Department of Medicinal Chemistry, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang China.
Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang China.
Expert Opin Ther Pat. 2021 Mar;31(3):239-246. doi: 10.1080/13543776.2021.1865312. Epub 2020 Dec 23.
The β adrenergic receptor (βAR) 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 βAR 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 βAR agonists over the past 5 years.
This review offers an update for the development of βAR 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 β adrenergic receptor agonist activity are reviewed.
βAR 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 βAR 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.
β肾上腺素能受体(βAR)是 G 蛋白偶联受体(GPCR)的成员,介导大多数细胞对外界刺激的反应。激动剂可引起平滑肌松弛;因此,许多βAR 激动剂已被开发出来,特别是用于治疗哮喘和慢性阻塞性肺疾病(COPD)等肺部疾病。在过去的 5 年中,许多新的天然和合成化合物已被发现并开发为新型βAR 激动剂。
本综述提供了 2015 年至 2020 年期间发表的专利中βAR 激动剂开发的最新情况,包括用于治疗哮喘和 COPD 的新天然和合成化合物。特别综述了具有毒蕈碱受体拮抗剂和β肾上腺素能受体激动剂活性的化合物的最新专利。
βAR 激动剂已广泛开发用于治疗哮喘和 COPD。在过去的 5 年中,天然来源和合成方法的新型激动剂得到了深入开发。同时具有毒蕈碱受体拮抗剂和βAR 激动剂活性的化合物代表了该领域的一个新趋势,因为它们可能能够以协同方式一起发挥作用,从而通过两种不同的机制缓解患者的症状。