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1. WO2000040592 - ACID STABLE BACKBONE MODIFIED END-BLOCKED NUCLEIC ACIDS AND THERAPEUTIC USES THEREOF

Publication Number WO/2000/040592
Publication Date 13.07.2000
International Application No. PCT/US1999/030266
International Filing Date 16.12.1999
Chapter 2 Demand Filed 23.05.2000
IPC
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
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
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
  • OLIGOS ETC. INC. [US/US]; Building C6 9775 SW Commerce Circle Wilsonville, OR 97070, US (AllExceptUS)
  • DALE, Roderic, M., K. [US/US]; US (UsOnly)
  • GATTON, Steven, L. [US/US]; US (UsOnly)
  • ARROW, Amy [US/US]; US (UsOnly)
Inventors
  • DALE, Roderic, M., K.; US
  • GATTON, Steven, L.; US
  • ARROW, Amy; US
Agents
  • FRANCIS, Carol, L.; Bozicevic, Field & Francis LLP Suite 200 200 Middlefield Road Menlo Park, CA 94025, US
Priority Data
09/223,49830.12.1998US
09/356,06919.07.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ACID STABLE BACKBONE MODIFIED END-BLOCKED NUCLEIC ACIDS AND THERAPEUTIC USES THEREOF
(FR) ACIDES NUCLEIQUES A EXTREMITES BLOQUEES, SQUELETTE MODIFIE ET STABILITE ACIDE ET LEURS UTILISATIONS THERAPEUTIQUES
Abstract
(EN)
The present invention provides end-blocked nucleic acids, e.g., 2'-O-R, 2'-O-R-O-R, 3'-O-R, and 3'-O-R-O-R oligonucleotides, that exhibit significant low pH stability, nuclease resistance and optionally antibacterial properties. These low toxicity, highly specific, acid stable, end-blocked nucleic acids represent a novel and improved oligonucleotide structure for therapeutic treatments of diseases. The 3' and 5' acid stable, exonuclease resistant polymers of the invention are shown here to provide antibacterial effects when applied $i(in vivo), e.g., applied topically to skin with actual sites of infection on dogs and humans.
(FR)
La présente invention concerne des acides nucléiques à extrémités bloquées tels que, par exemple, des oligonucléotides 2'-O-R, 2'-O-R-O-R, 3'-O-R et 3'-O-R-O-R, possédant une stabilité de pH faible, une résistance aux nucléases et éventuellement des propriétés antibactériennes. Ces acides nucléiques à extrémités bloquées, à faible toxicité, à haute spécificité et à stabilité acide représentent une nouvelle structure d'oligonucléotides améliorée destinée au traitement par voie thérapeutique d'affections. Les polymères résistants aux exonucléases à stabilité acide 3' et 5' de la présente invention possèdent des effets antibactériens lors de leur application $i(in vivo), c.-à-d. lors de leur application topique sur une peau présentant des sites effectifs d'infection chez les chiens et les humains.
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