CN111018857B - 靶向蛋白酶降解平台(ted) - Google Patents

靶向蛋白酶降解平台(ted) Download PDF

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Publication number
CN111018857B
CN111018857B CN201811174965.7A CN201811174965A CN111018857B CN 111018857 B CN111018857 B CN 111018857B CN 201811174965 A CN201811174965 A CN 201811174965A CN 111018857 B CN111018857 B CN 111018857B
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ted
protein
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CN111018857A (zh
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曹小冬
王晓磊
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Youbo Biotechnology (Hong Kong) Limited
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Jiaxing Youbo Biotechnology Co ltd
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Application filed by Jiaxing Youbo Biotechnology Co ltd filed Critical Jiaxing Youbo Biotechnology Co ltd
Priority to CN201980066587.7A priority patent/CN112955182A/zh
Priority to US17/283,892 priority patent/US20210369853A1/en
Priority to JP2021546035A priority patent/JP2022513360A/ja
Priority to EP19872052.6A priority patent/EP3865152A4/en
Priority to CA3115871A priority patent/CA3115871A1/en
Priority to PCT/CN2019/110225 priority patent/WO2020073930A1/zh
Priority to AU2019357908A priority patent/AU2019357908A1/en
Publication of CN111018857A publication Critical patent/CN111018857A/zh
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    • 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K47/551—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 one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201811174965.7A 2018-10-09 2018-10-09 靶向蛋白酶降解平台(ted) Active CN111018857B (zh)

Priority Applications (8)

Application Number Priority Date Filing Date Title
CN201811174965.7A CN111018857B (zh) 2018-10-09 2018-10-09 靶向蛋白酶降解平台(ted)
US17/283,892 US20210369853A1 (en) 2018-10-09 2019-10-09 Targeted protease degradation platform
JP2021546035A JP2022513360A (ja) 2018-10-09 2019-10-09 標的プロテアーゼ分解プラットフォーム（ｔｅｄ）
EP19872052.6A EP3865152A4 (en) 2018-10-09 2019-10-09 TARGETED PROTEASE DEGRADATION PLATFORM
CN201980066587.7A CN112955182A (zh) 2018-10-09 2019-10-09 靶向蛋白酶降解平台(ted)
CA3115871A CA3115871A1 (en) 2018-10-09 2019-10-09 Targeted protease degradation platform (ted)
PCT/CN2019/110225 WO2020073930A1 (zh) 2018-10-09 2019-10-09 靶向蛋白酶降解平台(ted)
AU2019357908A AU2019357908A1 (en) 2018-10-09 2019-10-09 Targeted protease degradation platform

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201811174965.7A CN111018857B (zh) 2018-10-09 2018-10-09 靶向蛋白酶降解平台(ted)

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CN111018857A CN111018857A (zh) 2020-04-17
CN111018857B true CN111018857B (zh) 2023-06-02

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CN201980066587.7A Pending CN112955182A (zh) 2018-10-09 2019-10-09 靶向蛋白酶降解平台(ted)

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US (1) US20210369853A1 (enExample)
EP (1) EP3865152A4 (enExample)
JP (1) JP2022513360A (enExample)
CN (2) CN111018857B (enExample)
AU (1) AU2019357908A1 (enExample)
CA (1) CA3115871A1 (enExample)
WO (1) WO2020073930A1 (enExample)

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BR112020020307A2 (pt) 2018-04-04 2021-01-12 Arvinas Operations, Inc. Moduladores de proteólise e métodos de uso associados
EP3878472A1 (en) * 2020-03-12 2021-09-15 Julius-Maximilians-Universitaet Wuerzburg Proteolysis targeting chimera (protac) for degradation of aurora a-kinase
US20230158158A1 (en) 2020-03-27 2023-05-25 Uppthera Pyrazolo quinazoline derivative compounds inducing selective degradation of plk1
CN113509557A (zh) * 2020-04-09 2021-10-19 嘉兴优博生物技术有限公司 靶向蛋白酶降解平台(ted)
EP4168410A1 (en) * 2020-06-22 2023-04-26 The United States of America, as represented by the Secretary, Department of Health and Human Services Methotrexate analogs and methods of use
CN112062768B (zh) * 2020-07-20 2021-08-31 中山大学肿瘤防治中心（中山大学附属肿瘤医院、中山大学肿瘤研究所） 具有Aurora激酶降解活性的小分子及其制备方法和应用
WO2022165185A1 (en) * 2021-02-01 2022-08-04 Beth Israel Deaconess Medical Center, Inc. Cancer-selective target degradation by targeting group caged protacs
CN114106010A (zh) * 2021-04-20 2022-03-01 上海大学 一种蛋白降解靶向嵌合体的制备方法和应用
JP2024526259A (ja) 2021-07-02 2024-07-17 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 抗ｐｒｏｔａｃ抗体および複合体
CN115594733A (zh) * 2021-07-09 2023-01-13 上海大学（Cn） 化合物、蛋白降解靶向嵌合体及其制备方法和应用
JP7555155B2 (ja) * 2021-08-10 2024-09-24 オップテラ インコーポレイテッド 新規ｐｌｋ１分解誘導化合物
CN115894506B (zh) * 2021-09-30 2025-03-18 四川大学 一种嵌合体分子及其制备方法和用途
CN115960104A (zh) * 2021-10-09 2023-04-14 嘉兴优博生物技术有限公司 靶向蛋白酶降解(ted)平台
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CN120417934A (zh) * 2022-12-23 2025-08-01 基因泰克公司 Cereblon降解剂缀合物及其用途
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KR20260023524A (ko) * 2023-05-18 2026-02-20 파이어플라이 바이오, 인크. 이소인돌리논-글루타르이미드 항체 접합체 및 이의 용도
CN117946118A (zh) * 2024-01-15 2024-04-30 珃诺生物医药科技(杭州)有限公司 一种靶向降解erk5蛋白的化合物及其制备方法
WO2025168071A1 (zh) * 2024-02-08 2025-08-14 映恩生物制药（苏州）有限公司 一种含氮杂环化合物、其偶联物及其制备方法和用途
WO2025228305A1 (zh) * 2024-04-28 2025-11-06 中国科学院上海药物研究所 一种蛋白降解剂缀合物及其偶联物
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CA3115871A1 (en) 2020-04-16
WO2020073930A1 (zh) 2020-04-16
CN111018857A (zh) 2020-04-17
CN112955182A (zh) 2021-06-11
AU2019357908A1 (en) 2021-06-03
US20210369853A1 (en) 2021-12-02
EP3865152A1 (en) 2021-08-18
JP2022513360A (ja) 2022-02-07
EP3865152A4 (en) 2022-11-16

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