CN115380026A - 蛋白降解调节剂与其使用方法 - Google Patents

蛋白降解调节剂与其使用方法 Download PDF

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CN115380026A
CN115380026A CN202180024213.6A CN202180024213A CN115380026A CN 115380026 A CN115380026 A CN 115380026A CN 202180024213 A CN202180024213 A CN 202180024213A CN 115380026 A CN115380026 A CN 115380026A
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reaction
reaction mixture
ethyl acetate
room temperature
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CN115380026B (zh
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雷茂义
彭蕾
罗云富
徐雨
栗俊苗
邓新媛
康子圣
戈伟智
张国利
陈曙辉
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Medshine Discovery Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

一类蛋白降解靶向嵌合体(PROTAC)，及其在制备治疗相关疾病的药物中的应用。具体公开了式(I)所示化合物及其药学上可接受的盐。PTM‑L‑ULM(I)。

Description

PCT国内申请，说明书已公开。

Claims (20)

  1. PCT国内申请，权利要求书已公开。
CN202180024213.6A 2020-03-17 2021-03-17 蛋白降解调节剂与其使用方法 Active CN115380026B (zh)

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Application Number Priority Date Filing Date Title
CN202010187846 2020-03-17
CN2020101878466 2020-03-17
CN202011400367 2020-12-01
CN2020114003674 2020-12-01
CN202011583584 2020-12-28
CN2020115835841 2020-12-28
CN202110182231 2021-02-09
CN2021101822319 2021-02-09
PCT/CN2021/081375 WO2021185291A1 (zh) 2020-03-17 2021-03-17 蛋白降解调节剂与其使用方法

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CN115380026A true CN115380026A (zh) 2022-11-22
CN115380026B CN115380026B (zh) 2023-11-07

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EP (1) EP4122925A4 (zh)
JP (1) JP2023517393A (zh)
CN (1) CN115380026B (zh)
WO (1) WO2021185291A1 (zh)

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WO2023045978A1 (zh) * 2021-09-26 2023-03-30 南京明德新药研发有限公司 2,6-哌啶二酮类化合物与其应用
TW202325300A (zh) * 2021-11-18 2023-07-01 大陸商正大天晴藥業集團股份有限公司 稠合醯亞胺類衍生物及其應用
WO2023125944A1 (zh) * 2021-12-31 2023-07-06 正大天晴药业集团股份有限公司 含有杂环的化合物
CN114573534A (zh) * 2022-03-30 2022-06-03 八叶草健康产业研究院(厦门)有限公司 一种5-溴苯并呋喃酮的制备方法
WO2023227696A1 (en) * 2022-05-25 2023-11-30 Katholieke Universiteit Leuven New derivatives for treating trpm3 mediated disorders
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WO2024037616A1 (zh) * 2022-08-19 2024-02-22 正大天晴药业集团股份有限公司 包含环己基的化合物
WO2024055994A1 (zh) * 2022-09-14 2024-03-21 南京明德新药研发有限公司 萘并呋喃取代的戊二酰亚胺类化合物的晶型、制备方法及其应用
CN118005636A (zh) * 2022-11-08 2024-05-10 杭州格博生物医药有限公司 Wee1蛋白激酶降解剂及其用途

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JP2023517393A (ja) 2023-04-25
CN115380026B (zh) 2023-11-07
EP4122925A1 (en) 2023-01-25
WO2021185291A1 (zh) 2021-09-23
EP4122925A4 (en) 2024-04-17
US20230158152A1 (en) 2023-05-25

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