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WO2005011738A3 - Conjugues polymeres permettant d'etablir un diagnostic et d'effectuer une therapie - Google Patents

Conjugues polymeres permettant d'etablir un diagnostic et d'effectuer une therapie Download PDF

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Publication number
WO2005011738A3
WO2005011738A3 PCT/IT2004/000422 IT2004000422W WO2005011738A3 WO 2005011738 A3 WO2005011738 A3 WO 2005011738A3 IT 2004000422 W IT2004000422 W IT 2004000422W WO 2005011738 A3 WO2005011738 A3 WO 2005011738A3
Authority
WO
WIPO (PCT)
Prior art keywords
chelating
polymers
metal
phosphine
linkers
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.)
Ceased
Application number
PCT/IT2004/000422
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English (en)
Other versions
WO2005011738A2 (fr
Inventor
Francesco Veronese
Ulderico Mazzi
Gianfranco Pasut
Roberta Visentin
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.)
Universita degli Studi di Padova
Original Assignee
Universita degli Studi di Padova
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
Application filed by Universita degli Studi di Padova filed Critical Universita degli Studi di Padova
Publication of WO2005011738A2 publication Critical patent/WO2005011738A2/fr
Publication of WO2005011738A3 publication Critical patent/WO2005011738A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • 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
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/085—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier conjugated systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • A61K49/12—Macromolecular compounds
    • A61K49/126—Linear polymers, e.g. dextran, inulin, PEG

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Radiology & Medical Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne des polymères réactifs pouvant être conjugués, directement ou au moyen de liants et/ou d'autres polymères avec des agents de chélation, qui comprennent au moins un atome phosphoreux sous forme de phosphine ou d'oxyde de phosphine (ou de précurseurs de celui-ci) afin de former des conjugués utilisés dans des applications diagnostiques et thérapeutiques. L'invention concerne, en particulier, des conjugués comprenant un polymère hydrophile lié directement ou au moyen d'autres fractions, à au moins un groupe de chélation capable de chélater des radio-isotopes métalliques comprenant au moins une phosphine ou un oxyde de phosphine phosphoreux. Ces groupes de chélation peuvent être conjugués au polymère hydrophile directement ou via un ou plusieurs liant(s) et/ou un ou plusieurs polymère(s) supplémentaire(s). L'utilisation de ces polymères supplémentaires permet d'augmenter la charge d'agent de chélation. Les liants sont, de préférence, sélectionnés dans des groupes alkyle ou des groupes aromatiques ou des peptides clivables ou d'autres séquences biodégradable. De plus, une ou plusieurs molécule(s) de ciblage peut/peuvent être liée(s ) au polymère hydrophile directement ou au moyen de liants et/ou d'autres polymères. Du fait de leur structure polymère, les conjugués de l'invention possèdent une spécificité améliorée envers certains tissus, tels que les tumeurs, les tissus enflammés et le foie. Cette spécificité peut également être accrue par adjonction de fractions de ciblage telles que des anticorps ou des sucres. Ces conjugués peuvent être formulés afin de rester dans la circulation sanguine pendant une durée appropriée pour des applications diagnostiques et thérapeutiques. Ils possèdent, en outre, une stabilité thermodynamique et cinétique, permettant de conserver intact l'agent de chélation métallique dans des conditions physiques. L'invention concerne également une méthode très simple et très efficace permettant d'étiqueter des substances radiopharmaceutiques, ce qui permet d'éviter l'utilisation d'un agent de réduction supplémentaire. En conséquence, des ions métalliques du type technétium ou rhénium peuvent être ajoutés sous forme de pertechnétate ou pherrhénate aux agents de chélation comprenant un polymère et une phosphine. On a ainsi découvert de manière surprenante que des agents de chélation peuvent agir comme agents de réduction du métal et que l'utilisation d'un agent de réduction supplémentaire n'est pas nécessaire, ce qui permet de préparer des kits simples comprenant un composant (a) constitué de l'agent de chélation polymère et un composant (b) constitué de l'ion métallique dans son état d'oxydation le plus élevé. Ces deux composants peuvent être conservés séparément et combinés ensemble juste avant leur utilisation afin de produire le complexe métallique sans avoir recours à une étape de réduction et de purification.
PCT/IT2004/000422 2003-07-31 2004-07-29 Conjugues polymeres permettant d'etablir un diagnostic et d'effectuer une therapie Ceased WO2005011738A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT2003PD000174A ITPD20030174A1 (it) 2003-07-31 2003-07-31 Coniugati polimerici per diagnostica e terapia
ITPD2003A000174 2003-07-31

