{"title":"UNC-51 样激酶 1/2抑制剂专利回顾(2019 年至今)。","authors":"Zhiqi Zhang, Dejuan Sun, Yueying Yang, Samir Y Abbas, Hua Li, Lixia Chen","doi":"10.1080/13543776.2024.2423010","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>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.</p><p><strong>Area covered: </strong>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.</p><p><strong>Expert opinion: </strong>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.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4000,"publicationDate":"2024-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present).\",\"authors\":\"Zhiqi Zhang, Dejuan Sun, Yueying Yang, Samir Y Abbas, Hua Li, Lixia Chen\",\"doi\":\"10.1080/13543776.2024.2423010\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>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.</p><p><strong>Area covered: </strong>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.</p><p><strong>Expert opinion: </strong>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.</p>\",\"PeriodicalId\":12314,\"journal\":{\"name\":\"Expert Opinion on Therapeutic Patents\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":5.4000,\"publicationDate\":\"2024-11-04\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Expert Opinion on Therapeutic Patents\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/13543776.2024.2423010\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Expert Opinion on Therapeutic Patents","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/13543776.2024.2423010","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present).
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.
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
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