CN119488607A - 抗体-alk5抑制剂偶联物及其用途 - Google Patents

抗体-alk5抑制剂偶联物及其用途 Download PDF

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Publication number
CN119488607A
CN119488607A CN202411470468.7A CN202411470468A CN119488607A CN 119488607 A CN119488607 A CN 119488607A CN 202411470468 A CN202411470468 A CN 202411470468A CN 119488607 A CN119488607 A CN 119488607A
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CN
China
Prior art keywords
adc
antibody
linker
antigen
cell
Prior art date
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
CN202411470468.7A
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English (en)
Chinese (zh)
Inventor
D·A·托马斯-卡亚特
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.)
Hinthers Therapeutics Inc
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Hinthers Therapeutics 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
Publication date
Application filed by Hinthers Therapeutics Inc filed Critical Hinthers Therapeutics Inc
Priority to CN202411470468.7A priority Critical patent/CN119488607A/zh
Publication of CN119488607A publication Critical patent/CN119488607A/zh
Pending legal-status Critical Current

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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
    • A61K47/68—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
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6849—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
    • 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
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • 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
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/22—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors ; against growth regulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2806—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2896—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against molecules with a "CD"-designation, not provided for elsewhere
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/77—Internalization into the cell

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202411470468.7A 2018-07-09 2018-07-09 抗体-alk5抑制剂偶联物及其用途 Pending CN119488607A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202411470468.7A CN119488607A (zh) 2018-07-09 2018-07-09 抗体-alk5抑制剂偶联物及其用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/US2018/041291 WO2020013803A1 (en) 2018-07-09 2018-07-09 Antibody-alk5 inhibitor conjugates and their uses
CN201880096817.XA CN112601522B (zh) 2018-07-09 2018-07-09 抗体-alk5抑制剂偶联物及其用途
CN202411470468.7A CN119488607A (zh) 2018-07-09 2018-07-09 抗体-alk5抑制剂偶联物及其用途

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201880096817.XA Division CN112601522B (zh) 2018-07-09 2018-07-09 抗体-alk5抑制剂偶联物及其用途

Publications (1)

Publication Number Publication Date
CN119488607A true CN119488607A (zh) 2025-02-21

Family

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Family Applications (2)

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CN202411470468.7A Pending CN119488607A (zh) 2018-07-09 2018-07-09 抗体-alk5抑制剂偶联物及其用途
CN201880096817.XA Active CN112601522B (zh) 2018-07-09 2018-07-09 抗体-alk5抑制剂偶联物及其用途

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Country Status (7)

Country Link
US (1) US20210299268A1 (https=)
EP (1) EP3820467A4 (https=)
JP (3) JP7335957B2 (https=)
CN (2) CN119488607A (https=)
AU (2) AU2018431586B2 (https=)
CA (1) CA3104934A1 (https=)
WO (1) WO2020013803A1 (https=)

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US11583593B2 (en) 2016-01-14 2023-02-21 Synthis Therapeutics, Inc. Antibody-ALK5 inhibitor conjugates and their uses
EP3820467A4 (en) * 2018-07-09 2022-05-04 Synthis Therapeutics, Inc. ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES
WO2020256721A1 (en) * 2019-06-19 2020-12-24 Synthis, Llc Antib0dy-alk5 inhibitor conjugates and their uses
AU2021205893A1 (en) * 2020-01-08 2022-06-23 Synthis Therapeutics, Inc. ALK5 inhibitor conjugates and uses thereof
US11801304B2 (en) * 2020-02-19 2023-10-31 Nammi Therapeutics, Inc. Formulated and/or co-formulated liposome compositions containing TFGB antagonist prodrugs useful in the treatment of cancer and methods thereof
JP2023532304A (ja) 2020-07-01 2023-07-27 エーアールエス ファーマシューティカルズ オペレーションズ，インク． 抗ａｓｇｒ１抗体コンジュゲートおよびその使用
EP4219453A4 (en) * 2020-09-28 2024-10-09 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. PYRAZOLE COMPOUND AND ITS PREPARATION METHOD AND ITS USE
WO2022076905A1 (en) * 2020-10-09 2022-04-14 Silverback Therapeutics, Inc. Alk5 inhibitors, conjugates, and uses thereof
CN115192731B (zh) * 2021-04-12 2023-09-26 中国科学院上海有机化学研究所 一种抗体药物偶联物的制备方法
WO2023170608A1 (en) * 2022-03-09 2023-09-14 Orum Therapeutics, Inc. Activators of effector t cells
CN121712526A (zh) * 2023-06-13 2026-03-20 辛瑟斯治疗股份有限公司 抗cd5抗体及其用途

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US6491916B1 (en) * 1994-06-01 2002-12-10 Tolerance Therapeutics, Inc. Methods and materials for modulation of the immunosuppresive activity and toxicity of monoclonal antibodies
SE9402430L (sv) * 1994-07-11 1996-01-12 Pharmacia Ab Konjugat mellan modifierat superantigen och en målsökande förening samt användning av konjugaten
WO2004013135A1 (en) * 2002-07-31 2004-02-12 Smithkline Beecham Corporation 2-phenylpyridin-4-yl derivatives as alk5 inhibitors
UA80296C2 (en) 2002-09-06 2007-09-10 Biogen Inc Imidazolopyridines and methods of making and using the same
US20040202666A1 (en) * 2003-01-24 2004-10-14 Immunomedics, Inc. Anti-cancer anthracycline drug-antibody conjugates
US7498298B2 (en) 2003-11-06 2009-03-03 Seattle Genetics, Inc. Monomethylvaline compounds capable of conjugation to ligands
WO2007070866A2 (en) 2005-12-16 2007-06-21 Alcon, Inc. Control of intraocular pressure using alk5 modulation agents
CN102159248B (zh) * 2008-07-15 2013-09-11 健泰科生物技术公司 蒽环类衍生物缀合物、它们的制备方法以及它们作为抗肿瘤化合物的用途
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Also Published As

Publication number Publication date
JP2025023920A (ja) 2025-02-19
CN112601522A (zh) 2021-04-02
EP3820467A1 (en) 2021-05-19
CA3104934A1 (en) 2020-01-16
AU2025204026A1 (en) 2025-06-19
JP2022500486A (ja) 2022-01-04
AU2018431586B2 (en) 2025-03-20
US20210299268A1 (en) 2021-09-30
EP3820467A4 (en) 2022-05-04
JP7573685B2 (ja) 2024-10-25
JP7335957B2 (ja) 2023-08-30
AU2018431586A1 (en) 2021-01-21
JP2023113685A (ja) 2023-08-16
JP7798998B2 (ja) 2026-01-14
CN112601522B (zh) 2024-11-05
WO2020013803A1 (en) 2020-01-16

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