Recent progress in the development of β2 adrenergic receptor agonists: a patent review (2015-2020)

Abstract

Introduction: The β₂ adrenergic receptor (β₂AR) is a member of G protein-coupled receptors (GPCRs) that mediate the majority of cellular responses to external stimuli. The agonists can cause smooth muscle relaxation; therefore, many β₂AR agonists have been developed especially for the treatment of pulmonary disorders such as asthma and chronic obstructive pulmonary disease (COPD). Many new natural and synthetic compounds have been discovered and developed as novel β₂AR agonists over the past 5 years.

Areas covered: This review offers an update for the development of β₂AR agonists in the patents published from 2015 to 2020, including new natural and synthetic compounds for the treatment of asthma and COPD. In particular, the latest patents about compounds possessing both muscarinic receptor antagonist and β₂ adrenergic receptor agonist activity are reviewed.

Expert opinion: β₂AR agonists have been developed extensively for the treatment of asthma and COPD. In the past 5 years, novel agonists from both natural sources and synthetic methods were intensively developed. Compounds possessing both muscarinic receptor antagonist and β₂AR agonist activity represent a new trend in this area because they are possibly able to act together in a synergistic fashion, therefore, relieve the symptoms of patients through two distinct mechanisms.

Keywords: asthma; chronic obstructive pulmonary disease (COPD); Β2 adrenergic receptors (β2AR); β2AR agonists.