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用于治疗糖尿病并发症的醛糖还原酶抑制作用的挑战:专利文献 2019-2023 年更新。

The challenging inhibition of Aldose Reductase for the treatment of diabetic complications: a 2019-2023 update of the patent literature.

机构信息

Department of Pharmacy, University of Pisa, Pisa, Italy.

出版信息

Expert Opin Ther Pat. 2024 Nov;34(11):1085-1103. doi: 10.1080/13543776.2024.2412573. Epub 2024 Oct 11.

DOI:10.1080/13543776.2024.2412573
PMID:39365044
Abstract

INTRODUCTION

Aldose reductase (AKR1B1, EC: 1.1.1.21) is a recognized target for the treatment of long-term diabetic complications since its activation in hyperglycemia and role in the polyol pathway. In particular, the tissue-specificity of AKR1B1 expression makes the design of the traditional Aldose Reductase Inhibitors (ARIs) and the more recent Aldose Reductase Differential Inhibitors (ARDIs) exploitable strategies to treat pathologies resulting from diabetic conditions.

AREAS COVERED

A brief overview of the roles and functions of AKR1B1 along with known ARIs and ARDIs was provided. Then, the design of the latest inhibitors in the scientific scenario was discussed, aiming at introducing the research achievement in the field of intellectual properties. Patents dealing with AKR1B1 and diabetes filed in the 2019-2023 period were collected and analyzed. Reaxys, Espacenet, SciFinder, and Google Patents were surveyed, using 'aldose reductase' and 'inhibitor' as the reference keywords. The search results were then filtered by PRISMA protocol, thus obtaining 16 records to review.

EXPERT OPINION

Although fewer in number than in the early 2000s, patent applications are still being filed in the field of ARIs, with a large number of Chinese inventors reporting new synthetic ARIs in favor of the repositioning approach.

摘要

简介

醛糖还原酶(AKR1B1,EC:1.1.1.21)是治疗长期糖尿病并发症的公认靶点,因为它在高血糖中的激活作用及其在多元醇途径中的作用。特别是,AKR1B1 表达的组织特异性使得传统醛糖还原酶抑制剂(ARIs)和最近的醛糖还原酶差异抑制剂(ARDIs)的设计成为治疗糖尿病引起的病理的可行策略。

涵盖领域

简要概述了 AKR1B1 的作用和功能,以及已知的 ARIs 和 ARDIs。然后,讨论了科学领域中最新抑制剂的设计,旨在介绍知识产权领域的研究成果。收集并分析了 2019-2023 年期间与 AKR1B1 和糖尿病相关的专利。使用“醛糖还原酶”和“抑制剂”作为参考关键字,在 Reaxys、Espacenet、SciFinder 和 Google Patents 上进行了调查。然后,根据 PRISMA 协议对搜索结果进行了过滤,从而获得了 16 条记录进行审查。

专家意见

尽管与 21 世纪初相比,ARIs 领域的专利申请数量较少,但仍有大量中国发明人报告了新的合成 ARIs,支持重新定位方法。

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The challenging inhibition of Aldose Reductase for the treatment of diabetic complications: a 2019-2023 update of the patent literature.用于治疗糖尿病并发症的醛糖还原酶抑制作用的挑战:专利文献 2019-2023 年更新。
Expert Opin Ther Pat. 2024 Nov;34(11):1085-1103. doi: 10.1080/13543776.2024.2412573. Epub 2024 Oct 11.
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Acid Derivatives of Pyrazolo[1,5-a]pyrimidine as Aldose Reductase Differential Inhibitors.吡唑并[1,5-a]嘧啶的酸衍生物作为醛糖还原酶的差向抑制剂。
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