DK0524997T3 - 2-O-alkyl nucleotides as well as polymers containing such nucleotides - Google Patents

2-O-alkyl nucleotides as well as polymers containing such nucleotides

Info

Publication number
DK0524997T3
DK0524997T3 DK91907452.6T DK91907452T DK0524997T3 DK 0524997 T3 DK0524997 T3 DK 0524997T3 DK 91907452 T DK91907452 T DK 91907452T DK 0524997 T3 DK0524997 T3 DK 0524997T3
Authority
DK
Denmark
Prior art keywords
nucleotides
atom
different
same
possibly modified
Prior art date
Application number
DK91907452.6T
Other languages
Danish (da)
Inventor
Brian Sproat
Angus Lamond
Original Assignee
Europ Isches Lab F
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 Europ Isches Lab F filed Critical Europ Isches Lab F
Application granted granted Critical
Publication of DK0524997T3 publication Critical patent/DK0524997T3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Fixing For Electrophotography (AREA)
  • Electrophotography Configuration And Component (AREA)
  • Color Electrophotography (AREA)

Abstract

Oligonucleotides of the general formula (I), in which: B is any nucleo base; A is O or CH2; X or Z are O, S, NH or CH2, where X and Z may be the same or different; V and W are an O, S, Se, NH2 or an alkyloxy radical, OH or SH, where V and W may be the same or different in a monomer unit; and L is an H atom or a partner of a bonding pair and C is -O-R and R is a possibly modified alkyl group with at least one C atom or a possibly modified alkenyl or alkinyl group with at least 2 C atoms, whereby the modification consists in a substitution by one or more halogen, cyano, carboxy, hydroxy, nitro and/or mercapto radicals; n is any whole number; are stable and specifically binding anti-sense probes. Such oligo and polynucleotides are useful for controlling gene expression and as medicaments. They are synthesised from the corresponding 2'-substituted monomers by prior art processes, preferably on a solid phase.
DK91907452.6T 1990-04-09 1991-04-08 2-O-alkyl nucleotides as well as polymers containing such nucleotides DK0524997T3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE4011473 1990-04-09

Publications (1)

Publication Number Publication Date
DK0524997T3 true DK0524997T3 (en) 1995-01-02

Family

ID=6404077

Family Applications (1)

Application Number Title Priority Date Filing Date
DK91907452.6T DK0524997T3 (en) 1990-04-09 1991-04-08 2-O-alkyl nucleotides as well as polymers containing such nucleotides

Country Status (8)

