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引用次数: 0
摘要
神经炎症与阿尔茨海默病(AD)、肌萎缩性侧索硬化症(ALS)、多发性硬化症(MS)、亨廷顿病(HD)和帕金森病(PD)等神经退行性疾病相关。近年来,许多研究和专利都集中在设计和合成花生四烯酸脂氧合酶(ALOX)抑制剂,用于治疗神经退行性疾病。涵盖领域:该调查涵盖了天然产物、合成、杂交以及作为ALOX抑制剂在生物学研究中的生物效应评估。本文对2018年至今的专利出版物进行了调查,这些出版物取自b谷歌Scholar、Espanet、Web of Science、Drugbank、Scopus或PubMed。专家意见:作者建议(i)需要考虑生物学-药理学的许多领域:选择性、体内研究、毒性、生物利用度和药物相似性、在不同动物和人类中的作用机制、评价更有效和更有选择性的生物学试验;(ii)合成方法在发现和生产具有更高选择性的ALOX抑制剂方面优于其他方法。几种ALOX抑制剂在治疗神经系统疾病方面显示出有希望的结果。它们的临床评价将是评估治疗效果的关键。作用机制和生物利用度明确的化合物可作为治疗神经退行性疾病的先导化合物。
"A patent review on arachidonic acid lipoxygenase (LOX) inhibitors for the treatment of neurodegenerative diseases (2018-present)".
Introduction: Neuroinflammation is correlated to neurodegenerative diseases like Alzheimer's disease (AD), Amyotrophic Lateral Sclerosis (ALS), Multiple Sclerosis (MS), Huntington Disease (HD), and Parkinson's disease (PD). A lot of recent research and patents are focused on the design and synthesis of arachidonic acid lipoxygenase (ALOX) inhibitors for the treatment of neurodegenerative diseases.
Areas covered: The survey covers natural products, synthesis, hybrids, and assessments of biological effects in biological studies as ALOX inhibitors. A survey of patent publications from 2018 to present, taken from Google Scholar, Espanet, Web of Science, Drugbank, Scopus, or PubMed is analyzed.
Expert opinion: The authors suggest that (i) numerous areas of biology-pharmacology need to be considered: selectivity, in vivo studies, toxicity, bioavailability, and drug-likeness, the mechanism of action in different animals and humans, evaluation of more efficient and selective biological tests; (ii) synthetic method outbalance in the discovery and production of ALOX inhibitors with greater selectivity. Several ALOX inhibitors show promising results for the treatment of neurological disorders. Their clinical evaluation will be critical to assess therapeutic utility. The compounds for which the mechanism of action and their bioavailability are well defined can be used as lead compounds for the treatment of neurodegenerative diseases.
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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