CN107073131B - 缀合物和缀合试剂 - Google Patents

缀合物和缀合试剂 Download PDF

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Publication number
CN107073131B
CN107073131B CN201580057559.0A CN201580057559A CN107073131B CN 107073131 B CN107073131 B CN 107073131B CN 201580057559 A CN201580057559 A CN 201580057559A CN 107073131 B CN107073131 B CN 107073131B
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group
polyethylene glycol
conjugate
antibody
formula
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Chinese (zh)
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CN107073131A (zh
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A·戈德温
M·弗里赫里奥
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Abu Zena Uk Ltd
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Polytherics Ltd
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Priority claimed from GBGB1418989.8A external-priority patent/GB201418989D0/en
Priority claimed from GB1418984.9A external-priority patent/GB2531715A/en
Priority claimed from GBGB1418986.4A external-priority patent/GB201418986D0/en
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Publication of CN107073131A publication Critical patent/CN107073131A/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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • 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
    • 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
    • A61K47/6889—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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cell Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201580057559.0A 2014-10-24 2015-10-08 缀合物和缀合试剂 Active CN107073131B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GBGB1418989.8A GB201418989D0 (en) 2014-10-24 2014-10-24 Novel conjugation process and reagents
GB1418984.9A GB2531715A (en) 2014-10-24 2014-10-24 Novel drug conjugates
GB1418984.9 2014-10-24
GB1418986.4 2014-10-24
GBGB1418986.4A GB201418986D0 (en) 2014-10-24 2014-10-24 Novel conjugates and novel conjugating reagents
GB1418989.8 2014-10-24
PCT/GB2015/052953 WO2016063006A1 (en) 2014-10-24 2015-10-08 Conjugates and conjugating reagents

Publications (2)

Publication Number Publication Date
CN107073131A CN107073131A (zh) 2017-08-18
CN107073131B true CN107073131B (zh) 2021-05-25

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CN201580057559.0A Active CN107073131B (zh) 2014-10-24 2015-10-08 缀合物和缀合试剂

Country Status (15)

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US (3) US20170290925A1 (enExample)
EP (1) EP3220956B1 (enExample)
JP (1) JP6612860B2 (enExample)
KR (1) KR102513926B1 (enExample)
CN (1) CN107073131B (enExample)
AU (1) AU2015334717B2 (enExample)
BR (1) BR112017005760A2 (enExample)
CA (1) CA2963043A1 (enExample)
ES (1) ES2960741T3 (enExample)
IL (1) IL250644B (enExample)
MX (1) MX2017005199A (enExample)
RU (1) RU2017108448A (enExample)
SG (1) SG11201701342XA (enExample)
WO (1) WO2016063006A1 (enExample)
ZA (1) ZA201701337B (enExample)

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US10098960B2 (en) 2015-04-03 2018-10-16 Ucl Business Plc Polymer conjugate
CN108473590B (zh) 2016-01-12 2023-04-14 克雷森多生物制剂有限公司 治疗分子
WO2017161206A1 (en) 2016-03-16 2017-09-21 Halozyme, Inc. Conjugates containing conditionally active antibodies or antigen-binding fragments thereof, and methods of use
US11273224B2 (en) 2016-04-14 2022-03-15 Polytherics Limited Conjugates and conjugating reagents comprising a linker that includes at least two (-CH2—CH2—O-) units in a ring
GB201608936D0 (en) * 2016-05-20 2016-07-06 Polytherics Ltd Novel conjugates and novel conjugating reagents
CN109311996B (zh) 2016-06-06 2023-11-28 阿布泽纳(英国)有限公司 抗体、其用途及其缀合物
GB201614162D0 (en) * 2016-08-18 2016-10-05 Polytherics Ltd Antibodies, uses thereof and conjugates thereof
GB201615725D0 (en) 2016-09-15 2016-11-02 Polytherics Ltd Novel cytotoxic agents and conjugates thereof
US11419946B2 (en) 2017-03-30 2022-08-23 Nof Corporation Heterobifunctional monodispersed polyethylene glycol and conjugate using same
GB201711068D0 (en) 2017-07-10 2017-08-23 Crescendo Biologics Ltd Therapeutic molecules binding PSMA
EP3766917B1 (en) 2018-03-13 2023-04-19 NOF Corporation Heterobifunctional compound having monodispersed polyethylene glycol in main chain or side chain
EP3789401A1 (en) 2019-09-03 2021-03-10 Gamamabs Pharma Amhrii-binding antibody drug conjugates and their use thereof in the treatment of cancers
AU2021262526A1 (en) * 2020-04-29 2022-11-03 Araclon Biotech, S.L. Methods for quantification of amyloid beta peptides in plasma by mass spectrometry
GB2594753B (en) 2020-05-27 2022-05-18 Spirea Ltd Antibody-drug conjugates
WO2023047090A1 (en) 2021-09-21 2023-03-30 Spirea Limited Antibody-drug conjugates

