CN117794583A - 双苯并咪唑sting激动剂免疫缀合物及其用途 - Google Patents

双苯并咪唑sting激动剂免疫缀合物及其用途 Download PDF

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Publication number
CN117794583A
CN117794583A CN202280053551.7A CN202280053551A CN117794583A CN 117794583 A CN117794583 A CN 117794583A CN 202280053551 A CN202280053551 A CN 202280053551A CN 117794583 A CN117794583 A CN 117794583A
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CN
China
Prior art keywords
alkyldiyl
peg
immunoconjugate
antibody
pep
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Pending
Application number
CN202280053551.7A
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English (en)
Chinese (zh)
Inventor
G·勃兰特
R·库迪尔卡
B·萨芬娜
M·周
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Bolt Biotherapeutics Inc
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Bolt Biotherapeutics Inc
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Publication of CN117794583A publication Critical patent/CN117794583A/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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K47/56—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 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
    • A61K47/60—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 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
    • 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
    • A61K47/6851—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 determinant of a tumour cell
    • 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
    • A61K47/6851—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 determinant of a tumour cell
    • A61K47/6853—Carcino-embryonic antigens
    • 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

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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)
CN202280053551.7A 2021-06-25 2022-06-24 双苯并咪唑sting激动剂免疫缀合物及其用途 Pending CN117794583A (zh)

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 (1)

Publication Number Publication Date
CN117794583A true CN117794583A (zh) 2024-03-29

Family

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CN202280053551.7A Pending CN117794583A (zh) 2021-06-25 2022-06-24 双苯并咪唑sting激动剂免疫缀合物及其用途

Country Status (9)

Country Link
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

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3440076T (pt) * 2016-04-07 2022-07-29 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas úteis como modeladores de proteína
AR113224A1 (es) * 2017-04-28 2020-02-19 Novartis Ag Conjugados de anticuerpo que comprenden un agonista de sting
CA3077337A1 (en) * 2017-10-05 2019-04-11 Glaxosmithkline Intellectual Property Development Limited Modulators of stimulator of interferon genes (sting)
AU2018344902B2 (en) * 2017-10-05 2021-06-03 Glaxosmithkline Intellectual Property Development Limited Modulators of stimulator of interferon genes (STING) useful in treating HIV
EP3848054B1 (en) * 2018-09-06 2025-01-29 Daiichi Sankyo Company, Limited Antibody-drug conjugates of cyclic dinucleotide derivatives
WO2020092617A1 (en) * 2018-10-31 2020-05-07 Novartis Ag Dc-sign antibody conjugates comprising sting agonists
WO2020214858A1 (en) * 2019-04-17 2020-10-22 Avidea Technologies, Inc. Compositions and methods of manufacturing star polymers for ligand display and/or drug delivery
IL287938B2 (en) * 2019-05-10 2025-07-01 Takeda Pharmaceuticals Co Antibody-drug conjugates
US20200390899A1 (en) * 2019-06-13 2020-12-17 Bolt Biotherapeutics, Inc. Aminobenzazepine compounds, immunoconjugates, and uses thereof
CA3147890A1 (en) * 2019-07-19 2021-01-28 Immunesensor Therapeutics, Inc. Antibody-sting agonist conjugates and their use in immunotherapy
IL296901A (en) * 2020-04-02 2022-12-01 Mersana Therapeutics Inc Antibody-drug conjugates comprising sting agonists

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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
JP2024523453A (ja) 2024-06-28
EP4359007A1 (en) 2024-05-01
AU2022300383A1 (en) 2024-01-18

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