CA3115871A1 - Targeted protease degradation platform (ted) - Google Patents

Targeted protease degradation platform (ted) Download PDF

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Publication number
CA3115871A1
CA3115871A1 CA3115871A CA3115871A CA3115871A1 CA 3115871 A1 CA3115871 A1 CA 3115871A1 CA 3115871 A CA3115871 A CA 3115871A CA 3115871 A CA3115871 A CA 3115871A CA 3115871 A1 CA3115871 A1 CA 3115871A1
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CA
Canada
Prior art keywords
ubi
mmol
compound
substituted
group
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3115871A
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English (en)
French (fr)
Inventor
Sheldon Cao
Xiaolei Wang
Chaoran HUANG
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eubulus Biotherapeutics Inc
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Eubulus Biotherapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
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Application filed by Eubulus Biotherapeutics Inc filed Critical Eubulus Biotherapeutics Inc
Publication of CA3115871A1 publication Critical patent/CA3115871A1/en
Pending legal-status Critical Current

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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
    • A61K47/68—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
    • 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
    • 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

Landscapes

  • 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)
CA3115871A 2018-10-09 2019-10-09 Targeted protease degradation platform (ted) Pending CA3115871A1 (en)

Applications Claiming Priority (3)

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)
CN201811174965.7 2018-10-09
PCT/CN2019/110225 WO2020073930A1 (zh) 2018-10-09 2019-10-09 靶向蛋白酶降解平台(ted)

Publications (1)

Publication Number Publication Date
CA3115871A1 true CA3115871A1 (en) 2020-04-16

Family

ID=70164849

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3115871A Pending CA3115871A1 (en) 2018-10-09 2019-10-09 Targeted protease degradation platform (ted)

Country Status (7)

Country Link
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
WO2024086132A1 (en) * 2022-10-17 2024-04-25 Ohio University Protacs targeting viral enzymes for precise treatment of covid-19
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
IL321713A (en) 2022-12-27 2025-08-01 Merck Patent Gmbh Anti-PROTAC VHH antibodies and complexes
PE20260006A1 (es) 2023-01-26 2026-01-06 Arvinas Operations Inc Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos
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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Also Published As

Publication number Publication date
WO2020073930A1 (zh) 2020-04-16
CN111018857A (zh) 2020-04-17
CN112955182A (zh) 2021-06-11
CN111018857B (zh) 2023-06-02
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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