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WO2008043366A3 - Composés à trois domaines pour une administration transmembranaire - Google Patents

Composés à trois domaines pour une administration transmembranaire Download PDF

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Publication number
WO2008043366A3
WO2008043366A3 PCT/DK2007/050149 DK2007050149W WO2008043366A3 WO 2008043366 A3 WO2008043366 A3 WO 2008043366A3 DK 2007050149 W DK2007050149 W DK 2007050149W WO 2008043366 A3 WO2008043366 A3 WO 2008043366A3
Authority
WO
WIPO (PCT)
Prior art keywords
domain
transmembrane delivery
compounds
delivery
present
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/DK2007/050149
Other languages
English (en)
Other versions
WO2008043366A2 (fr
Inventor
Uffe Koppelhus
Peter Eigil Nielsen
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.)
Københavns Universitet
Original Assignee
Københavns Universitet
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 Københavns Universitet filed Critical Københavns Universitet
Publication of WO2008043366A2 publication Critical patent/WO2008043366A2/fr
Publication of WO2008043366A3 publication Critical patent/WO2008043366A3/fr
Anticipated expiration legal-status Critical
Ceased 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
    • A61K47/50—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
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • A61K47/6455—Polycationic oligopeptides, polypeptides or polyamino acids, e.g. for complexing nucleic acids
    • 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
    • A61K47/54—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 compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino 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
    • A61K47/62—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
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La présente invention est basée sur la découverte d'après laquelle l'administration transmembranaire d'un agent biologique couplé à un domaine cationique peut être encore améliorée par le couplage à un domaine lipophile, tel qu'un acide gras. Ainsi, un aspect de la présente invention porte sur des composés à trois domaines permettant une administration transmembranaire améliorée. D'autres aspects sont l'utilisation des composés à trois domaines pour une thérapie, des compositions pharmaceutiques comprenant le composé à trois domaines, ainsi que des procédés pour améliorer l'administration transmembranaire.
PCT/DK2007/050149 2006-10-13 2007-10-15 Composés à trois domaines pour une administration transmembranaire Ceased WO2008043366A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA200601335 2006-10-13
DKPA200601335 2006-10-13

Publications (2)

Publication Number Publication Date
WO2008043366A2 WO2008043366A2 (fr) 2008-04-17
WO2008043366A3 true WO2008043366A3 (fr) 2009-01-15

Family

ID=39081572

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DK2007/050149 Ceased WO2008043366A2 (fr) 2006-10-13 2007-10-15 Composés à trois domaines pour une administration transmembranaire

Country Status (1)

Country Link
WO (1) WO2008043366A2 (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110250685A1 (en) * 2008-06-03 2011-10-13 Nash Huw M Compositions and methods for enhancing cellular transport of biomolecules
ES2333835B2 (es) * 2008-08-29 2010-07-05 Universidade De Santiago De Compostela Compuestos hibridos tripirrol-octaarginina.
EP2355852A4 (fr) * 2008-09-16 2015-06-24 Ge Healthcare Bio Sciences Ab Peptides de pénétration cellulaire chimiquement modifiés pour une administration améliorée de composés de modulation de gène
US20110229581A1 (en) * 2008-11-17 2011-09-22 Enzon Pharmaceuticals, Inc. Releasable cationic lipids for nucleic acids delivery systems
CN102216462A (zh) * 2008-11-17 2011-10-12 安龙制药公司 用于核酸递送系统的支化阳离子脂质
EP3252068B1 (fr) 2009-10-12 2025-07-02 Larry J. Smith Procédés et compositions permettant de moduler l'expression génique à l'aide de médicaments à base d'oligonucléotides administrés in vivo ou in vitro
CA3142856A1 (fr) 2013-12-23 2015-07-02 Memorial Sloan-Kettering Cancer Center Methodes et compositions pour le traitement du cancer utilisant des agents a base d'acides nucleiques de peptides
WO2018013924A1 (fr) * 2016-07-15 2018-01-18 Massachusetts Institute Of Technology Nanoparticules synthétiques pour l'administration de composés immunomodulateurs

Non-Patent Citations (13)

