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腺苷受体拮抗剂和激动剂的治疗潜力。

Therapeutic potential of adenosine receptor antagonists and agonists.

机构信息

Novartis Institutes for Biomedical Research, Wimblehurst Road, Horsham, West Sussex, RH12 5AB, UK.

出版信息

Expert Opin Ther Pat. 2007 Aug;17(8):979-91. doi: 10.1517/13543776.17.8.979.

Abstract

The adenosine receptors (A(1), A(2A), A(2B) and A(3)) are important and ubiquitous mediators of cellular signalling, which play vital roles in protecting tissues and organs from damage. Launched drugs include the adenosine receptor antagonists theophylline and doxofylline (both used as bronchodilators in respiratory disorders such as asthma), while several compounds are presently in clinical trials for a range of indications, including heart failure, Parkinson's disease, rheumatoid arthritis, cancer, pain and chronic obstructive pulmonary disease. A host of companies and institutions are addressing the huge potential for the development of selective adenosine receptor agonists and antagonists, so that it appears we are on the verge of a new wave of compounds approaching the market for many unmet medical needs. This review presents an analysis of the patenting activity in the area for 2006 and an interpretation and reflection on the developments that we can expect in the future.

摘要

腺苷受体(A(1)、A(2A)、A(2B)和 A(3))是细胞信号转导的重要和普遍的介质,在保护组织和器官免受损伤方面发挥着重要作用。已上市的药物包括腺苷受体拮抗剂茶碱和多索茶碱(两者均用作哮喘等呼吸道疾病的支气管扩张剂),而目前有多种化合物正在进行临床试验,用于治疗多种适应症,包括心力衰竭、帕金森病、类风湿性关节炎、癌症、疼痛和慢性阻塞性肺疾病。许多公司和机构正在关注开发选择性腺苷受体激动剂和拮抗剂的巨大潜力,因此,我们似乎即将迎来一波新的化合物进入市场,以满足许多未满足的医疗需求。本文对 2006 年该领域的专利活动进行了分析,并对未来的发展进行了解释和思考。

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