Publications (2)

Publication Number Publication Date
WO2005011738A2 WO2005011738A2 (fr) 2005-02-10
WO2005011738A3 true WO2005011738A3 (fr) 2005-04-14

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IT2004/000422 Ceased WO2005011738A2 (fr) 2003-07-31 2004-07-29 Conjugues polymeres permettant d'etablir un diagnostic et d'effectuer une therapie

Country Status (2)

Country Link
IT (1) ITPD20030174A1 (fr)
WO (1) WO2005011738A2 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0804406D0 (en) * 2008-03-10 2008-04-16 Univ Zuerich Metal complexes
US9603940B2 (en) 2010-04-06 2017-03-28 Ihi Corporation Metal salen complex derivative and process for production thereof
US9902690B2 (en) 2013-12-27 2018-02-27 Novus International, Inc. Ethoxylated surfactants
US10584306B2 (en) 2017-08-11 2020-03-10 Board Of Regents Of The University Of Oklahoma Surfactant microemulsions

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0277088A2 (fr) * 1987-01-19 1988-08-03 Schering Aktiengesellschaft Complexes de polymères, leur procédé de préparation et compositions pharmaceutiques les contenant
WO1991018630A1 (fr) * 1990-05-30 1991-12-12 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Agents anti-tumoraux substitues avec du polyether
EP0481526A1 (fr) * 1989-04-07 1992-04-22 Nycomed Salutar, Inc. Agents de chélation
US5155215A (en) * 1985-11-18 1992-10-13 Access Pharmaceuticals Inc. Polychelating agents for image and spectral enhancement (and spectral shift)
US5900228A (en) * 1996-07-31 1999-05-04 California Institute Of Technology Bifunctional detection agents having a polymer covalently linked to an MRI agent and an optical dye
WO2001019838A1 (fr) * 1999-09-13 2001-03-22 Du Pont Pharmaceuticals Company Chelateurs macrocycliques destines a des produits metallopharmaceutiques
WO2003014157A2 (fr) * 2001-08-03 2003-02-20 Bracco Imaging S.P.A. Conjugues peptidiques, leurs derives a complexes metalliques et leur utilisation dans l'imagerie par resonance magnetique (irm)
WO2004010868A2 (fr) * 2002-07-31 2004-02-05 General Electric Company Procede de liaison d'agents moleculaires a des vaisseaux sanguins angiogeniques

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5155215A (en) * 1985-11-18 1992-10-13 Access Pharmaceuticals Inc. Polychelating agents for image and spectral enhancement (and spectral shift)
EP0277088A2 (fr) * 1987-01-19 1988-08-03 Schering Aktiengesellschaft Complexes de polymères, leur procédé de préparation et compositions pharmaceutiques les contenant
EP0481526A1 (fr) * 1989-04-07 1992-04-22 Nycomed Salutar, Inc. Agents de chélation
WO1991018630A1 (fr) * 1990-05-30 1991-12-12 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Agents anti-tumoraux substitues avec du polyether
US5900228A (en) * 1996-07-31 1999-05-04 California Institute Of Technology Bifunctional detection agents having a polymer covalently linked to an MRI agent and an optical dye
WO2001019838A1 (fr) * 1999-09-13 2001-03-22 Du Pont Pharmaceuticals Company Chelateurs macrocycliques destines a des produits metallopharmaceutiques
WO2003014157A2 (fr) * 2001-08-03 2003-02-20 Bracco Imaging S.P.A. Conjugues peptidiques, leurs derives a complexes metalliques et leur utilisation dans l'imagerie par resonance magnetique (irm)
WO2004010868A2 (fr) * 2002-07-31 2004-02-05 General Electric Company Procede de liaison d'agents moleculaires a des vaisseaux sanguins angiogeniques

