Nurr1 modulators - a patent review (2019-present).

IF 4.6 2区医学 Q1 CHEMISTRY, MEDICINAL

Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-06-18 DOI:10.1080/13543776.2025.2516780

Markus Egner, Daniel Merk

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引用次数: 0

Abstract

Background: Nuclear receptor related 1 (Nurr1) is a ligand-activated transcription factor and considered as neuroprotective and anti-neuroinflammatory target. Several lines of evidence support potential of Nurr1 modulation in treating neurodegenerative diseases as well as in certain cancers, but potent and selective Nurr1 modulators are rare.

Areas covered: Development of small molecule Nurr1 modulators is gaining momentum which is also reflected in recent patent applications (published between 01/2019 and 09/2024, available on Google Patents). The claimed Nurr1 ligands are derived from the natural ligands prostaglandin A and dihydroxyindole as well as synthetic scaffolds. Their proposed use mainly refers to neurodegenerative disease and cancer treatment.

Expert opinion: Nurr1 modulation is emerging as new therapeutic concept in neurodegeneration and beyond and considerable progress has been made in Nurr1 ligand discovery with several promising compounds covered by patent applications. However, some reported and claimed ligands seem to lack validation and some claims appear very broad without presenting respective examples.

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Nurr1调制器-专利审查（2019年至今）。

背景：核受体相关1 （Nurr1）是一种配体激活的转录因子，被认为是神经保护和抗神经炎症的靶点。一些证据支持Nurr1调节在治疗神经退行性疾病和某些癌症方面的潜力，但有效和选择性的Nurr1调节剂很少。涵盖领域：小分子Nurr1调节剂的开发正在获得动力，这也反映在最近的专利申请中（发布于2019年1月1日至2024年9月，可在谷歌Patents上获得）。所述Nurr1配体来源于天然配体前列腺素A和二羟基吲哚以及合成支架。它们的用途主要是指神经退行性疾病和癌症的治疗。专家意见：Nurr1调节正在成为神经退行性疾病及其他领域的新治疗概念，Nurr1配体的发现取得了相当大的进展，一些有前途的化合物已被专利申请。然而，一些报道和要求的配体似乎缺乏验证，一些要求似乎非常宽泛，没有给出相应的例子。

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.