BR112014016338A2 - polímeros de polioxazolina e processos para a sua preparação, conjugados destes polímeros e usos médicos dos mesmos - Google Patents

polímeros de polioxazolina e processos para a sua preparação, conjugados destes polímeros e usos médicos dos mesmos

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Publication number
BR112014016338A2
BR112014016338A2 BR112014016338A BR112014016338A BR112014016338A2 BR 112014016338 A2 BR112014016338 A2 BR 112014016338A2 BR 112014016338 A BR112014016338 A BR 112014016338A BR 112014016338 A BR112014016338 A BR 112014016338A BR 112014016338 A2 BR112014016338 A2 BR 112014016338A2
Authority
BR
Brazil
Prior art keywords
polymers
conjugates
polyoxazoline
moiety
therapeutic
Prior art date
Application number
BR112014016338A
Other languages
English (en)
Other versions
BR112014016338A8 (pt
BR112014016338B1 (pt
Inventor
Hoogenboom Richard
Original Assignee
Univ Gent
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 PCT/NL2012/050001 external-priority patent/WO2012057628A2/en
Application filed by Univ Gent filed Critical Univ Gent
Publication of BR112014016338A2 publication Critical patent/BR112014016338A2/pt
Publication of BR112014016338A8 publication Critical patent/BR112014016338A8/pt
Publication of BR112014016338B1 publication Critical patent/BR112014016338B1/pt

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/06—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
    • A61K51/065—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules conjugates with carriers being macromolecules
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G73/00—Macromolecular compounds obtained by reactions forming a linkage containing nitrogen with or without oxygen or carbon in the main chain of the macromolecule, not provided for in groups C08G12/00 - C08G71/00
    • C08G73/02—Polyamines
    • C08G73/0233—Polyamines derived from (poly)oxazolines, (poly)oxazines or having pendant acyl groups
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/06—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L79/00—Compositions of macromolecular compounds obtained by reactions forming in the main chain of the macromolecule a linkage containing nitrogen with or without oxygen or carbon only, not provided for in groups C08L61/00 - C08L77/00
    • C08L79/02—Polyamines

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

resumo polímeros de polioxazolina e processos para a sua preparação, conjugados destes polímeros e usos médicos dos mesmos a presente invenção se refere a polímeros de poli(2-oxazolina) funcionalizados, que são muito adequados como um transportador e/ou veículo (conjugado) de liberação de drogas, tais como moléculas terapêuticas pequenas e bio- farmacêuticas. esses polímeros são caracterizados pelo fato de conterem unidades de repetição que são representadas pela seguinte fórmula -[n(r1)-(chr2)m]-, em que r1 é r3- (chr4)n-conh-r5; r2 é selecionado a partir de h e alquila c1-5 opcionalmente substituído; r3 é ch2, co, c(o)o, c(o)nh ou c(s)nh; r4 é selecionado a partir de h e alquila c1-5 opcionalmente substituído; r5 é h, um grupo alquila c1-5; arila ou um radical que compreende um grupo funcional que pode ser utilizado para a conjugação; m é 2 ou 3; e n é 1 a 5 ou n é 0 e r3 é ch2. a invenção se refere ainda a um conjugado destes polímeros de polioxazolina com pelo menos uma porção ativa, tal como uma porção terapêutica, uma porção de direcionamento e/ou uma porção de diagnóstico, bem como ao uso destes conjugados no tratamento terapêutico ou tratamento profilático ou de diagnóstico de uma doença ou distúrbio.
BR112014016338-3A 2012-01-02 2012-12-28 polímeros de polioxazolina e processos para a sua preparação, conjugados destes polímeros e usos médicos dos mesmos BR112014016338B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
NLPCT/NL2012/050001 2012-01-02
PCT/NL2012/050001 WO2012057628A2 (en) 2011-01-04 2012-01-02 Cross-linked polymers and implants derived from electrophilically activated polyoxazoline
EP12159986.4 2012-03-16
EP12159986 2012-03-16
PCT/NL2012/050933 WO2013103297A1 (en) 2012-01-02 2012-12-28 Polyoxazoline polymers and methods for their preparation, conjugates of these polymers and medical uses thereof

Publications (3)

Publication Number Publication Date
BR112014016338A2 true BR112014016338A2 (pt) 2017-06-13
BR112014016338A8 BR112014016338A8 (pt) 2017-07-04
BR112014016338B1 BR112014016338B1 (pt) 2021-01-26

Family

ID=48745312

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014016338-3A BR112014016338B1 (pt) 2012-01-02 2012-12-28 polímeros de polioxazolina e processos para a sua preparação, conjugados destes polímeros e usos médicos dos mesmos

Country Status (7)

Country Link
US (1) US9180202B2 (pt)
EP (1) EP2800773B1 (pt)
JP (1) JP6159973B2 (pt)
CN (1) CN104024306B (pt)
BR (1) BR112014016338B1 (pt)
ES (1) ES2661461T3 (pt)
WO (1) WO2013103297A1 (pt)

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JP6652808B2 (ja) * 2014-10-16 2020-02-26 キヤノン株式会社 重合体、前記重合体を有する光音響イメージング用造影剤
EP3442501A1 (en) 2016-04-15 2019-02-20 Fairhaven Health, LLC Compositions and methods for maintaining or enhancing homeostasis or function of female lower reproductive tract
JP7036510B2 (ja) 2016-07-01 2022-03-15 ユニヴェルシテイト ヘント ポリ（環状イミノエーテル）
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US11793878B2 (en) 2018-03-16 2023-10-24 Universiteit Gent Drug formulations comprising polyoxazolines as matrix excipient
EP3802632A1 (en) 2018-05-24 2021-04-14 Universiteit Gent Amidation of polymers containing ester side chains using functionalized amines
US11993670B2 (en) 2018-06-06 2024-05-28 The Board Of Trustees Of The University Of Illinois Zwitterionic biocompatible polymers, methods, and uses thereof
BR112022001554A2 (pt) 2019-07-30 2022-03-22 Gatt Tech B V Copolímero de polioxazolina, uso do copolímero, produto médico biocompatível e processo de preparação de copolímeros
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EP4222190A1 (en) 2020-09-30 2023-08-09 Universiteit Gent Amorphous thermoresponsive polymers
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Also Published As

Publication number Publication date
US9180202B2 (en) 2015-11-10
CN104024306B (zh) 2017-06-13
BR112014016338A8 (pt) 2017-07-04
US20150025196A1 (en) 2015-01-22
WO2013103297A1 (en) 2013-07-11
BR112014016338B1 (pt) 2021-01-26
ES2661461T3 (es) 2018-04-02
JP2015503556A (ja) 2015-02-02
CN104024306A (zh) 2014-09-03
EP2800773A1 (en) 2014-11-12
JP6159973B2 (ja) 2017-07-12
EP2800773B1 (en) 2017-12-13

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B15K Others concerning applications: alteration of classification

Ipc: C08G 73/02 (2006.01), A61K 47/34 (2017.01), C08L 7

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 28/12/2012, OBSERVADAS AS CONDICOES LEGAIS.