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

Gang Xing, Ce Yi, Peiyuan Dou, Zhengxing Zhi, Bin Lin, Maosheng Cheng

Expert opinion on therapeutic patents 2021 Mar

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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. 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. 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.

Citation

Gang Xing, Ce Yi, Peiyuan Dou, Zhengxing Zhi, Bin Lin, Maosheng Cheng. Recent progress in the development of β2 adrenergic receptor agonists: a patent review (2015-2020). Expert opinion on therapeutic patents. 2021 Mar;31(3):239-246