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WO1998004575A3 - Analogues lipophiles d'oligonucleotides - Google Patents

Analogues lipophiles d'oligonucleotides Download PDF

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Publication number
WO1998004575A3
WO1998004575A3 PCT/US1996/012530 US9612530W WO9804575A3 WO 1998004575 A3 WO1998004575 A3 WO 1998004575A3 US 9612530 W US9612530 W US 9612530W WO 9804575 A3 WO9804575 A3 WO 9804575A3
Authority
WO
WIPO (PCT)
Prior art keywords
lipophilic
oligonucleotide analogs
contain
oligonucleotides
substitutions
Prior art date
Application number
PCT/US1996/012530
Other languages
English (en)
Other versions
WO1998004575A2 (fr
Inventor
Norbert W Bischofberger
Kenneth W Kent
Richard W Wagner
Chris A Buhr
Kuei-Ying Lin
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Priority to PCT/US1996/012530 priority Critical patent/WO1998004575A2/fr
Priority to EP96926831A priority patent/EP0923596A2/fr
Priority to CA002261704A priority patent/CA2261704A1/fr
Publication of WO1998004575A2 publication Critical patent/WO1998004575A2/fr
Publication of WO1998004575A3 publication Critical patent/WO1998004575A3/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Analogues lipophiles d'oligonucléotides capables de se diffuser passivement et efficacement à travers les membranes cellulaires. Ces oligonucléotides contiennent au moins deux résidus de nucléotides et ont un coefficient de partage octanol:eau allant de -0,3 à +2,5 environ et une solubilité dans l'eau d'au moins 0,001 νg/mL. L'invention porte notamment sur des analogues lipophiles d'oligonucléotides dont au moins 60 % des liaisons inter-nucléotides sont lipophiles, ou dont au moins 60 % des bases contiennent des substitutions lipophiles, ou dont au moins 60 % des glucides contiennent des substitutions lipophiles, ou qui présentent une combinaison de ceux-ci à raison de 60 %. Ces oligonucléotides peuvent être conjugués pour former un marqueur et utilisés pour visualiser des cellules ou des compartiments infracellulaires.
PCT/US1996/012530 1996-07-31 1996-07-31 Analogues lipophiles d'oligonucleotides WO1998004575A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
PCT/US1996/012530 WO1998004575A2 (fr) 1996-07-31 1996-07-31 Analogues lipophiles d'oligonucleotides
EP96926831A EP0923596A2 (fr) 1996-07-31 1996-07-31 Analogues lipophiles d'oligonucleotides
CA002261704A CA2261704A1 (fr) 1996-07-31 1996-07-31 Analogues lipophiles d'oligonucleotides

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/US1996/012530 WO1998004575A2 (fr) 1996-07-31 1996-07-31 Analogues lipophiles d'oligonucleotides
CA002261704A CA2261704A1 (fr) 1996-07-31 1996-07-31 Analogues lipophiles d'oligonucleotides

Publications (2)

Publication Number Publication Date
WO1998004575A2 WO1998004575A2 (fr) 1998-02-05
WO1998004575A3 true WO1998004575A3 (fr) 1998-03-19

Family

ID=25680807

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1996/012530 WO1998004575A2 (fr) 1996-07-31 1996-07-31 Analogues lipophiles d'oligonucleotides

Country Status (3)

Country Link
EP (1) EP0923596A2 (fr)
CA (1) CA2261704A1 (fr)
WO (1) WO1998004575A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7575918B2 (en) 1999-04-14 2009-08-18 The Penn State Research Foundation Tissue-specific and pathogen-specific ribozymes

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005537028A (ja) 2002-06-26 2005-12-08 ザ　ペン　ステート　リサーチ　ファウンデーション ヒト乳頭腫ウイルス感染症を治療する方法及び材料
MX2011008563A (es) 2009-02-13 2012-06-19 Chem Inc X Metodos de crear y analizar/seleccionar bibliotecas codificadas por adn.
EP3000898B1 (fr) 2013-05-21 2020-11-18 Hitgen Inc. Procédé de capture de cibles de médicaments
CA3127137A1 (fr) 2019-01-22 2020-07-30 Vipergen Aps Procede de criblage d'une banque d'affichage in vitro dans une cellule

