US 7,687,617 B2 · Oligonucleotides with alternating segments of locked and non-locked nucleotides

Abstract

The present invention is directed to novel oligonucleotides with improved antisense properties. The novel oligonucleotides comprise at least one Locked Nucleic Acid (LNA) selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides. The present invention also provides a new class of pharmaceuticals which comprise antisense oligonucleotides and are useful in antisense therapy.

Claims26

Dependent claims

An oligonucleotide which has the formula (In 5′ to 3′ order):

A-B-C-D, in which,
A represents a sequence of between 2-6 locked nucleotide units;
B represents a sequence of between 4-12 non-locked nucleotide units;
C represents a sequence of between 1-5 locked nucleotide units;
and
D represents a non-locked nucleotide unit or a sequence of between 1-3 non-locked nucleotide units;
and the overall length of the oligonucleotide is between 8-26 nucleotide units.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

10/717,434Filed 18 Nov 2003 · us provisional application

Priority

18 Nov 2002

Published

US 2009/0209748 A120 Aug 2009

Granted

30 Mar 2010

Term ends

Not estimatedThe source records don’t support an estimate.

Classification20 codes

C12N 15/113
DNA or RNA fragments; Modified forms thereof ; Non-coding nucleic acids having a biological activity: non-coding nucleic acids modulating the…
A61K 31/7088
Carbohydrates; Sugars; Derivatives thereof: compounds having three or more nucleosides or nucleotides
C07H 19/04
Sharing nitrogen: heterocyclic radicals containing only nitrogen atoms as ring hetero atom
C07H 19/06
Heterocyclic radicals containing only nitrogen atoms as ring hetero atom: pyrimidine radicals

Oligonucleotides with alternating segments of locked and non-locked nucleotides

Life of this patent

Oligonucleotides with alternating segments of locked and non-locked nucleotides

Life of this patent

Abstract

Claims26