CN115515644A - 一种抗体-药物偶联物，其制备方法及应用 - Google Patents

一种抗体-药物偶联物，其制备方法及应用 Download PDF

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Publication number
CN115515644A
CN115515644A CN202180034171.4A CN202180034171A CN115515644A CN 115515644 A CN115515644 A CN 115515644A CN 202180034171 A CN202180034171 A CN 202180034171A CN 115515644 A CN115515644 A CN 115515644A
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China
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antibody
drug conjugate
formula
group
stereoisomer
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CN202180034171.4A
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English (en)
Inventor
柯天一
丁会
劳芳
于海勇
刘岩
张西东
檀琳
姚德惠
欧阳芳幸
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Kunshan Xinyunda Biotech Co ltd
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Kunshan Xinyunda Biotech Co ltd
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Publication of CN115515644A publication Critical patent/CN115515644A/zh
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • 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 [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)

Abstract

一种抗体‑药物偶联物、其制备方法及应用。所述的抗体‑药物偶联物是将式(I)表示的化合物与抗体经由式(II)表示的接头、通过由存在于抗体的铰链部的二硫键部分形成的硫醚键连接而形成的式(V)表示的抗体‑药物偶联物。所述抗体‑药物偶联物具有更快起效时间、更长药物半衰期、更适中的稳定性、良好的生物相容性、低免疫原性和安全性，并且可以防止聚集，该抗体‑药物偶联物具有优异的抗肿瘤效果。

Description

PCT国内申请，说明书已公开。

Claims (20)

  1. PCT国内申请，权利要求书已公开。
CN202180034171.4A 2020-06-28 2021-06-25 一种抗体-药物偶联物，其制备方法及应用 Pending CN115515644A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN202010601193 2020-06-28
CN2020106011931 2020-06-28
CN202010664259 2020-07-10
CN2020106642591 2020-07-10
PCT/CN2021/102332 WO2022001864A1 (zh) 2020-06-28 2021-06-25 一种抗体-药物偶联物，其制备方法及应用

Publications (1)

Publication Number Publication Date
CN115515644A true CN115515644A (zh) 2022-12-23

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Application Number Title Priority Date Filing Date
CN202180034171.4A Pending CN115515644A (zh) 2020-06-28 2021-06-25 一种抗体-药物偶联物，其制备方法及应用

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CN (1) CN115515644A (zh)
WO (1) WO2022001864A1 (zh)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11806405B1 (en) * 2021-07-19 2023-11-07 Zeno Management, Inc. Immunoconjugates and methods
JP2024532295A (ja) * 2021-08-24 2024-09-05 クンシャン シンユンター バイオテック カンパニー，リミティド 切断可能なリンカーを介して結合した抗体薬物複合体
WO2023214849A1 (ko) * 2022-05-04 2023-11-09 주식회사 피노바이오 Ddx5 단백질에 결합하는 캄토테신계 약물이 산 민감성 링커에 연결된 접합체 및 이를 이용한 면역접합체
KR20240001074A (ko) * 2022-06-24 2024-01-03 주식회사 피노바이오 하나의 항체에 2종의 약물-링커 접합체가 연결된 항체-약물접합체
WO2024008102A1 (en) * 2022-07-05 2024-01-11 Wuxi Xdc (Shanghai) Co., Ltd. Linker for conjugation
CN117917248A (zh) * 2022-10-20 2024-04-23 英诺湖医药(杭州)有限公司 酶裂解连接子及包含其的配体-艾瑞布林偶联物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7591994B2 (en) * 2002-12-13 2009-09-22 Immunomedics, Inc. Camptothecin-binding moiety conjugates
PT3903829T (pt) * 2009-02-13 2023-06-02 Immunomedics Inc Imunoconjugados com uma ligação intracelular clivável
US10744129B2 (en) * 2012-12-13 2020-08-18 Immunomedics, Inc. Therapy of small-cell lung cancer (SCLC) with a topoisomerase-I inhibiting antibody-drug conjugate (ADC) targeting Trop-2
MX2016008192A (es) * 2013-12-25 2017-02-27 Daiichi Sankyo Co Ltd Conjugado anticuerpo anti-trop2-farmaco.
RS62618B1 (sr) * 2014-01-31 2021-12-31 Daiichi Sankyo Co Ltd Anti-her2 antitelo-lek konjugat
CN110903395A (zh) * 2018-09-14 2020-03-24 四川科伦博泰生物医药股份有限公司 抗体、偶联物及其制备方法和用途

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