Phosphodiesterase 2 (PDE2) inhibitors: an updated patent review (2017-present).

IF 5.4 2区医学 Q1 CHEMISTRY, MEDICINAL

Expert Opinion on Therapeutic Patents Pub Date : 2024-11-01 Epub Date: 2024-10-09 DOI:10.1080/13543776.2024.2412577

Bei Zhang, Mei-Yan Jiang, Wei-Hao Luo, Chen Zhang, Yinuo Wu

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引用次数: 0

Abstract

Introduction: PDE2 is a dual-specific enzyme that hydrolyzes two intracellular substrates, cAMP and cGMP. PDE2 is mainly distributed in the brain, which indicates that PDE2 can serve as a potential target for central nervous system diseases without causing other peripheral side effects. Discovery of new mechanisms of PDE2 inhibitors is expected to bring new opportunities for the treatment of central nervous system diseases.

Area covered: This review aims to provide an overview of PDE2 inhibitors reported in patents from 2017 to present.

Expert opinion: In recent years, the development of PDE2 inhibitors and their application in the treatment of brain diseases have received much attention. The main reason is the high expression of PDE2 in the brain, which gives PDE2 a natural advantage as a research target for central nervous system diseases. This review summarizes the scaffolds of PDE2 inhibitors reported in various patents since 2017, as well as the scientific issues that need to be addressed in terms of subtype selectivity and metabolic stability, intending to provide insights for the discovery of highly active and selective PDE2 inhibitors in the future.

查看原文本刊更多论文

磷酸二酯酶 2 (PDE2) 抑制剂：最新专利回顾（2017 年至今）。

简介PDE2 是一种双特异性酶，可水解细胞内的两种底物--cAMP 和 cGMP。PDE2 主要分布在大脑中，这表明 PDE2 可作为中枢神经系统疾病的潜在靶点，且不会引起其他外周副作用。发现 PDE2 抑制剂的新机制有望为治疗中枢神经系统疾病带来新的机遇：本综述旨在概述2017年至今专利中报道的PDE2抑制剂：近年来，PDE2抑制剂的研发及其在脑疾病治疗中的应用备受关注。主要原因是PDE2在大脑中的高表达，使得PDE2作为中枢神经系统疾病的研究靶点具有天然优势。本综述总结了2017年以来各类专利中报道的PDE2抑制剂支架，以及亚型选择性和代谢稳定性等方面需要解决的科学问题，意在为未来发现高活性、高选择性的PDE2抑制剂提供启示。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Expert Opinion on Therapeutic Patents 医学-药学

CiteScore

12.10

自引率

1.50%

发文量

审稿时长

6-12 weeks

期刊介绍： Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.