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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
Application number
PCT/DK2007/050149
Other languages
English (en)
Other versions
WO2008043366A2 (fr
Inventor
Uffe Koppelhus
Peter Eigil Nielsen
Original Assignee
Univ Koebenhavn
Uffe Koppelhus
Peter Eigil Nielsen
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 Univ Koebenhavn, Uffe Koppelhus, Peter Eigil Nielsen filed Critical Univ Koebenhavn
Publication of WO2008043366A2 publication Critical patent/WO2008043366A2/fr
Publication of WO2008043366A3 publication Critical patent/WO2008043366A3/fr

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 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 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
WO2009149214A2 (fr) * 2008-06-03 2009-12-10 Aileron Therapeutics, Inc. Compositions et procédés pour améliorer le transport cellulaire de biomolécules
ES2333835B2 (es) * 2008-08-29 2010-07-05 Universidade De Santiago De Compostela Compuestos hibridos tripirrol-octaarginina.
US20110212028A1 (en) * 2008-09-16 2011-09-01 Kariem Ahmed Chemically modified cell-penetrating peptides for improved delivery of gene modulating compounds
TW201019969A (en) * 2008-11-17 2010-06-01 Enzon Pharmaceuticals Inc Branched cationic lipids for nucleic acids delivery system
US20110229581A1 (en) * 2008-11-17 2011-09-22 Enzon Pharmaceuticals, Inc. Releasable cationic lipids for nucleic acids delivery systems
US20130079382A1 (en) 2009-10-12 2013-03-28 Larry J. Smith Methods and Compositions for Modulating Gene Expression Using Oligonucleotide Based Drugs Administered in vivo or in vitro
EP3581653A3 (fr) 2013-12-23 2020-02-19 Memorial Sloan-Kettering Cancer Center Procédés et compositions pour le traitement du cancer au moyen d'agents à base d'acides nucléiques de peptides
US10300145B2 (en) 2016-07-15 2019-05-28 Massachusetts Institute Of Technology Synthetic nanoparticles for delivery of immunomodulatory compounds

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 *

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