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乙酰胆碱酯酶抑制剂治疗阿尔茨海默病的专利研究进展(2016 年至今)

Acetylcholinesterase inhibitors for the treatment of Alzheimer's disease - a patent review (2016-present).

机构信息

Department of Scienze Di Base E Applicate per l'Ingegneria, Sapienza University of Rome, Rome, Italy.

Department of Chimica E Tecnologia Del Farmaco, Dipartimento Di Eccellenza 2018-2022, Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza University of Rome, Rome, Italy.

出版信息

Expert Opin Ther Pat. 2021 May;31(5):399-420. doi: 10.1080/13543776.2021.1874344. Epub 2021 Jan 14.

Abstract
  • AD, the most common form of dementia, has a multifactorial etiology, and the current therapy (AChEIs and memantine) is unable to interrupt its progress and fatal outcome. This is reflected in the research programs that are oriented toward the development of new therapeutics able to operate on multiple targets involved in the disease progression. - The patents from 2016 to present regarding the use of AChEIs in AD, concerns the development of new AChEIs, multitarget or multifunctional ligands, or the associations of currently used AChEIs with other compounds acting on different targets involved in the AD. - The development of new multitarget AChEIs promises to identify compounds with great therapeutic potential but requires more time and effort in order to obtain drugs with the optimal pharmacodynamic profile. Otherwise, the research on new combinations of existing drugs, with known pharmacodynamic and ADME profile, could shorten the time and reduce the costs to develop a new therapeutic treatment for AD. From the analyzed data, it seems more likely that a response to the urgent need to develop effective treatments for AD therapy could come more quickly from studies on drug combinations than from the development of new AChEIs.
摘要

阿尔茨海默病(AD)是最常见的痴呆症形式,具有多因素病因,目前的治疗方法(乙酰胆碱酯酶抑制剂和美金刚)无法阻止其进展和致命结局。这反映在研究计划中,这些计划旨在开发能够针对参与疾病进展的多个目标的新疗法。

  • 自 2016 年以来,关于在 AD 中使用乙酰胆碱酯酶抑制剂的专利,涉及新的乙酰胆碱酯酶抑制剂、多靶点或多功能配体的开发,或目前使用的乙酰胆碱酯酶抑制剂与其他作用于 AD 中涉及的不同靶点的化合物的联合使用。

  • 开发新的多靶点乙酰胆碱酯酶抑制剂有望识别出具有巨大治疗潜力的化合物,但需要更多的时间和精力来获得具有最佳药效学特征的药物。否则,对现有药物的新组合的研究,具有已知的药效学和 ADME 特征,可能会缩短时间并降低开发 AD 新治疗方法的成本。从分析的数据来看,似乎更有可能的是,针对开发有效 AD 治疗方法的紧迫需求的研究,可能会比开发新的乙酰胆碱酯酶抑制剂更快地产生反应。

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