KR102349925B1 - Fl118 약물을 포함하는 화합물 및 이를 이용한 면역접합체 - Google Patents

Fl118 약물을 포함하는 화합물 및 이를 이용한 면역접합체 Download PDF

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KR102349925B1
KR102349925B1 KR1020210060721A KR20210060721A KR102349925B1 KR 102349925 B1 KR102349925 B1 KR 102349925B1 KR 1020210060721 A KR1020210060721 A KR 1020210060721A KR 20210060721 A KR20210060721 A KR 20210060721A KR 102349925 B1 KR102349925 B1 KR 102349925B1
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immunoconjugate
cancer
drug
linker
antibody
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Korean (ko)
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정두영
이진수
조현용
최신혜
이병성
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주식회사 피노바이오
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Priority to CN202180062303.4A priority Critical patent/CN116075321A/zh
Priority to US18/016,331 priority patent/US20230270867A1/en
Priority to CA3189462A priority patent/CA3189462A1/en
Priority to PCT/KR2021/009204 priority patent/WO2022015110A1/ko
Priority to JP2023503070A priority patent/JP7660186B2/ja
Priority to EP21841752.5A priority patent/EP4183418A4/en
Priority to AU2021308834A priority patent/AU2021308834A1/en
Priority to KR1020210137595A priority patent/KR102857180B1/ko
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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
    • A61K47/6889—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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K47/54—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 compound
    • A61K47/545—Heterocyclic compounds
    • 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
    • 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
    • A61K47/68037—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
    • 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
    • A61K47/6835—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
    • A61K47/6855—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 the tumour determinant being from breast cancer cell
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020210060721A 2020-07-16 2021-05-11 Fl118 약물을 포함하는 화합물 및 이를 이용한 면역접합체 Active KR102349925B1 (ko)

Priority Applications (8)

Application Number Priority Date Filing Date Title
US18/016,331 US20230270867A1 (en) 2020-07-16 2021-07-16 Conjugate in which fl118 drug is linked to acid-sensitive linker, and immunoconjugate using same
CA3189462A CA3189462A1 (en) 2020-07-16 2021-07-16 Conjugate in which fl118 drug is linked to acid-sensitive linker, and immunoconjugate using the same
PCT/KR2021/009204 WO2022015110A1 (ko) 2020-07-16 2021-07-16 Fl118 약물이 산 민감성 링커에 연결된 접합체 및 이를 이용한 면역접합체
JP2023503070A JP7660186B2 (ja) 2020-07-16 2021-07-16 Ｆｌ１１８薬物が酸感受性リンカーに結合された複合体及びそれを用いた免疫複合体
CN202180062303.4A CN116075321A (zh) 2020-07-16 2021-07-16 Fl118药物与酸敏感接头连接的缀合物，以及使用该缀合物的免疫缀合物
EP21841752.5A EP4183418A4 (en) 2020-07-16 2021-07-16 Conjugate in which fl118 drug is linked to acid-sensitive linker, and immunoconjugate using same
AU2021308834A AU2021308834A1 (en) 2020-07-16 2021-07-16 Conjugate in which FL118 drug is linked to acid-sensitive linker, and immunoconjugate using same
KR1020210137595A KR102857180B1 (ko) 2020-07-16 2021-10-15 Fl118 약물을 포함하는 면역접합체

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20200088005 2020-07-16
KR1020200088005 2020-07-16

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020210137595A Division KR102857180B1 (ko) 2020-07-16 2021-10-15 Fl118 약물을 포함하는 면역접합체

Publications (1)

Publication Number Publication Date
KR102349925B1 true KR102349925B1 (ko) 2022-01-12

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Family Applications (3)

Application Number Title Priority Date Filing Date
KR1020210060721A Active KR102349925B1 (ko) 2020-07-16 2021-05-11 Fl118 약물을 포함하는 화합물 및 이를 이용한 면역접합체
KR1020210093769A Ceased KR20220009916A (ko) 2020-07-16 2021-07-16 Fl118 약물이 산 민감성 링커에 연결된 접합체 및 이를 이용한 면역접합체
KR1020210137595A Active KR102857180B1 (ko) 2020-07-16 2021-10-15 Fl118 약물을 포함하는 면역접합체

Family Applications After (2)

