AU2018431586B2 - Antibody-ALK5 inhibitor conjugates and their uses - Google Patents

Antibody-ALK5 inhibitor conjugates and their uses Download PDF

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Publication number
AU2018431586B2
AU2018431586B2 AU2018431586A AU2018431586A AU2018431586B2 AU 2018431586 B2 AU2018431586 B2 AU 2018431586B2 AU 2018431586 A AU2018431586 A AU 2018431586A AU 2018431586 A AU2018431586 A AU 2018431586A AU 2018431586 B2 AU2018431586 B2 AU 2018431586B2
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Australia
Prior art keywords
adc
antibody
pyridin
linker
pyrazol
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AU2018431586A
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AU2018431586A1 (en
Inventor
Dori A. THOMAS-KARYAT
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Synthis Therapeutics Inc
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Synthis Therapeutics Inc
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Priority to AU2025204026A priority Critical patent/AU2025204026A1/en
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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)
AU2018431586A 2018-07-09 2018-07-09 Antibody-ALK5 inhibitor conjugates and their uses Active AU2018431586B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2025204026A AU2025204026A1 (en) 2018-07-09 2025-05-29 Antibody-alk5 inhibitor conjugates and their uses

Applications Claiming Priority (1)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2025204026A Division AU2025204026A1 (en) 2018-07-09 2025-05-29 Antibody-alk5 inhibitor conjugates and their uses

Publications (2)

Publication Number Publication Date
AU2018431586A1 AU2018431586A1 (en) 2021-01-21
AU2018431586B2 true AU2018431586B2 (en) 2025-03-20

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AU2018431586A Active AU2018431586B2 (en) 2018-07-09 2018-07-09 Antibody-ALK5 inhibitor conjugates and their uses
AU2025204026A Pending AU2025204026A1 (en) 2018-07-09 2025-05-29 Antibody-alk5 inhibitor conjugates and their uses

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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=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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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US20040202666A1 (en) * 2003-01-24 2004-10-14 Immunomedics, Inc. Anti-cancer anthracycline drug-antibody conjugates
US20120022016A1 (en) * 2010-07-21 2012-01-26 Barbeau Donald L Compounds and methods for selectively targeting tumor-associated mucins
US9695240B2 (en) * 2008-07-15 2017-07-04 Genentech, Inc. Anthracycline derivative conjugates, process for their preparation and their use as antitumor compounds
WO2018208720A1 (en) * 2017-05-09 2018-11-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Combination pdl1 and tgf-beta blockade in patients with hpv+ malignancies

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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
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Also Published As

Publication number Publication date
CN119488607A (zh) 2025-02-21
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
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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