Country Link
EP (1) EP0524997B1 (en)
JP (1) JPH07103150B2 (en)
AT (1) ATE109788T1 (en)
CA (1) CA2080231C (en)
DE (2) DE4037363A1 (en)
DK (1) DK0524997T3 (en)
ES (1) ES2059132T3 (en)
WO (1) WO1991015499A1 (en)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5914396A (en) * 1990-01-11 1999-06-22 Isis Pharmaceuticals, Inc. 2'-O-modified nucleosides and phosphoramidites
US7101993B1 (en) 1990-01-11 2006-09-05 Isis Pharmaceuticals, Inc. Oligonucleotides containing 2′-O-modified purines
US5955589A (en) * 1991-12-24 1999-09-21 Isis Pharmaceuticals Inc. Gapped 2' modified oligonucleotides
US5872232A (en) * 1990-01-11 1999-02-16 Isis Pharmaceuticals Inc. 2'-O-modified oligonucleotides
US5670633A (en) * 1990-01-11 1997-09-23 Isis Pharmaceuticals, Inc. Sugar modified oligonucleotides that detect and modulate gene expression
US5623065A (en) * 1990-08-13 1997-04-22 Isis Pharmaceuticals, Inc. Gapped 2' modified oligonucleotides
US6358931B1 (en) 1990-01-11 2002-03-19 Isis Pharmaceuticals, Inc. Compositions and methods for modulating RNA
US6005087A (en) 1995-06-06 1999-12-21 Isis Pharmaceuticals, Inc. 2'-modified oligonucleotides
US5514786A (en) * 1990-01-11 1996-05-07 Isis Pharmaceuticals, Inc. Compositions for inhibiting RNA activity
US6399754B1 (en) 1991-12-24 2002-06-04 Isis Pharmaceuticals, Inc. Sugar modified oligonucleotides
US5859221A (en) * 1990-01-11 1999-01-12 Isis Pharmaceuticals, Inc. 2'-modified oligonucleotides
US7015315B1 (en) 1991-12-24 2006-03-21 Isis Pharmaceuticals, Inc. Gapped oligonucleotides
US5965722A (en) 1991-05-21 1999-10-12 Isis Pharmaceuticals, Inc. Antisense inhibition of ras gene with chimeric and alternating oligonucleotides
US7119184B2 (en) 1991-08-12 2006-10-10 Isis Pharmaceuticals, Inc. Oligonucleotides having A-DNA form and B-DNA form conformational geometry
US6307040B1 (en) 1992-03-05 2001-10-23 Isis Pharmaceuticals, Inc. Sugar modified oligonucleotides that detect and modulate gene expression
US5856455A (en) * 1991-12-24 1999-01-05 Isis Pharmaceuticals, Inc. Gapped 2'-modified oligonucleotides
EP1695979B1 (en) 1991-12-24 2011-07-06 Isis Pharmaceuticals, Inc. Gapped modified oligonucleotides
US6277603B1 (en) 1991-12-24 2001-08-21 Isis Pharmaceuticals, Inc. PNA-DNA-PNA chimeric macromolecules
US5700922A (en) * 1991-12-24 1997-12-23 Isis Pharmaceuticals, Inc. PNA-DNA-PNA chimeric macromolecules
TW244371B (en) * 1992-07-23 1995-04-01 Tri Clover Inc
US6346614B1 (en) 1992-07-23 2002-02-12 Hybridon, Inc. Hybrid oligonucleotide phosphorothioates
US5652355A (en) * 1992-07-23 1997-07-29 Worcester Foundation For Experimental Biology Hybrid oligonucleotide phosphorothioates
GB9304618D0 (en) * 1993-03-06 1993-04-21 Ciba Geigy Ag Chemical compounds
DK0679657T3 (en) * 1994-04-27 2003-10-27 Novartis Ag Nucleosides and oligonucleotides with 2'-ether groups
GB9417746D0 (en) * 1994-09-03 1994-10-19 Ciba Geigy Ag Chemical compounds
GB9417938D0 (en) * 1994-09-06 1994-10-26 Ciba Geigy Ag Compounds
US6166197A (en) * 1995-03-06 2000-12-26 Isis Pharmaceuticals, Inc. Oligomeric compounds having pyrimidine nucleotide (S) with 2'and 5 substitutions
JPH10512894A (en) 1995-03-06 1998-12-08 アイシス・ファーマシューティカルス・インコーポレーテッド Improved method for the synthesis of 2'-O-substituted pyrimidines and their oligomeric compounds
GB9606158D0 (en) * 1996-03-23 1996-05-29 Ciba Geigy Ag Chemical compounds
US5856099A (en) * 1996-05-21 1999-01-05 Isis Pharmaceuticals, Inc. Antisense compositions and methods for modulating type I interleukin-1 receptor expression
US9096636B2 (en) 1996-06-06 2015-08-04 Isis Pharmaceuticals, Inc. Chimeric oligomeric compounds and their use in gene modulation
US7812149B2 (en) 1996-06-06 2010-10-12 Isis Pharmaceuticals, Inc. 2′-Fluoro substituted oligomeric compounds and compositions for use in gene modulations
US5898031A (en) 1996-06-06 1999-04-27 Isis Pharmaceuticals, Inc. Oligoribonucleotides for cleaving RNA
ATE251638T1 (en) 1996-06-06 2003-10-15 Novartis Pharma Gmbh 2-SUBSTITUTED NUCLEOSIDE AND OLIGONUCLEOTIDE DERIVATIVES
GB9612600D0 (en) 1996-06-13 1996-08-21 Ciba Geigy Ag Chemical compounds
US6127533A (en) 1997-02-14 2000-10-03 Isis Pharmaceuticals, Inc. 2'-O-aminooxy-modified oligonucleotides
US6172209B1 (en) 1997-02-14 2001-01-09 Isis Pharmaceuticals Inc. Aminooxy-modified oligonucleotides and methods for making same
US6576752B1 (en) 1997-02-14 2003-06-10 Isis Pharmaceuticals, Inc. Aminooxy functionalized oligomers
JP4688294B2 (en) * 1998-12-30 2011-05-25 オリゴス・イーティーシー・インコーポレイテッド End-blocked nucleic acids modified with an acid-stable backbone and therapeutic uses thereof
CA2504929C (en) 2002-11-05 2014-07-22 Charles Allerson Compositions comprising alternating 2'-modified nucleosides for use in gene modulation
US8569474B2 (en) 2004-03-09 2013-10-29 Isis Pharmaceuticals, Inc. Double stranded constructs comprising one or more short strands hybridized to a longer strand
US8394947B2 (en) 2004-06-03 2013-03-12 Isis Pharmaceuticals, Inc. Positionally modified siRNA constructs
US7884086B2 (en) 2004-09-08 2011-02-08 Isis Pharmaceuticals, Inc. Conjugates for use in hepatocyte free uptake assays

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3788914T2 (en) * 1986-09-08 1994-08-25 Ajinomoto Kk Compounds for cleaving RNA at a specific position, oligomers used in the preparation of these compounds and starting materials for the synthesis of these oligomers.
US4843066A (en) * 1986-11-27 1989-06-27 Nippon Zoki Pharmaceutical Co., Ltd. Novel adenosine derivatives and pharmaceutical composition containing them as an active ingredient
FR2632955B1 (en) * 1988-06-20 1991-12-27 Oris Ind NUCLEOSIDE DERIVATIVES FOR USE IN THE SYNTHESIS OF MARKED OLIGONUCLEOTIDES, OLIGONUCLEOTIDES OBTAINED FROM SUCH DERIVATIVES AND THEIR SYNTHESIS
GB2226027B (en) * 1988-12-13 1992-05-20 Sandoz Ltd Adenosine derivatives,their production and use
JPH0372493A (en) * 1989-08-10 1991-03-27 Kikkoman Corp Production of 2'-o-substituted-adenosine-3',5'-cyclic phosphoric acid or its salt

Also Published As

Publication number Publication date
EP0524997B1 (en) 1994-08-10
EP0524997A1 (en) 1993-02-03
CA2080231A1 (en) 1991-10-10
DE59102512D1 (en) 1994-09-15
DE4037363A1 (en) 1991-10-10
ATE109788T1 (en) 1994-08-15
JPH07103150B2 (en) 1995-11-08
ES2059132T3 (en) 1994-11-01
CA2080231C (en) 2000-10-10
WO1991015499A1 (en) 1991-10-17
JPH05505197A (en) 1993-08-05

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