* Cited by examiner, † Cited by third party
Title
ANTOPOLSKY M ET AL: "PEPTIDE-OLIGONUCLEOTIDE PHOSPHOROTHIOATE CONJUGATES WITH MEMBRANE TRANSLOCATION AND NUCLEAR LOCALIZATION PROPERTIES", BIOCONJUGATE CHEMISTRY, ACS, WASHINGTON, DC, US, vol. 10, no. 4, 1 January 1999 (1999-01-01), pages 598 - 606, XP002949113, ISSN: 1043-1802 *
BENDIFALLAH N ET AL: "Evaluation of cell-penetrating peptides (CPPs) as vehicles for intracellular delivery of antisense peptide nucleic acid (PNA)", BIOCONJUGATE CHEMISTRY 200605 US, vol. 17, no. 3, May 2006 (2006-05-01), pages 750 - 758, XP002499767, ISSN: 1043-1802 *
CHEN C-P ET AL: "A concise method for the preparation of peptide and arginine-rich peptide-conjugated antisense oligonucleotide", BIOCONJUGATE CHEMISTRY, ACS, WASHINGTON, DC, US, vol. 14, no. 3, 1 May 2003 (2003-05-01), pages 532 - 538, XP002314110, ISSN: 1043-1802 *
DIETZ ET AL: "Peptide-enhanced cellular internalization of proteins in neuroscience", BRAIN RESEARCH BULLETIN, ELSEVIER SCIENCE LTD, OXFORD, GB, vol. 68, no. 1-2, 15 December 2005 (2005-12-15), pages 103 - 114, XP005187753, ISSN: 0361-9230 *
FERNANDEZ-CARNEADO J ET AL: "Fatty acyl moieties: Improving Pro-rich peptide uptake inside HeLa cells", JOURNAL OF PEPTIDE RESEARCH 200506 GB, vol. 65, no. 6, June 2005 (2005-06-01), pages 580 - 590, XP002499766, ISSN: 1397-002X *
FUTAKI S ET AL: "STEARYLATED ARGININE-RICH PEPTIDES: A NEW CLASS OF TRANSFECTION SYSTEMS", BIOCONJUGATE CHEMISTRY, ACS, WASHINGTON, DC, US, vol. 12, no. 6, 1 November 2001 (2001-11-01), pages 1005 - 1011, XP001092542, ISSN: 1043-1802 *
FUTAKI S: "Membrane-permeable arginine-rich peptides and the translocation mechanisms", ADVANCED DRUG DELIVERY REVIEWS, ELSEVIER BV, AMSTERDAM, NL, vol. 57, no. 4, 28 February 2005 (2005-02-28), pages 547 - 558, XP004752187, ISSN: 0169-409X *
KHALIL I A ET AL: "Mechanism of improved gene transfer by the N-terminal stearylation of octaarginine: Enhanced cellular association by hydrophobic core formation", GENE THERAPY 200404 GB, vol. 11, no. 7, April 2004 (2004-04-01), pages 636 - 644, XP002499763, ISSN: 0969-7128 *
KIM W J ET AL: "Cholesteryl Oligoarginine Delivering Vascular Endothelial Growth Factor siRNA Effectively Inhibits Tumor Growth in Colon Adenocarcinoma", MOLECULAR THERAPY 200609 US, vol. 14, no. 3, September 2006 (2006-09-01), pages 343 - 350, XP002499764, ISSN: 1525-0016 *
MOULTON H M ET AL: "CELLULAR UPTAKE OF ANTISENSE MORPHOLINO OLIGOMERS CONJUGATED TO ARGININE-RICH PEPTIDES", BIOCONJUGATE CHEMISTRY, ACS, WASHINGTON, DC, US, vol. 15, no. 2, 1 January 2004 (2004-01-01), pages 290 - 299, XP002999956, ISSN: 1043-1802 *
PHAM WELLINGTON ET AL: "Enhancing membrane permeability by fatty acylation of oligoarginine peptides.", CHEMBIOCHEM : A EUROPEAN JOURNAL OF CHEMICAL BIOLOGY 6 AUG 2004, vol. 5, no. 8, 6 August 2004 (2004-08-06), pages 1148 - 1151, XP002499761, ISSN: 1439-4227 *
TONGES L ET AL: "Stearylated octaarginine and artificial virus-like particles for transfection of siRNA into primary rat neurons", RNA 2006 US, vol. 12, no. 7, 12 May 2006 (2006-05-12), pages 1431 - 1438, XP002499765, ISSN: 1355-8382 1469-9001 *
TURNER J J ET AL: "Synthesis, cellular uptake and HIV-1 Tat-dependent trans-activation inhibition activity of oligonucleotide analogues disulphide-conjugated to cell-penetrating peptides", NUCLEIC ACIDS RESEARCH 2005 GB, vol. 33, no. 1, 2005, pages 27 - 42, XP002499762, ISSN: 0305-1048 *

Also Published As

Publication number Publication date
WO2008043366A2 (fr) 2008-04-17

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