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1. WO1996004295 - 5'-DITHIO-MODIFIED OLIGONUCLEOTIDES

Publication Number WO/1996/004295
Publication Date 15.02.1996
International Application No. PCT/US1995/009475
International Filing Date 27.07.1995
Chapter 2 Demand Filed 26.02.1996
IPC
C07H 19/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
06Pyrimidine radicals
10with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
16Purine radicals
20with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 21/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
CPC
C07H 19/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
06Pyrimidine radicals
10with the saccharide radical esterified by phosphoric or polyphosphoric acids
C07H 19/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
16Purine radicals
20with the saccharide radical esterified by phosphoric or polyphosphoric acids
C07H 21/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
Applicants
  • AMGEN INC. [US/US]; Amgen Center 1840 Dehavilland Drive Thousand Oaks, CA 91320-1789, US
Inventors
  • RUSSO-RODRIGUEZ, Sandra, E.; US
  • KOGA, Tepper, M.; US
Agents
  • ODRE, Steven, M. ; Amgen Inc. Amgen Center 1840 Dehavilland Drive Thousand Oaks, CA 91320-1789, US
Priority Data
08/282,38329.07.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 5'-DITHIO-MODIFIED OLIGONUCLEOTIDES
(FR) OLIGONUCLEOTIDES A MODIFICATION 5'-DITHIO
Abstract
(EN)
The present invention provides nuclease resistant 5'-dithio-modified oligonucleotides that are useful in nucleic acid therapeutics and diagnostics. The novel modified oligonucleotides have at least one 5'-dithioate linkage, wherein both the oxygen atom at the 5'-position (5'-bridging oxygen) and at least one of the non-bridging oxygen atoms of a naturally occurring phosphodiester linkage are independently replaced with a single sulfur atom. The invention also provides a polymer-supported method for making 5'-dithio-modified and 5'-thio-modified oligonucleotides as well as novel monomeric nucleoside and nucleotide intermediates useful in the synthetic method.
(FR)
La présente invention concerne des oligonucléotides à modification 5'-dithio résistant aux nucléases et qui sont utiles dans les diagnostics et thérapies à base d'acide nucléique. Les nouveaux oligonucléotides modifiés présentent au moins une liaison 5'-dithioate dans laquelle, aussi bien l'atome d'oxygène en position 5' (oxygène pontant 5'), que l'un au moins des atomes d'oxygène non pontants d'une liaison phosphodiester survenant naturellement, sont remplacés indépendamment par un seul atome de soufre. L'invention concerne également un procédé à base de polymère permettant la production d'oligonucléotides à modification 5'-dithio et à modification 5'-thio, ainsi que des nouveaux intermédiaires de nucléosides et de nucléotides monomères utiles dans le procédé de synthèse.
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