CN113164495B - E3连接酶的共价靶向 - Google Patents

E3连接酶的共价靶向 Download PDF

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Publication number
CN113164495B
CN113164495B CN201980079494.8A CN201980079494A CN113164495B CN 113164495 B CN113164495 B CN 113164495B CN 201980079494 A CN201980079494 A CN 201980079494A CN 113164495 B CN113164495 B CN 113164495B
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substituted
unsubstituted
ubiquitin ligase
membered
binding agent
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Chinese (zh)
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CN113164495A (zh
Inventor
J·斯普拉德林
C·C·沃德
D·K·野村
M·席尔勒
J·A·塔拉里科
J·麦肯纳
T·J·马伊莫内
胡曦睿
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Morphochem GmbH
University of California San Diego UCSD
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Morphochem AG fuer Kombinatorische Chemie
University of California San Diego UCSD
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K47/55—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Other Investigation Or Analysis Of Materials By Electrical Means (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201980079494.8A 2018-10-09 2019-10-09 E3连接酶的共价靶向 Active CN113164495B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202510552209.7A CN120468320A (zh) 2018-10-09 2019-10-09 E3连接酶的共价靶向

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862743337P 2018-10-09 2018-10-09
US62/743,337 2018-10-09
PCT/US2019/055461 WO2020076996A1 (en) 2018-10-09 2019-10-09 Covalent targeting of e3 ligases

Related Child Applications (1)

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CN202510552209.7A Division CN120468320A (zh) 2018-10-09 2019-10-09 E3连接酶的共价靶向

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CN113164495B true CN113164495B (zh) 2025-04-22

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EP (1) EP3863642A4 (enExample)
JP (2) JP7631191B2 (enExample)
CN (2) CN113164495B (enExample)
WO (1) WO2020076996A1 (enExample)

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EP3768708A4 (en) 2018-03-23 2022-08-03 The Regents of the University of California METHODS AND COMPOUNDS FOR TARGETED AUTOPHAGY
GB202005876D0 (en) * 2020-04-22 2020-06-03 Univ Dundee Protein degradation
EP4188907A1 (en) * 2020-07-30 2023-06-07 Sanofi Acrylamide-substituted indane compounds and therapeutic use thereof
JP2024502467A (ja) * 2021-01-08 2024-01-19 ザ ボード オブ リージェンツ オブ ザ ユニバーシティー オブ テキサス システム ニンボリドアナログ及びその使用方法
US20250276069A1 (en) * 2021-03-04 2025-09-04 The Scripps Research Institute Heterobifunctional compositions for targeted protein degradation and methods for their use
WO2022201162A1 (en) * 2021-03-25 2022-09-29 Technion Research & Development Foundation Limited Rnf4 targeting compounds and uses thereof
CN113527270B (zh) * 2021-07-16 2024-03-01 河南大学 一种靶向单酰基甘油脂肪酶的protac分子的医药中间体、制备方法及应用
CN116676273A (zh) * 2022-02-22 2023-09-01 中国科学院深圳先进技术研究院 一种蛋白水解靶向流感病毒及其制备方法和应用
CN114560908B (zh) * 2022-03-11 2024-10-25 国家纳米科学中心 一种多肽protac分子及其制备方法和应用
CN115417913B (zh) * 2022-08-26 2024-10-29 天津医科大学 靶向雌激素受体的谷胱甘肽响应protac降解剂的制备方法及应用
TW202416958A (zh) * 2022-10-13 2024-05-01 南韓商韓美藥品股份有限公司 用於抑制yap-tead交互作用的新穎雜雙環化合物及包含其之藥學組成物
EP4605088A1 (en) * 2022-10-21 2025-08-27 Novartis AG Molecular glue degrader compounds and uses thereof
WO2025226951A1 (en) * 2024-04-24 2025-10-30 Novartis Ag Molecular glue degrader compounds and uses thereof
CN119331047B (zh) * 2024-10-09 2025-09-30 重庆医科大学 一种蛋白水解靶向嵌合体及其制备方法
CN119405823B (zh) * 2024-11-15 2025-10-21 湖南大学 一种基于g四链体rna的蛋白降解靶向嵌合体及其制备方法与应用

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Publication number Publication date
US20250120982A1 (en) 2025-04-17
US12161648B2 (en) 2024-12-10
CN113164495A (zh) 2021-07-23
JP2022512643A (ja) 2022-02-07
EP3863642A4 (en) 2022-06-29
US20210369731A1 (en) 2021-12-02
JP7631191B2 (ja) 2025-02-18
CN120468320A (zh) 2025-08-12
WO2020076996A1 (en) 2020-04-16
EP3863642A1 (en) 2021-08-18
JP2025072508A (ja) 2025-05-09

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