A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present).

IF 5.4 2区医学 Q1 CHEMISTRY, MEDICINAL Expert Opinion on Therapeutic Patents Pub Date : 2024-11-04 DOI:10.1080/13543776.2024.2423010

Zhiqi Zhang, Dejuan Sun, Yueying Yang, Samir Y Abbas, Hua Li, Lixia Chen

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Abstract

Introduction: UNC-51-like kinase 1/2 (ULK1/2) are serine/threonine kinases that play a crucial role in autophagy activation and maintaining cellular homeostasis. Given their broad physiological relevance, ULK1/2 are candidate targets for treating various diseases. In recent years, ULK1/2 inhibitors have made significant progress, and the highly potent ULK1/2 inhibitors have entered clinical trials.

Area covered: This review aims to provide an updated analysis of patents describing ULK1/2 inhibitors and their potential therapeutic applications that were disclosed between 2019 and 2024.

Expert opinion: Due to their crucial role in various diseases, the invention of small-molecule drugs targeting ULK1/2 is particularly important, especially in cancer treatment. Despite the great success of ULK1/2 inhibitors development, ULK1/2 inhibitors are ATP competitive inhibitors of aminopyrimidines currently, and most ULK1/2 inhibitors are still in the preclinical research stage, with only DCC-3116 entered clinical research. Therefore, developing highly selective ULK1/2 inhibitors with low side effects and high bioavailability remains a challenging and promising research direction.

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UNC-51 样激酶 1/2抑制剂专利回顾（2019 年至今）。

简介UNC-51 样激酶 1/2（ULK1/2）是丝氨酸/苏氨酸激酶，在自噬激活和维持细胞稳态方面发挥着至关重要的作用。鉴于其广泛的生理相关性，ULK1/2 是治疗各种疾病的候选靶点。近年来，ULK1/2抑制剂的研究取得了重大进展，强效ULK1/2抑制剂已进入临床试验阶段：本综述旨在对2019年至2024年间公开的描述ULK1/2抑制剂及其潜在治疗应用的专利进行最新分析：由于ULK1/2在各种疾病中的关键作用，靶向ULK1/2的小分子药物的发明尤为重要，特别是在癌症治疗方面。尽管ULK1/2抑制剂的研发取得了巨大成功，但目前ULK1/2抑制剂是氨基嘧啶类的ATP竞争性抑制剂，大多数ULK1/2抑制剂仍处于临床前研究阶段，只有DCC-3116进入临床研究。因此，开发副作用小、生物利用度高的高选择性 ULK1/2 抑制剂仍是一个具有挑战性且前景广阔的研究方向。

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.