Application Number Title Priority Date Filing Date
KR1020210093769A Ceased KR20220009916A (ko) 2020-07-16 2021-07-16 Fl118 약물이 산 민감성 링커에 연결된 접합체 및 이를 이용한 면역접합체
KR1020210137595A Active KR102857180B1 (ko) 2020-07-16 2021-10-15 Fl118 약물을 포함하는 면역접합체

Country Status (8)

Country Link
US (1) US20230270867A1 (https=)
EP (1) EP4183418A4 (https=)
JP (1) JP7660186B2 (https=)
KR (3) KR102349925B1 (https=)
CN (1) CN116075321A (https=)
AU (1) AU2021308834A1 (https=)
CA (1) CA3189462A1 (https=)
WO (1) WO2022015110A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024049220A1 (ko) 2022-08-30 2024-03-07 주식회사 피노바이오 캄토테신계 약물이, 항원 결합 친화도가 낮은 항체에 링커를 통해 연결된 항체-약물 접합체

Families Citing this family (4)

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Publication number Priority date Publication date Assignee Title
CN119546346A (zh) * 2022-05-04 2025-02-28 匹诺生物股份有限公司 与ddx5蛋白结合的喜树碱类药物与酸敏感性接头连接的缀合物及使用该缀合物的免疫缀合物
JP2025523863A (ja) * 2022-07-11 2025-07-25 ピノットバイオ インコーポレイテッド Ｄｄｘ５タンパク質に結合するカンプトセシン誘導体およびそのプロドラッグ
KR20250163350A (ko) * 2023-03-28 2025-11-20 한서 바이오 엘엘씨 리간드-세포 독성 약물 접합체 및 이의 약학적 용도
WO2025170834A1 (en) * 2024-02-06 2025-08-14 Canget Biotekpharma, Llc Fl118 complexes for targeting ddx5, ube2t or usp2a

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US20170360770A1 (en) * 2012-12-13 2017-12-21 Immunomedics, Inc. EFFICACY OF ANTI-HLA-DR ANTIBODY DRUG CONJUGATE IMMU-140 (hL243-CL2A-SN-38) IN HLA-DR POSITIVE CANCERS
US20180170944A1 (en) * 2014-03-26 2018-06-21 Canget Biotekpharma, Llc Use of the fl-one hundred eighteen core chemical structure platform to generate fl-one hundred eighteen derivatives for treatment of human disease

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SI2900277T1 (sl) * 2012-12-13 2022-05-31 Immunomedics, Inc. Odmerki imunokonjugatov protiteles in SN-38 za boljšo učinkovitost in zmanjšano toksičnost
WO2015012904A2 (en) * 2012-12-13 2015-01-29 Immunomedics, Inc. Antibody-sn-38 immunoconjugates with a cl2a linker
AU2014293670B2 (en) 2013-07-23 2019-08-01 Immunomedics, Inc. Antibody-SN-38 immunoconjugates with a CL2A linker
SI3466976T1 (sl) 2014-01-31 2021-12-31 Daiichi Sankyo Company, Limited Anti-her2 konjugat protitelesa-zdravila
TWI851577B (zh) 2018-06-07 2024-08-11 美商思進公司 喜樹鹼結合物

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US20170360770A1 (en) * 2012-12-13 2017-12-21 Immunomedics, Inc. EFFICACY OF ANTI-HLA-DR ANTIBODY DRUG CONJUGATE IMMU-140 (hL243-CL2A-SN-38) IN HLA-DR POSITIVE CANCERS
US20180170944A1 (en) * 2014-03-26 2018-06-21 Canget Biotekpharma, Llc Use of the fl-one hundred eighteen core chemical structure platform to generate fl-one hundred eighteen derivatives for treatment of human disease

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WO2024049220A1 (ko) 2022-08-30 2024-03-07 주식회사 피노바이오 캄토테신계 약물이, 항원 결합 친화도가 낮은 항체에 링커를 통해 연결된 항체-약물 접합체

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JP2023534292A (ja) 2023-08-08
AU2021308834A2 (en) 2023-10-19
WO2022015110A1 (ko) 2022-01-20
KR102857180B1 (ko) 2025-09-09
US20230270867A1 (en) 2023-08-31
CA3189462A1 (en) 2022-01-20
KR20220009916A (ko) 2022-01-25
JP7660186B2 (ja) 2025-04-10
AU2021308834A1 (en) 2023-02-16
KR20220009928A (ko) 2022-01-25
CN116075321A (zh) 2023-05-05
EP4183418A4 (en) 2025-02-12
EP4183418A1 (en) 2023-05-24

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