锰酸盐抑制剂:专利审查。

IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pharmaceutical patent analyst Pub Date : 2021-01-01 Epub Date: 2021-01-14 DOI:10.4155/ppa-2020-0028
Ahmed M Abdelaziz, Mingfeng Yu, Shudong Wang
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引用次数: 8

摘要

mRNA翻译的改变在确定细胞蛋白质组的变化中起着至关重要的作用。真核起始因子4E被丝裂原激活的蛋白激酶相互作用激酶(Mnks)磷酸化,导致特定致癌蛋白mrna的释放和翻译。近年来,制药行业开发新型化学骨架以制造有效和选择性的Mnk抑制剂的努力取得了丰硕成果。吡啶酮-动物支架已被用于生成多个系列的Mnk抑制剂,并在多个专利申请和研究文章中提出。Tomivosertib (eFT508)就是具有这种支架的分子之一。它是首批进入临床试验的两种Mnk抑制剂之一,并已显示出对几种实体和血液系统癌症的重大活性。本文通过对近5年来相关专利申请的分析,简要回顾了吡酮-氨基衍生的Mnk抑制剂的发展现状。
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Mnk inhibitors: a patent review.

The alteration of mRNA translation has a crucial role in defining the changes in cellular proteome. The phosphorylation of eukaryotic initiation factor 4E by mitogen-activated protein kinase-interacting kinases (Mnks) leads to the release and translation of mRNAs of specific oncogenic proteins. In recent years, the efforts made by the pharmaceutical industry to develop novel chemical skeletons to create potent and selective Mnk inhibitors have been fruitful. The pyridone-aminal scaffold has been utilized to generate several series of Mnk inhibitors presented in multiple patent applications and research articles. Tomivosertib (eFT508) is one of the molecules with such scaffold. It is one of the first two Mnk inhibitors that entered clinical trials, and has displayed momentous activity against several solid and hematological cancers. The present compilation provides a succinct review of the current state of development of pyridone-aminal-derived Mnk inhibitors through the analysis of relevant patent applications filed in the last 5 years.

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来源期刊
Pharmaceutical patent analyst
Pharmaceutical patent analyst PHARMACOLOGY & PHARMACY-
CiteScore
1.80
自引率
0.00%
发文量
22
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