JP2022514348A - チオール多重リンカーを有するadc - Google Patents

チオール多重リンカーを有するadc Download PDF

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Publication number
JP2022514348A
JP2022514348A JP2021535547A JP2021535547A JP2022514348A JP 2022514348 A JP2022514348 A JP 2022514348A JP 2021535547 A JP2021535547 A JP 2021535547A JP 2021535547 A JP2021535547 A JP 2021535547A JP 2022514348 A JP2022514348 A JP 2022514348A
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Prior art keywords
group
antibody
drug
thiol
mla
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Japanese (ja)
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JPWO2020132655A5 (https=
JP2022514348A5 (https=
Inventor
スコット ジェフリー
クン-パーン ワング
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シージェン インコーポレイテッド
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Publication of JP2022514348A publication Critical patent/JP2022514348A/ja
Publication of JPWO2020132655A5 publication Critical patent/JPWO2020132655A5/ja
Publication of JP2022514348A5 publication Critical patent/JP2022514348A5/ja
Priority to JP2024163811A priority Critical patent/JP2024178320A/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2878Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95
    • 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
    • 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
    • A61K47/6849Medicinal 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
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/36Seven-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/515Complete light chain, i.e. VL + CL

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2021535547A 2018-12-21 2019-12-20 チオール多重リンカーを有するadc Ceased JP2022514348A (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024163811A JP2024178320A (ja) 2018-12-21 2024-09-20 チオール多重リンカーを有するadc

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862783582P 2018-12-21 2018-12-21
US201862783707P 2018-12-21 2018-12-21
US62/783,582 2018-12-21
US62/783,707 2018-12-21
PCT/US2019/068178 WO2020132655A1 (en) 2018-12-21 2019-12-20 Adcs with thiol multiplex linkers

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2024163811A Division JP2024178320A (ja) 2018-12-21 2024-09-20 チオール多重リンカーを有するadc

Publications (3)

Publication Number Publication Date
JP2022514348A true JP2022514348A (ja) 2022-02-10
JPWO2020132655A5 JPWO2020132655A5 (https=) 2022-12-20
JP2022514348A5 JP2022514348A5 (https=) 2022-12-20

Family

ID=71101991

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2021535547A Ceased JP2022514348A (ja) 2018-12-21 2019-12-20 チオール多重リンカーを有するadc
JP2024163811A Pending JP2024178320A (ja) 2018-12-21 2024-09-20 チオール多重リンカーを有するadc

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2024163811A Pending JP2024178320A (ja) 2018-12-21 2024-09-20 チオール多重リンカーを有するadc

Country Status (12)

Country Link
US (1) US20220040320A1 (https=)
EP (1) EP3897734A4 (https=)
JP (2) JP2022514348A (https=)
KR (1) KR20210141918A (https=)
CN (1) CN113543812A (https=)
AU (1) AU2019403552A1 (https=)
CA (1) CA3122316A1 (https=)
IL (1) IL284147A (https=)
MX (1) MX2021007548A (https=)
SG (1) SG11202106122QA (https=)
TW (1) TW202039008A (https=)
WO (1) WO2020132655A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021207701A1 (en) * 2020-04-10 2021-10-14 Seagen Inc. Charge variant linkers
CA3254333A1 (en) * 2022-05-18 2025-07-04 Systimmune, Inc. Ligand-drug conjugate and use thereof
AR132368A1 (es) 2023-04-18 2025-06-18 Astrazeneca Ab Conjugados que comprenden enlazadores escindibles

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007132998A1 (en) * 2006-05-12 2007-11-22 Korea Research Institute Of Bioscience And Biotechnology Linker molecules for substrate surface treatment and specific protein immobilization, and method for preparing the same
WO2008147481A1 (en) * 2007-02-09 2008-12-04 Northeastern University Precision-guided nanoparticle systems for drug delivery
JP2015521187A (ja) * 2012-05-15 2015-07-27 シアトル ジェネティクス,インコーポレイティド 自己安定化リンカー結合体
US20150231285A1 (en) * 2013-09-18 2015-08-20 Institute Of Nuclear Energy Research Atomic Energy Council, Executive Yuan Radiolabeled active targeting pharmaceutical composition and the use thereof
WO2016025752A1 (en) * 2014-08-14 2016-02-18 Prolynx Llc Reagents for thiol conjugation and conjugates formed therefrom

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE234635T1 (de) * 1995-12-22 2003-04-15 Bristol Myers Squibb Co Verzweigte hydrazongruppen enthaltende kuppler
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
DE10048417A1 (de) * 2000-09-29 2002-04-11 Roche Diagnostics Gmbh Verbindungen mit verzweigtem Linker
US6821529B2 (en) * 2001-09-05 2004-11-23 Deanna Jean Nelson Oligo(ethylene glycoll)-terminated 1,2-dithiolanes and their conjugates useful for preparing self-assembled monolayers
US20130195799A1 (en) * 2010-08-19 2013-08-01 Peg Biosciences, Inc. Synergistic biomolecule-polymer conjugates
EP3842074A1 (en) * 2010-09-29 2021-06-30 Philogen S.p.A. Protein-drug conjugates
US9981046B2 (en) * 2012-05-15 2018-05-29 Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. Drug-conjugates, conjugation methods, and uses thereof
PL2872157T3 (pl) * 2012-07-12 2020-07-13 Hangzhou Dac Biotech Co., Ltd Koniugaty wiążących komórkę cząsteczek ze środkami cytotoksycznymi
AU2014312215B2 (en) * 2013-08-28 2020-02-27 Abbvie Stemcentrx Llc Site-specific antibody conjugation methods and compositions
ES2826398T3 (es) * 2013-10-15 2021-05-18 Seagen Inc Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco
US11135307B2 (en) * 2016-11-23 2021-10-05 Mersana Therapeutics, Inc. Peptide-containing linkers for antibody-drug conjugates
WO2021207701A1 (en) * 2020-04-10 2021-10-14 Seagen Inc. Charge variant linkers

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007132998A1 (en) * 2006-05-12 2007-11-22 Korea Research Institute Of Bioscience And Biotechnology Linker molecules for substrate surface treatment and specific protein immobilization, and method for preparing the same
WO2008147481A1 (en) * 2007-02-09 2008-12-04 Northeastern University Precision-guided nanoparticle systems for drug delivery
JP2015521187A (ja) * 2012-05-15 2015-07-27 シアトル ジェネティクス,インコーポレイティド 自己安定化リンカー結合体
US20150231285A1 (en) * 2013-09-18 2015-08-20 Institute Of Nuclear Energy Research Atomic Energy Council, Executive Yuan Radiolabeled active targeting pharmaceutical composition and the use thereof
WO2016025752A1 (en) * 2014-08-14 2016-02-18 Prolynx Llc Reagents for thiol conjugation and conjugates formed therefrom

Also Published As

Publication number Publication date
EP3897734A1 (en) 2021-10-27
JP2024178320A (ja) 2024-12-24
US20220040320A1 (en) 2022-02-10
CN113543812A (zh) 2021-10-22
AU2019403552A1 (en) 2021-06-17
MX2021007548A (es) 2021-12-10
SG11202106122QA (en) 2021-07-29
EP3897734A4 (en) 2022-12-07
TW202039008A (zh) 2020-11-01
WO2020132655A1 (en) 2020-06-25
IL284147A (en) 2021-08-31
CA3122316A1 (en) 2020-06-25
KR20210141918A (ko) 2021-11-23

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