CA2963043A1 - Conjugates and conjugating reagents - Google Patents

Conjugates and conjugating reagents Download PDF

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Publication number
CA2963043A1
CA2963043A1 CA2963043A CA2963043A CA2963043A1 CA 2963043 A1 CA2963043 A1 CA 2963043A1 CA 2963043 A CA2963043 A CA 2963043A CA 2963043 A CA2963043 A CA 2963043A CA 2963043 A1 CA2963043 A1 CA 2963043A1
Authority
CA
Canada
Prior art keywords
group
protein
conjugate
peptide
polyethylene glycol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2963043A
Other languages
English (en)
French (fr)
Inventor
Antony Godwin
Mark Frigerio
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abzena UK Ltd
Original Assignee
Polytherics Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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
Application filed by Polytherics Ltd filed Critical Polytherics Ltd
Publication of CA2963043A1 publication Critical patent/CA2963043A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K47/50—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (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)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
CA2963043A 2014-10-24 2015-10-08 Conjugates and conjugating reagents Abandoned CA2963043A1 (en)

Applications Claiming Priority (7)

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

Publications (1)

Publication Number Publication Date
CA2963043A1 true CA2963043A1 (en) 2016-04-28

Family

ID=54337308

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2963043A Abandoned CA2963043A1 (en) 2014-10-24 2015-10-08 Conjugates and conjugating reagents

Country Status (15)

Country Link
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)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10098960B2 (en) 2015-04-03 2018-10-16 Ucl Business Plc Polymer conjugate
US11236174B2 (en) 2016-01-12 2022-02-01 Crescendo Biologics Limited Therapeutic molecules
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
EP3464379B1 (en) 2016-06-06 2023-09-27 Abzena (UK) Limited Antibodies, uses thereof and conjugates thereof
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
EP3604385B1 (en) 2017-03-30 2024-05-01 NOF Corporation Heterobifunctional monodispersed polyethylene glycol and conjugate using the same
GB201711068D0 (en) 2017-07-10 2017-08-23 Crescendo Biologics Ltd Therapeutic molecules binding PSMA
KR102542988B1 (ko) 2018-03-13 2023-06-13 니치유 가부시키가이샤 주쇄 및 측쇄에 단분산 폴리에틸렌 글리콜을 가지는 헤테로이관능성 화합물
EP3789401A1 (en) 2019-09-03 2021-03-10 Gamamabs Pharma Amhrii-binding antibody drug conjugates and their use thereof in the treatment of cancers
MX2022012703A (es) * 2020-04-29 2022-11-07 Araclon Biotech Sl Procedimientos para la cuantificacion de peptidos beta amiloides en plasma mediante espectrometria de masas.
GB2594753B (en) 2020-05-27 2022-05-18 Spirea Ltd Antibody-drug conjugates
EP4404974A1 (en) 2021-09-21 2024-07-31 Spirea Limited Antibody-drug conjugates

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5446090A (en) * 1993-11-12 1995-08-29 Shearwater Polymers, Inc. Isolatable, water soluble, and hydrolytically stable active sulfones of poly(ethylene glycol) and related polymers for modification of surfaces and molecules
EP1411075B1 (en) * 1998-03-12 2008-07-02 Nektar Therapeutics Al, Corporation Method for preparing polymer conjugates
KR100511749B1 (ko) * 2001-11-06 2005-09-02 선바이오(주) 변형된 인터페론-베타, 및 이의 화학적으로 변형된 배합체
DK1725249T3 (en) * 2003-11-06 2014-03-17 Seattle Genetics Inc Monomethylvaline compounds capable of conjugating to ligands.
EP1909846B1 (en) * 2005-08-05 2018-12-26 Syntarga B.V. Triazole-containing releasable linkers, conjugates comprising the same and processes for their preparation
US20070141134A1 (en) * 2005-12-16 2007-06-21 Kosak Matthew K Shielded micelles for polynucleotide delivery
KR20090057383A (ko) * 2006-09-15 2009-06-05 엔존 파마슈티컬즈, 인코포레이티드 다기능성 링커를 포함하는 표적화된 고분자 전구약물
EP2118150B1 (en) * 2007-02-14 2015-09-23 Biocompatibles UK Limited Derivatisation of biological molecules
GB0922354D0 (en) * 2009-12-21 2010-02-03 Polytherics Ltd Novel polymer conjugates
CN104906592B (zh) * 2011-02-25 2017-11-03 广州南沙龙沙有限公司 用于蛋白质药物偶联物的支链联接体
EP2678037B1 (en) * 2011-02-25 2014-12-03 Lonza Ltd Branched linker for protein drug conjugates
US9650331B2 (en) * 2012-06-18 2017-05-16 Polytherics Limited Conjugation reagents
GB201210770D0 (en) * 2012-06-18 2012-08-01 Polytherics Ltd Novel conjugation reagents
SG11201407600UA (en) * 2012-06-19 2014-12-30 Polytherics Ltd Novel process for preparation of antibody conjugates and novel antibody conjugates
ES2623209T3 (es) * 2012-10-24 2017-07-10 Polytherics Limited Conjugados fármaco-proteína
NO2789793T3 (enExample) * 2012-10-24 2018-01-27
CA3187392A1 (en) * 2013-10-15 2015-04-23 Seagen Inc. Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics

Also Published As

Publication number Publication date
AU2015334717A1 (en) 2017-04-13
CN107073131A (zh) 2017-08-18
AU2015334717B2 (en) 2021-02-25
IL250644A0 (en) 2017-06-29
SG11201701342XA (en) 2017-03-30
US20240293549A1 (en) 2024-09-05
RU2017108448A (ru) 2018-11-27
BR112017005760A2 (pt) 2017-12-12
ZA201701337B (en) 2018-05-30
MX2017005199A (es) 2017-07-26
EP3220956B1 (en) 2023-08-09
ES2960741T3 (es) 2024-03-06
EP3220956A1 (en) 2017-09-27
IL250644B (en) 2020-10-29
JP2017537062A (ja) 2017-12-14
CN107073131B (zh) 2021-05-25
KR102513926B1 (ko) 2023-03-23
US20170290925A1 (en) 2017-10-12
JP6612860B2 (ja) 2019-11-27
US20200268885A1 (en) 2020-08-27
WO2016063006A1 (en) 2016-04-28
KR20170075724A (ko) 2017-07-03

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20191009

FZDE Discontinued

Effective date: 20191009