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 GBGB1418986.4A external-priority patent/GB201418986D0/en
Priority claimed from GB1418984.9A external-priority patent/GB2531715A/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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
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
GBGB1418989.8A GB201418989D0 (en) 2014-10-24 2014-10-24 Novel conjugation process and reagents
GB1418986.4 2014-10-24
GB1418984.9 2014-10-24
GB1418989.8 2014-10-24
GBGB1418986.4A GB201418986D0 (en) 2014-10-24 2014-10-24 Novel conjugates and novel conjugating reagents
GB1418984.9A GB2531715A (en) 2014-10-24 2014-10-24 Novel drug conjugates
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
JP2019506155A (ja) 2016-01-12 2019-03-07 クレッシェンド、バイオロジックス、リミテッドＣｒｅｓｃｅｎｄｏ Ｂｉｏｌｏｇｉｃｓ Ｌｉｍｉｔｅｄ 治療分子
WO2017161206A1 (en) 2016-03-16 2017-09-21 Halozyme, Inc. Conjugates containing conditionally active antibodies or antigen-binding fragments thereof, and methods of use
WO2017178828A1 (en) * 2016-04-14 2017-10-19 Polytherics Limited Conjugates and conjugating reagents comprising a linker that includes at least two (-ch2-ch2-0-) units in a ring
GB201608936D0 (en) * 2016-05-20 2016-07-06 Polytherics Ltd Novel conjugates and novel conjugating reagents
US11485792B2 (en) 2016-06-06 2022-11-01 Polytherics 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
US12091502B2 (en) 2018-03-13 2024-09-17 Nof Corporation Heterobifunctional compound having monodispersed polyethylene glycol in main chain and 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
KR20230002465A (ko) * 2020-04-29 2023-01-05 아라클론 바이오테크, 에스.엘. 질량 분석법에 의한 혈장에서의 아밀로이드 베타 펩티드의 정량화를 위한 방법
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

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
US6362254B2 (en) * 1998-03-12 2002-03-26 Shearwater Corporation Poly(ethylene glycol) derivatives with proximal reactive groups
KR100511749B1 (ko) * 2001-11-06 2005-09-02 선바이오(주) 변형된 인터페론-베타, 및 이의 화학적으로 변형된 배합체
EP3434275A1 (en) * 2003-11-06 2019-01-30 Seattle Genetics, Inc. Assay for cancer cells based on the use of auristatin conjugates with antibodies
US8158590B2 (en) * 2005-08-05 2012-04-17 Syntarga B.V. Triazole-containing releasable linkers, conjugates thereof, and methods of preparation
US20070141134A1 (en) * 2005-12-16 2007-06-21 Kosak Matthew K Shielded micelles for polynucleotide delivery
EP2073820A4 (en) * 2006-09-15 2014-07-16 Belrose Pharma Inc TARGETED POLYMER PRODRUGS WITH MULTIFUNCTIONAL CONNECTORS
WO2008098930A1 (en) * 2007-02-14 2008-08-21 Biocompatibes Uk Limited Derivatisation of biological molecules
GB0922354D0 (en) * 2009-12-21 2010-02-03 Polytherics Ltd Novel polymer conjugates
ES2531471T3 (es) * 2011-02-25 2015-03-16 Lonza Ltd Enlazador ramificado para conjugados de proteínas-fármacos
CN103384534B (zh) * 2011-02-25 2015-09-30 隆萨有限公司 用于蛋白质药物偶联物的支链联接体
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
US20150290342A1 (en) * 2012-10-24 2015-10-15 Polytherics Limited Drug-protein conjugates
NO2789793T3 (enExample) * 2012-10-24 2018-01-27
AU2014337555C1 (en) * 2013-10-15 2021-01-28 Seagen Inc. PEGylated drug-linkers for improved Ligand-Drug Conjugate pharmacokinetics

Also Published As

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

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20191009