JP7613580B2 - 抗体および機能性物質のコンジュゲートまたはその塩、ならびにその製造に用いられる化合物またはその塩 - Google Patents

抗体および機能性物質のコンジュゲートまたはその塩、ならびにその製造に用いられる化合物またはその塩 Download PDF

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JP7613580B2
JP7613580B2 JP2023525901A JP2023525901A JP7613580B2 JP 7613580 B2 JP7613580 B2 JP 7613580B2 JP 2023525901 A JP2023525901 A JP 2023525901A JP 2023525901 A JP2023525901 A JP 2023525901A JP 7613580 B2 JP7613580 B2 JP 7613580B2
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JPWO2022255425A5 (https=
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豊 松田
友博 藤井
竜介 平間
トーマス マルコタン
アラン プライア
クリストファー ウォン
コンスタンティノ プラカス
友博 渡部
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Ajinomoto Co Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68031Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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 determinant of a tumour cell
    • A61K47/6855Medicinal 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 determinant of a tumour cell the tumour determinant being from breast cancer cell
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6883Polymer-drug antibody conjugates, e.g. mitomycin-dextran-Ab; DNA-polylysine-antibody complex or conjugate used for therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6889Conjugates 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2023525901A 2021-06-01 2022-06-01 抗体および機能性物質のコンジュゲートまたはその塩、ならびにその製造に用いられる化合物またはその塩 Active JP7613580B2 (ja)

Priority Applications (1)

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JP2024231090A JP2025060910A (ja) 2021-06-01 2024-12-26 抗体および機能性物質のコンジュゲートまたはその塩、ならびにその製造に用いられる化合物またはその塩

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202163195448P 2021-06-01 2021-06-01
US63/195,448 2021-06-01
US202263312489P 2022-02-22 2022-02-22
US63/312,489 2022-02-22
PCT/JP2022/022393 WO2022255425A1 (ja) 2021-06-01 2022-06-01 抗体および機能性物質のコンジュゲートまたはその塩、ならびにその製造に用いられる化合物またはその塩

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JPWO2022255425A1 JPWO2022255425A1 (https=) 2022-12-08
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JP7613580B2 true JP7613580B2 (ja) 2025-01-15

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JP2024231090A Pending JP2025060910A (ja) 2021-06-01 2024-12-26 抗体および機能性物質のコンジュゲートまたはその塩、ならびにその製造に用いられる化合物またはその塩

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US (1) US20240165260A1 (https=)
EP (1) EP4349373A1 (https=)
JP (2) JP7613580B2 (https=)
KR (1) KR20240016287A (https=)
AU (1) AU2022286137A1 (https=)
CA (1) CA3222015A1 (https=)
WO (1) WO2022255425A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN120813388A (zh) * 2023-03-02 2025-10-17 日本医事物理股份有限公司 放射性金属标记抗体、放射性药物及化合物
WO2026054053A1 (ja) * 2024-09-05 2026-03-12 日本メジフィジックス株式会社 修飾抗体、放射性金属標識抗体及び放射性医薬

Citations (9)

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JP2001505194A (ja) 1996-11-05 2001-04-17 ブリストル―マイヤーズ・スクイブ・カンパニー 分枝ペプチド・リンカー
JP2016534990A (ja) 2013-10-15 2016-11-10 シアトル ジェネティックス, インコーポレイテッド 改善されたリガンド−薬物コンジュゲート薬物動態のためのpeg化薬物−リンカー
WO2018213077A1 (en) 2017-05-18 2018-11-22 Regeneron Pharmaceuticals, Inc. Cyclodextrin protein drug conjugates
WO2018218004A1 (en) 2017-05-24 2018-11-29 The Board Of Regents Of The University Of Texas System Linkers for antibody drug conjugates
WO2019231879A1 (en) 2018-05-29 2019-12-05 Bristol-Myers Squibb Company Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making
JP2019536765A (ja) 2016-11-08 2019-12-19 レゲネロン ファーマシューティカルス,インコーポレーテッド ステロイド及びそのタンパク質コンジュゲート
WO2019240288A1 (ja) 2018-06-14 2019-12-19 味の素株式会社 抗体に対する親和性物質、および生体直交性官能基を有する化合物またはその塩
WO2020252043A1 (en) 2019-06-10 2020-12-17 Sutro Biopharma, Inc. 5H-PYRROLO[3,2-d]PYRIMIDINE-2,4-DIAMINO COMPOUNDS AND ANTIBODY CONJUGATES THEREOF
JP2021502341A (ja) 2017-11-07 2021-01-28 レゲネロン ファーマシューティカルス,インコーポレーテッド 抗体薬物コンジュゲートのための親水性リンカー

