JP2024523453A - ビス-ベンゾイミダゾールstingアゴニスト免疫複合体及びその使用 - Google Patents

ビス-ベンゾイミダゾールstingアゴニスト免疫複合体及びその使用 Download PDF

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JP2024523453A
JP2024523453A JP2023578817A JP2023578817A JP2024523453A JP 2024523453 A JP2024523453 A JP 2024523453A JP 2023578817 A JP2023578817 A JP 2023578817A JP 2023578817 A JP2023578817 A JP 2023578817A JP 2024523453 A JP2024523453 A JP 2024523453A
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alkyldiyl
peg
ethoxy
antibody
pep
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JP2024523453A5 (https=
Inventor
ゲイリー ブラント,
ロマス クディルカ,
ブライアン サフィナ,
マシュー チョウ,
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ボルト バイオセラピューティクス、インコーポレーテッド
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Publication of JP2024523453A publication Critical patent/JP2024523453A/ja
Publication of JP2024523453A5 publication Critical patent/JP2024523453A5/ja
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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K47/56Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • 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
    • A61K47/6853Carcino-embryonic antigens
    • 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

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Oncology (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)
JP2023578817A 2021-06-25 2022-06-24 ビス-ベンゾイミダゾールstingアゴニスト免疫複合体及びその使用 Pending JP2024523453A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163215100P 2021-06-25 2021-06-25
US63/215,100 2021-06-25
PCT/US2022/034865 WO2022272039A1 (en) 2021-06-25 2022-06-24 Bis-benzimidazole sting agonist immunoconjugates, and uses thereof

Publications (2)

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JP2024523453A true JP2024523453A (ja) 2024-06-28
JP2024523453A5 JP2024523453A5 (https=) 2025-06-16

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US (1) US20250057967A2 (https=)
EP (1) EP4359007A1 (https=)
JP (1) JP2024523453A (https=)
KR (1) KR20240027018A (https=)
CN (1) CN117794583A (https=)
AU (1) AU2022300383A1 (https=)
CA (1) CA3222082A1 (https=)
IL (1) IL309278A (https=)
WO (1) WO2022272039A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024137619A1 (en) * 2022-12-20 2024-06-27 Bolt Biotherapeutics, Inc. Anti-claudin, bis-benzimid azole sting agonist immunoconjugates, and uses thereof
WO2024174863A1 (zh) * 2023-02-22 2024-08-29 深圳众格生物科技有限公司 Sting激动剂及其制备方法和医药用途
WO2025029832A2 (en) 2023-07-31 2025-02-06 Sutro Biopharma, Inc. Sting agonist compounds and conjugates
CN117771206B (zh) * 2023-08-02 2024-05-28 首都医科大学附属北京儿童医院 Sting激动剂仿生纳米递送系统及其制备方法和应用
WO2025233676A1 (en) * 2024-05-08 2025-11-13 Ligachem Biosciences Inc. Compositions and methods related to a combination therapy of sting agonists and immune checkpoint inhibitors
WO2025233679A1 (en) * 2024-05-08 2025-11-13 Ligachem Biosciences Inc. Compositions and methods related to a combination therapy of sting agonists and antibody drug conjugates
US20260053942A1 (en) 2024-05-30 2026-02-26 Astellas Pharama Inc. Sting agonist immunostimulatory antibody drug conjugates
WO2026055185A1 (en) * 2024-09-04 2026-03-12 Bolt Biotherapeutics, Inc. Sting agonist immunoconjugates and uses thereof
WO2026078593A1 (en) 2024-10-08 2026-04-16 Sun Pharma Advanced Research Company Limited Sting agonists and antibody drug conjugates thereof

Citations (8)

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JP2019510796A (ja) * 2016-04-07 2019-04-18 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited タンパク質調節因子として有用な複素環式アミド
WO2020050406A1 (ja) * 2018-09-06 2020-03-12 第一三共株式会社 新規環状ジヌクレオチド誘導体及びその抗体薬物コンジュゲート
WO2020092617A1 (en) * 2018-10-31 2020-05-07 Novartis Ag Dc-sign antibody conjugates comprising sting agonists
JP2020517700A (ja) * 2017-04-28 2020-06-18 ノバルティス アーゲー Stingアゴニストを含む抗体コンジュゲート
WO2020229982A1 (en) * 2019-05-10 2020-11-19 Takeda Pharmaceutical Company Limited Antibody drug conjugates
JP2020536106A (ja) * 2017-10-05 2020-12-10 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited Hivの処置に有用なインターフェロン遺伝子の刺激物質(sting)の調節物質
WO2020252294A1 (en) * 2019-06-13 2020-12-17 Bolt Biotherapeutics, Inc. Aminobenzazepine compounds, immunoconjugates, and uses thereof
WO2021016204A1 (en) * 2019-07-19 2021-01-28 Immunesensor Therapeutics, Inc. Antibody-sting agonist conjugates and their use in immunotherapy

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JP2020517700A (ja) * 2017-04-28 2020-06-18 ノバルティス アーゲー Stingアゴニストを含む抗体コンジュゲート
JP2020536106A (ja) * 2017-10-05 2020-12-10 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited Hivの処置に有用なインターフェロン遺伝子の刺激物質(sting)の調節物質
WO2020050406A1 (ja) * 2018-09-06 2020-03-12 第一三共株式会社 新規環状ジヌクレオチド誘導体及びその抗体薬物コンジュゲート
WO2020092617A1 (en) * 2018-10-31 2020-05-07 Novartis Ag Dc-sign antibody conjugates comprising sting agonists
WO2020229982A1 (en) * 2019-05-10 2020-11-19 Takeda Pharmaceutical Company Limited Antibody drug conjugates
WO2020252294A1 (en) * 2019-06-13 2020-12-17 Bolt Biotherapeutics, Inc. Aminobenzazepine compounds, immunoconjugates, and uses thereof
WO2021016204A1 (en) * 2019-07-19 2021-01-28 Immunesensor Therapeutics, Inc. Antibody-sting agonist conjugates and their use in immunotherapy

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Publication number Publication date
WO2022272039A1 (en) 2022-12-29
IL309278A (en) 2024-02-01
CA3222082A1 (en) 2022-12-29
US20240335557A1 (en) 2024-10-10
US20250057967A2 (en) 2025-02-20
KR20240027018A (ko) 2024-02-29
EP4359007A1 (en) 2024-05-01
CN117794583A (zh) 2024-03-29
AU2022300383A1 (en) 2024-01-18

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