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WO1999045964A1 (en) * 1998-03-12 1999-09-16 Shearwater Polymers, Incorporated Poly(ethylene glycol) derivatives with proximal reactive groups
CN1085689C (zh) * 1993-11-12 2002-05-29 舍沃特聚合物公司 可分离的水溶性和水解稳定的活性聚乙二醇砜及有关的聚合物用于表面和分子的改性
KR20030037598A (ko) * 2001-11-06 2003-05-14 선바이오(주) 변형된 인터페론-베타, 및 이의 화학적으로 변형된 배합체
WO2011077067A1 (en) * 2009-12-21 2011-06-30 Polytherics Limited Polymer conjugates of non-glycosylated erythropoietin
CN103384534A (zh) * 2011-02-25 2013-11-06 隆萨有限公司 用于蛋白质药物偶联物的支链联接体
WO2013190272A1 (en) * 2012-06-18 2013-12-27 Polytherics Limited Conjugation reagents
WO2013190292A3 (en) * 2012-06-19 2014-03-20 Polytherics Limited Novel process for preparation of antibody conjugates and novel antibody conjugates
WO2014064423A1 (en) * 2012-10-24 2014-05-01 Polytherics Limited Drug-protein conjugates

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Publication number Priority date Publication date Assignee Title
CN1085689C (zh) * 1993-11-12 2002-05-29 舍沃特聚合物公司 可分离的水溶性和水解稳定的活性聚乙二醇砜及有关的聚合物用于表面和分子的改性
WO1999045964A1 (en) * 1998-03-12 1999-09-16 Shearwater Polymers, Incorporated Poly(ethylene glycol) derivatives with proximal reactive groups
KR20030037598A (ko) * 2001-11-06 2003-05-14 선바이오(주) 변형된 인터페론-베타, 및 이의 화학적으로 변형된 배합체
WO2011077067A1 (en) * 2009-12-21 2011-06-30 Polytherics Limited Polymer conjugates of non-glycosylated erythropoietin
CN103384534A (zh) * 2011-02-25 2013-11-06 隆萨有限公司 用于蛋白质药物偶联物的支链联接体
WO2013190272A1 (en) * 2012-06-18 2013-12-27 Polytherics Limited Conjugation reagents
WO2013190292A3 (en) * 2012-06-19 2014-03-20 Polytherics Limited Novel process for preparation of antibody conjugates and novel antibody conjugates
WO2014064423A1 (en) * 2012-10-24 2014-05-01 Polytherics Limited Drug-protein conjugates

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Also Published As

Publication number Publication date
EP3220956A1 (en) 2017-09-27
AU2015334717A1 (en) 2017-04-13
KR20170075724A (ko) 2017-07-03
JP6612860B2 (ja) 2019-11-27
SG11201701342XA (en) 2017-03-30
ZA201701337B (en) 2018-05-30
US20240293549A1 (en) 2024-09-05
CN107073131A (zh) 2017-08-18
MX2017005199A (es) 2017-07-26
BR112017005760A2 (pt) 2017-12-12
RU2017108448A (ru) 2018-11-27
AU2015334717B2 (en) 2021-02-25
ES2960741T3 (es) 2024-03-06
KR102513926B1 (ko) 2023-03-23
CA2963043A1 (en) 2016-04-28
EP3220956B1 (en) 2023-08-09
JP2017537062A (ja) 2017-12-14
IL250644B (en) 2020-10-29
US20200268885A1 (en) 2020-08-27
US20170290925A1 (en) 2017-10-12
WO2016063006A1 (en) 2016-04-28
IL250644A0 (en) 2017-06-29

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