receptor antagonists (2016-present).

Beatrice Francucci, Diego Dal Ben, Catia Lambertucci, Andrea Spinaci, Rosaria Volpini, Gabriella Marucci, Michela Buccioni

Expert opinion on therapeutic patents 2022 Jun

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A2B adenosine receptor (A2BAR) plays a crucial role in pathophysiologic conditions associated with high adenosine release, typical of airway inflammatory pathologies, gastrointestinal disorders, cancer, asthma, type 2 diabetes, and atherosclerosis. In some pathologies, simultaneous inactivation of A2A and A2BARs is desirable to have a synergism of action that leads to a greater efficacy of the pharmacological treatment and less side effects due to the dose of drug administered. In this context, it is strongly required to identify molecules capable of selectively antagonizing A2BAR or A2A/A2BARs. The review provides a summary of patents, published from 2016 to present, on chemicals and their clinical use. In this paper, information on the biological activity of representative structures of recently developed A2B or A2A/A2B receptor ligands is reported. Among the four P1 receptors, A2BAR is the most inscrutable and the least studied until a few years ago, but its involvement in various inflammatory pathologies has recently made it a pharmacological target of high interest. Many efforts by the academy and pharmaceutical companies have been made to discover potential A2BAR and A2A/A2BARs drugs. Although several compounds have been synthesized only a few molecules have entered clinical trials.

Citation

Beatrice Francucci, Diego Dal Ben, Catia Lambertucci, Andrea Spinaci, Rosaria Volpini, Gabriella Marucci, Michela Buccioni. A patent review of adenosine A2B receptor antagonists (2016-present). Expert opinion on therapeutic patents. 2022 Jun;32(6):689-712