BR112017005760A2 - conjugados e reagentes de conjugação - Google Patents

conjugados e reagentes de conjugação

Info

Publication number
BR112017005760A2
BR112017005760A2 BR112017005760A BR112017005760A BR112017005760A2 BR 112017005760 A2 BR112017005760 A2 BR 112017005760A2 BR 112017005760 A BR112017005760 A BR 112017005760A BR 112017005760 A BR112017005760 A BR 112017005760A BR 112017005760 A2 BR112017005760 A2 BR 112017005760A2
Authority
BR
Brazil
Prior art keywords
protein
peptide
group
polyethylene glycol
conjugate
Prior art date
Application number
BR112017005760A
Other languages
English (en)
Inventor
Godwin Antony
Frigerio Mark
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 GB1418984.9A external-priority patent/GB2531715A/en
Priority claimed from GBGB1418986.4A external-priority patent/GB201418986D0/en
Priority claimed from GBGB1418989.8A external-priority patent/GB201418989D0/en
Application filed by Polytherics Ltd filed Critical Polytherics Ltd
Publication of BR112017005760A2 publication Critical patent/BR112017005760A2/pt

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
    • 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
    • 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
    • A61K47/62—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)

Abstract

a presente invenção refere-se a um conjugado de uma proteína ou peptídeo com um agente terapêutico, de diagnóstico ou de rotulagem, o referido conjugado contendo uma porção de ligação de proteína ou peptídeo e uma porção de polietileno glicol; em que a referida porção de ligação de proteína ou peptídeo tem a fórmula geral: em que pr representa referida proteína ou peptídeo, cada nu representa um nucleófilo presente em ou ligado à proteína ou peptídeo, cada de a e b independentemente representa uma cadeia de c1-4alquileno ou alquenileno, e w representa um grupo de remoção de elétron ou um grupo obtido por redução de um grupo de remoção de elétron; e em que referida porção de polietileno glicol é ou inclui uma cadeia de polietileno glicol pendente que tem um grupo de extremidade terminal de fórmula ch2ch2or em que r representa um átomo de hidrogênio, um grupo alquila, ou um grupo arila opcionalmente substituído. também reivindicados são um método para preparar um tal conjugado, e novos reagentes úteis naquele método.
BR112017005760A 2014-10-24 2015-10-08 conjugados e reagentes de conjugação BR112017005760A2 (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
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
GBGB1418989.8A GB201418989D0 (en) 2014-10-24 2014-10-24 Novel conjugation process and reagents
PCT/GB2015/052953 WO2016063006A1 (en) 2014-10-24 2015-10-08 Conjugates and conjugating reagents

Publications (1)

Publication Number Publication Date
BR112017005760A2 true BR112017005760A2 (pt) 2017-12-12

Family

ID=54337308

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017005760A BR112017005760A2 (pt) 2014-10-24 2015-10-08 conjugados e reagentes de conjugação

Country Status (15)

Country Link
US (2) US20170290925A1 (pt)
EP (1) EP3220956B1 (pt)
JP (1) JP6612860B2 (pt)
KR (1) KR102513926B1 (pt)
CN (1) CN107073131B (pt)
AU (1) AU2015334717B2 (pt)
BR (1) BR112017005760A2 (pt)
CA (1) CA2963043A1 (pt)
ES (1) ES2960741T3 (pt)
IL (1) IL250644B (pt)
MX (1) MX2017005199A (pt)
RU (1) RU2017108448A (pt)
SG (1) SG11201701342XA (pt)
WO (1) WO2016063006A1 (pt)
ZA (1) ZA201701337B (pt)

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Publication number Priority date Publication date Assignee Title
US10098960B2 (en) 2015-04-03 2018-10-16 Ucl Business Plc Polymer conjugate
EP3402825A1 (en) 2016-01-12 2018-11-21 Crescendo Biologics Limited Molecules that bind prostate specific membrane antigen (psma)
WO2017161206A1 (en) 2016-03-16 2017-09-21 Halozyme, Inc. Conjugates containing conditionally active antibodies or antigen-binding fragments thereof, and methods of use
EP3442595A1 (en) 2016-04-14 2019-02-20 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
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
JP6990355B2 (ja) 2017-03-30 2022-01-12 日油株式会社 ヘテロ二官能性単分散ポリエチレングリコール及びそれを用いた複合体
GB201711068D0 (en) 2017-07-10 2017-08-23 Crescendo Biologics Ltd Therapeutic molecules binding PSMA
CA3093645A1 (en) 2018-03-13 2019-09-19 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
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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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
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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.
US8158590B2 (en) * 2005-08-05 2012-04-17 Syntarga B.V. Triazole-containing releasable linkers, conjugates thereof, and methods of preparation
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NO2789793T3 (pt) * 2012-10-24 2018-01-27
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Also Published As

Publication number Publication date
RU2017108448A (ru) 2018-11-27
ES2960741T3 (es) 2024-03-06
SG11201701342XA (en) 2017-03-30
CN107073131A (zh) 2017-08-18
US20170290925A1 (en) 2017-10-12
EP3220956A1 (en) 2017-09-27
IL250644A0 (en) 2017-06-29
IL250644B (en) 2020-10-29
CA2963043A1 (en) 2016-04-28
KR102513926B1 (ko) 2023-03-23
AU2015334717A1 (en) 2017-04-13
EP3220956B1 (en) 2023-08-09
ZA201701337B (en) 2018-05-30
WO2016063006A1 (en) 2016-04-28
JP6612860B2 (ja) 2019-11-27
CN107073131B (zh) 2021-05-25
US20200268885A1 (en) 2020-08-27
AU2015334717B2 (en) 2021-02-25
MX2017005199A (es) 2017-07-26
JP2017537062A (ja) 2017-12-14
KR20170075724A (ko) 2017-07-03

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Legal Events

Date Code Title Description
B15K Others concerning applications: alteration of classification

Ipc: A61K 47/00 (2006.01), A61P 35/00 (2006.01)

B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]