CN115279751A - 一种特异性降解tau蛋白的小分子化合物及其用途 - Google Patents

一种特异性降解tau蛋白的小分子化合物及其用途 Download PDF

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CN115279751A
CN115279751A CN202180012446.4A CN202180012446A CN115279751A CN 115279751 A CN115279751 A CN 115279751A CN 202180012446 A CN202180012446 A CN 202180012446A CN 115279751 A CN115279751 A CN 115279751A
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CN115279751B (zh
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汪义朋
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Wang Yipeng
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Shanghai Qiangrei Biotechnology Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
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Abstract

本发明涉及双功能分子化合物技术领域,公开了一种具有特异性降解tau蛋白功能的小分子化合物及其应用。该特异性降解tau蛋白的小分子化合物的化学结构为TBM‑L‑ULM或其药学上可接受的盐、对映体、立体异构体、溶剂化物、多晶型物或N‑氧化物,其中,TBM为tau蛋白结合部分,L为连接体基团,ULM为泛素连接酶结合部分,所述tau蛋白结合部分与所述泛素连接酶结合部分通过连接体基团连接。本发明所述的特异性降解tau蛋白的小分子化合物能增强细胞中tau蛋白的降解,从而降低tau蛋白的含量。

Description

PCT国内申请,说明书已公开。

Claims (8)

  1. PCT国内申请,权利要求书已公开。
CN202180012446.4A 2020-02-13 2021-02-04 一种特异性降解tau蛋白的小分子化合物及其用途 Active CN115279751B (zh)

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CN202010090680.6A CN113248484A (zh) 2020-02-13 2020-02-13 一种特异性降解tau蛋白的小分子化合物及其应用
CN2020100906806 2020-02-13
PCT/CN2021/075201 WO2021160012A1 (zh) 2020-02-13 2021-02-04 一种特异性降解tau蛋白的小分子化合物及其用途

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Publication number Priority date Publication date Assignee Title
CN116964038A (zh) * 2021-03-03 2023-10-27 汪义朋 与tau蛋白结合的小分子化合物
CN115385908B (zh) * 2022-07-26 2024-04-12 阿茨可利(杭州)医学科技有限公司 靶向促进tau蛋白去磷酸化的小分子嵌合体及其应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106458993A (zh) * 2014-04-14 2017-02-22 阿尔维纳斯股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
CN108137507A (zh) * 2015-07-10 2018-06-08 阿尔维纳斯股份有限公司 基于mdm2的蛋白水解调节剂和相关的使用方法
CN110234646A (zh) * 2016-11-01 2019-09-13 阿尔维纳斯股份有限公司 靶向PROTAC的Tau蛋白及相关使用方法
WO2020014489A2 (en) * 2018-07-11 2020-01-16 H. Lee Moffitt Cancer Center And Research Institute, Inc. Dimeric immuno-modulatory compounds against cereblon-based mechanisms
CN110713480A (zh) * 2019-10-28 2020-01-21 浙江省医学科学院 AChE蛋白降解物及其制备方法和应用

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106458993A (zh) * 2014-04-14 2017-02-22 阿尔维纳斯股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
CN108137507A (zh) * 2015-07-10 2018-06-08 阿尔维纳斯股份有限公司 基于mdm2的蛋白水解调节剂和相关的使用方法
CN110234646A (zh) * 2016-11-01 2019-09-13 阿尔维纳斯股份有限公司 靶向PROTAC的Tau蛋白及相关使用方法
WO2020014489A2 (en) * 2018-07-11 2020-01-16 H. Lee Moffitt Cancer Center And Research Institute, Inc. Dimeric immuno-modulatory compounds against cereblon-based mechanisms
CN110713480A (zh) * 2019-10-28 2020-01-21 浙江省医学科学院 AChE蛋白降解物及其制备方法和应用

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