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HK1243931A1 (zh) 2014-12-03 2018-07-27 F. Hoffmann-La Roche Ag 抗金黄色葡萄球菌抗体利福霉素缀合物及其用途
AU2018259856B2 (en) 2017-04-28 2025-05-01 Ajinomoto Co., Inc. Compound having substance that has affinity for soluble protein, cleavable moiety, and reactive group, or salt thereof
JPWO2019093495A1 (ja) * 2017-11-10 2020-11-26 株式会社明治 たんぱく質検出法
KR102921757B1 (ko) * 2018-06-14 2026-02-03 아지노모토 가부시키가이샤 항체에 대한 친화성 물질, 절단성 부분 및 반응성기를 갖는 화합물 또는 이의 염
JPWO2020090979A1 (ja) 2018-10-31 2021-09-24 味の素株式会社 抗体に対する親和性物質、切断性部分および反応性基を有する化合物またはその塩
CN113853219B (zh) * 2019-05-20 2025-01-07 诺华股份有限公司 具有包含亲水性基团的接头的抗体药物缀合物

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Publication number Priority date Publication date Assignee Title
JP2001505194A (ja) 1996-11-05 2001-04-17 ブリストル―マイヤーズ・スクイブ・カンパニー 分枝ペプチド・リンカー
JP2016534990A (ja) 2013-10-15 2016-11-10 シアトル ジェネティックス, インコーポレイテッド 改善されたリガンド−薬物コンジュゲート薬物動態のためのpeg化薬物−リンカー
JP2019536765A (ja) 2016-11-08 2019-12-19 レゲネロン ファーマシューティカルス,インコーポレーテッド ステロイド及びそのタンパク質コンジュゲート
WO2018213077A1 (en) 2017-05-18 2018-11-22 Regeneron Pharmaceuticals, Inc. Cyclodextrin protein drug conjugates
WO2018218004A1 (en) 2017-05-24 2018-11-29 The Board Of Regents Of The University Of Texas System Linkers for antibody drug conjugates
JP2021502341A (ja) 2017-11-07 2021-01-28 レゲネロン ファーマシューティカルス,インコーポレーテッド 抗体薬物コンジュゲートのための親水性リンカー
WO2019231879A1 (en) 2018-05-29 2019-12-05 Bristol-Myers Squibb Company Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making
WO2019240288A1 (ja) 2018-06-14 2019-12-19 味の素株式会社 抗体に対する親和性物質、および生体直交性官能基を有する化合物またはその塩
WO2020252043A1 (en) 2019-06-10 2020-12-17 Sutro Biopharma, Inc. 5H-PYRROLO[3,2-d]PYRIMIDINE-2,4-DIAMINO COMPOUNDS AND ANTIBODY CONJUGATES THEREOF

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WO2022255425A1 (ja) 2022-12-08
JPWO2022255425A1 (https=) 2022-12-08
EP4349373A1 (en) 2024-04-10
AU2022286137A2 (en) 2024-01-11
JP2025060910A (ja) 2025-04-10
KR20240016287A (ko) 2024-02-06
AU2022286137A1 (en) 2023-12-14
US20240165260A1 (en) 2024-05-23
CA3222015A1 (en) 2022-12-08

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