Non-Patent Citations (9)

* Cited by examiner, † Cited by third party
Title
"UNITA? DI RICERCA DI PADOVA, Sezione Radiofarmaci", CIRC MSB, UNITÀ AFFERENTI, UNIVERSITÀ DEGLI STUDI DI PADOVA, ATTIVITÀ ANNO 2002, 2002, pages 1 - 26, XP002312000, Retrieved from the Internet <URL:http://www.circmsb.uniba.it/rel2002/UNITA%20padova.pdf> *
BERGBREITER D E ET AL: "Tridentate SCS palladium(II) complexes: New, highly stable, recyclable catalysts for the heck reaction", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY 1999 UNITED STATES, vol. 121, no. 41, 1999, pages 9531 - 9538, XP002312003, ISSN: 0002-7863 *
HARWIG C W ET AL: "Soluble polymers: New options in both traditional and combinatorial synthesis", CHEMTRACTS, vol. 12, no. 1, 1999, pages 1 - 26, XP008038355, ISSN: 1431-9268 *
JAN KOTEK ET AL.: "Lanthanide(III) Complexes of Novel Mixed Carboxylic-Phosphorus Acid Derivatives of Diethylenetriamine: A Step towards More Efficient MRI Contrast Agents", CHEM. EUR. J., vol. 9, no. 23, 5 December 2003 (2003-12-05), pages 5899 - 5915, XP002312001 *
KÖLLHOFER AXEL ET AL: "Homogeneous catalysts supported on soluble polymers: biphasic Sonogashira coupling of aryl halides and acetylenes using MeOPEG-bound phosphine-palladium catalysts for efficient catalyst recycling.", CHEMISTRY (WEINHEIM AN DER BERGSTRASSE, GERMANY) 17 MAR 2003, vol. 9, no. 6, 17 March 2003 (2003-03-17), pages 1416 - 1425, XP002312002, ISSN: 0947-6539 *
MATTHEWS S E ET AL: "Macromolecular systems for chemotherapy and magnetic resonance Imaging", ADVANCED DRUG DELIVERY REVIEWS 1996 NETHERLANDS, vol. 18, no. 2, 1996, pages 219 - 267, XP002311999, ISSN: 0169-409X *
SIEBER F ET AL: "DEVELOPMENT AND APPLICATION OF A POLY(ETHYLENE GLYCOL)-SUPPORTED TRIARYLPHOSPHINE REAGENT: EXPANDING THE SPHERE OF LIQUID-PHASE ORGANIC SYNTHESIS", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY. EASTON, US, vol. 64, no. 14, 9 July 1999 (1999-07-09), pages 5188 - 5192, XP000830433, ISSN: 0022-3263 *
UOZUMI Y ET AL: "New Amphiphilic Palladium-Phosphine Complexes Bound to Solid Supports: Preparation and Use for Catalytic Allylic Substitution in Aqueous Media", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 38, no. 20, 19 May 1997 (1997-05-19), pages 3557 - 3560, XP004061958, ISSN: 0040-4039 *
VISENTIN R ET AL: "99mtechnetium labeling of pegylated PN2S ligand in presence or absence of Tin(II).", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 46, no. Supplement 1, August 2003 (2003-08-01), & 15TH INTERNATIONAL SYMPOSIUM ON RADIOPHARMACEUTICAL CHEMISTRY; SYDNEY, AUSTRALIA; AUGUST 10-14, 2003, pages S26, XP002311998, ISSN: 0362-4803 *

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Publication number Publication date
ITPD20030174A1 (it) 2003-10-29
WO2005011738A2 (fr) 2005-02-10

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