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4904582A (en) * 1987-06-11 1990-02-27 Synthetic Genetics Novel amphiphilic nucleic acid conjugates
WO1990010448A2 (fr) * 1989-03-07 1990-09-20 Genentech, Inc. Conjugue covalent de lipides et d'oligonucleotides
WO1993010820A1 (fr) * 1991-11-26 1993-06-10 Gilead Sciences, Inc. Formation amelioree de triple et double helices a l'aide d'oligomeres contenant des pyrimidines modifiees
EP0547008A1 (fr) * 1991-11-26 1993-06-16 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Oligonucléotides antisenses
US5420330A (en) * 1990-09-07 1995-05-30 Pharmacia P-L Biochemicals Inc. Lipo-phosphoramidites
WO1996029337A1 (fr) * 1995-03-23 1996-09-26 Hybridon, Inc. Phosphorothioates d'oligodesoxynucleotides anti-sens modifies de thiono-triester
US5633360A (en) * 1992-04-14 1997-05-27 Gilead Sciences, Inc. Oligonucleotide analogs capable of passive cell membrane permeation

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5484908A (en) 1991-11-26 1996-01-16 Gilead Sciences, Inc. Oligonucleotides containing 5-propynyl pyrimidines

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4904582A (en) * 1987-06-11 1990-02-27 Synthetic Genetics Novel amphiphilic nucleic acid conjugates
WO1990010448A2 (fr) * 1989-03-07 1990-09-20 Genentech, Inc. Conjugue covalent de lipides et d'oligonucleotides
US5420330A (en) * 1990-09-07 1995-05-30 Pharmacia P-L Biochemicals Inc. Lipo-phosphoramidites
WO1993010820A1 (fr) * 1991-11-26 1993-06-10 Gilead Sciences, Inc. Formation amelioree de triple et double helices a l'aide d'oligomeres contenant des pyrimidines modifiees
EP0547008A1 (fr) * 1991-11-26 1993-06-16 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Oligonucléotides antisenses
US5633360A (en) * 1992-04-14 1997-05-27 Gilead Sciences, Inc. Oligonucleotide analogs capable of passive cell membrane permeation
WO1996029337A1 (fr) * 1995-03-23 1996-09-26 Hybridon, Inc. Phosphorothioates d'oligodesoxynucleotides anti-sens modifies de thiono-triester

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
J.F.HUGHES ET AL.: "Lipid Membrane Permeability of 2'-Modified Derivatives of Phosphorothioate Oligonucleotides.", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 83, no. 4, April 1994 (1994-04-01), pages 597 - 600, XP002052615 *
J.M.DAGLE ET AL.: "Physical Properties of Oligonucleotides Containing Phosphoramidate-Modified Internucleoside Linkages.", NUCLEIC ACIDS RESEARCH., vol. 19, no. 8, 1991, OXFORD GB, pages 1805 - 1810, XP002052616 *
S.AKHTAR ET AL.: "Interactions of Antisense DNA Oligonucleotide Analogs with Phospholipid Membranes (Liposomes).", NUCLEIC ACIDS RESEARCH., vol. 19, no. 20, 1991, OXFORD GB, pages 5551 - 5559, XP002052617 *
Z.ZHANG ET AL.: "Thiono Triester Modified Antisense Oligonucleotides for Inhibition of Human Cytomegalovirus in vitro.", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 6, no. 16, August 1996 (1996-08-01), pages 1911 - 1916, XP000677176 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7575918B2 (en) 1999-04-14 2009-08-18 The Penn State Research Foundation Tissue-specific and pathogen-specific ribozymes

Also Published As

Publication number Publication date
EP0923596A2 (fr) 1999-06-23
CA2261704A1 (fr) 1998-02-05
WO1998004575A2 (fr) 1998-02-05

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