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

Antibody-ALK5 inhibitor conjugates and their uses Download PDF

Info

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
Authority
AU
Australia
Prior art keywords
adc
antibody
pyridin
linker
pyrazol
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.)
Active
Application number
AU2018431586A
Other languages
English (en)
Other versions
AU2018431586A1 (en
Inventor
Dori A. THOMAS-KARYAT
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.)
Synthis Therapeutics Inc
Original Assignee
Synthis 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 Synthis Therapeutics Inc filed Critical Synthis Therapeutics Inc
Publication of AU2018431586A1 publication Critical patent/AU2018431586A1/en
Application granted granted Critical
Publication of AU2018431586B2 publication Critical patent/AU2018431586B2/en
Priority to AU2025204026A priority Critical patent/AU2025204026A1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (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

Family

ID=69142765

Family Applications (2)

Application Number Title Priority Date Filing Date
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

Family Applications After (1)

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

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
WO2020013803A1 (en) * 2018-07-09 2020-01-16 Synthis, Llc Antibody-alk5 inhibitor conjugates and their uses
WO2020256721A1 (en) * 2019-06-19 2020-12-24 Synthis, Llc Antib0dy-alk5 inhibitor conjugates and their uses
JP2023509760A (ja) * 2020-01-08 2023-03-09 シンシス セラピューティクス，インコーポレイテッド Ａｌｋ５阻害剤複合体およびその使用
WO2021167703A1 (en) 2020-02-19 2021-08-26 Nammi Therapeutics, Inc. Formulated and/or co-formulated liposome compositions containing tgfb 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
WO2022063050A1 (zh) * 2020-09-28 2022-03-31 四川科伦博泰生物医药股份有限公司 吡唑类化合物及其制备方法和用途
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
AU2023230346A1 (en) * 2022-03-09 2024-10-17 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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP1539748A1 (en) * 2002-07-31 2005-06-15 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
EP2478912B1 (en) 2003-11-06 2016-08-31 Seattle Genetics, Inc. Auristatin conjugates with anti-HER2 or anti-CD22 antibodies and their use in therapy
CN101330914A (zh) 2005-12-16 2008-12-24 爱尔康公司 使用alk5调节剂控制眼内压
CA2891280C (en) * 2012-11-24 2018-03-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
WO2016115218A1 (en) * 2015-01-14 2016-07-21 The California Institute For Biomedical Research Antibody drug conjugates for the treatment of immune conditions
WO2016115345A1 (en) * 2015-01-14 2016-07-21 The Brigham And Women's Hospital, Treatment of cancer with anti-lap monoclonal antibodies
US20170158772A1 (en) * 2015-12-07 2017-06-08 Opi Vi - Ip Holdco Llc Compositions of antibody construct - agonist conjugates and methods of use thereof
WO2019195278A1 (en) * 2018-04-02 2019-10-10 Silverback Therapeutics, Inc. Alk5 inhibitors, conjugates, and uses thereof
WO2020013803A1 (en) 2018-07-09 2020-01-16 Synthis, Llc Antibody-alk5 inhibitor conjugates and their uses

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040202666A1 (en) * 2003-01-24 2004-10-14 Immunomedics, Inc. Anti-cancer anthracycline drug-antibody conjugates
US9695240B2 (en) * 2008-07-15 2017-07-04 Genentech, Inc. Anthracycline derivative conjugates, process for their preparation and their use as antitumor compounds
US20120022016A1 (en) * 2010-07-21 2012-01-26 Barbeau Donald L Compounds and methods for selectively targeting tumor-associated mucins
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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MIZEJEWSKI GJ. "The adenocarcinoma cell surface mucin receptor for alpha-fetoprotein: is the same receptor present on circulating monocytes and macrophages? A commentary." TUMOUR BIOLOGY. 2014, Vol. 35, issue 8, pp 7397-7402. *
RIKKEB HOLMGAARD ET AL: "Targeting the TGF[beta] pathway with galunisertib, a TGF[beta]RI small molecule inhibitor, promotes anti-tumor immunity leading to durable..." JOURNAL FOR IMMUNOTHERAPY OF CANCER, 2018, Vol. 6, issue 1, pp 1-15. *

Also Published As

Publication number Publication date
WO2020013803A1 (en) 2020-01-16
JP7573685B2 (ja) 2024-10-25
CN112601522A (zh) 2021-04-02
JP7798998B2 (ja) 2026-01-14
US20210299268A1 (en) 2021-09-30
AU2025204026A1 (en) 2025-06-19
EP3820467A1 (en) 2021-05-19
CA3104934A1 (en) 2020-01-16
JP2025023920A (ja) 2025-02-19
CN112601522B (zh) 2024-11-05
AU2018431586A1 (en) 2021-01-21
CN119488607A (zh) 2025-02-21
JP7335957B2 (ja) 2023-08-30
EP3820467A4 (en) 2022-05-04
JP2023113685A (ja) 2023-08-16
JP2022500486A (ja) 2022-01-04

Similar Documents

Publication Publication Date Title
AU2018431586B2 (en) Antibody-ALK5 inhibitor conjugates and their uses
US11987558B1 (en) ALK5 inhibitors and their uses
JP2023116596A (ja) Ｃｄ１１７＋細胞を減少させるための組成物及び方法
JP7854462B2 (ja) 抗体－ａｌｋ５阻害剤コンジュゲートおよびその使用
JP2018502839A (ja) Ｂｃｌ−ｘＬ阻害性化合物およびこれを含む抗体薬物コンジュゲート
JP2026000988A (ja) Ａｌｋ５阻害剤複合体およびその使用
JP7689606B2 (ja) ネクチン－４抗体及び抗体－薬物コンジュゲート

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)