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专利视角下的人中性粒细胞弹性蛋白酶(HNE)抑制剂(2014-2018 年)及其治疗应用。

A patenting perspective on human neutrophil elastase (HNE) inhibitors (2014-2018) and their therapeutic applications.

机构信息

a Department of NEUROFARBA, Pharmaceutical and Nutraceutical Section , University of Florence , Florence , Italy.

b Department of Microbiology and Immunology , Montana State University , Bozeman , MT , USA.

出版信息

Expert Opin Ther Pat. 2019 Jul;29(7):555-578. doi: 10.1080/13543776.2019.1630379. Epub 2019 Jun 16.

Abstract

INTRODUCTION

Human neutrophil elastase (HNE) is involved in a variety of serious chronic diseases, especially cardiopulmonary pathologies. For this reason, the regulation of HNE activity represents a promising therapeutic approach, which is evident by the development of a number of new and selective HNE inhibitors, both in the academic and pharmaceutical environments.

AREAS COVERED

The present review analyzes and summarizes the patent literature regarding human neutrophil elastase inhibitors for the treatment of cardiopulmonary diseases over 2014-2018.

EXPERT OPINION

HNE is an interesting and defined target to treat various inflammatory diseases, including a number of cardiopulmonary pathologies. The research in this field is quite active, and a number of HNE inhibitors are currently in various stages of clinical development. In addition, new opportunities for HNE inhibitor development stem from recent studies demonstrating the involvement of HNE in many other inflammatory pathologies, including rheumatoid arthritis, inflammatory bowel disease, skin diseases, and cancer. Furthermore, the development of dual HNE/proteinase 3 inhibitors is being pursued as an innovative approach for the treatment of neutrophilic inflammatory diseases. Thus, these new developments will likely stimulate new and increased interest in this important therapeutic target and for the development of novel and selective HNE inhibitors.

摘要

简介

人中性粒细胞弹性蛋白酶(HNE)参与多种严重的慢性疾病,尤其是心肺病理。出于这个原因,HNE 活性的调节代表了一种有前途的治疗方法,这一点在学术和制药环境中开发的许多新型和选择性 HNE 抑制剂中显而易见。

涵盖领域

本综述分析并总结了 2014-2018 年间针对心肺疾病治疗的人中性粒细胞弹性蛋白酶抑制剂的专利文献。

专家意见

HNE 是治疗各种炎症性疾病(包括多种心肺疾病)的一个有趣且明确的靶点。该领域的研究非常活跃,目前有许多 HNE 抑制剂处于不同的临床开发阶段。此外,HNE 抑制剂开发的新机会源于最近的研究表明 HNE 参与了许多其他炎症性疾病,包括类风湿关节炎、炎症性肠病、皮肤病和癌症。此外,还在探索双重 HNE/蛋白酶 3 抑制剂作为治疗中性粒细胞炎症性疾病的一种创新方法。因此,这些新的发展可能会激发人们对这一重要治疗靶点以及新型和选择性 HNE 抑制剂的新的和更大的兴趣。

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本文引用的文献

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