Oligomeric compounds and compositions for the use in modulation of micrornas
AssigneeIsis Pharmaceuticals, Inc.
InventorsChristine Esau, Eric E. Swayze, Balkrishen Bhat, Garth A. Kinberger
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Abstract
Compounds, compositions and methods are provided for modulating the levels expression, processing and function of miRNAs. The compositions comprise oligomeric compounds targeted to small non-coding RNAs and miRNAs. The oligomeric compounds possess potent miRNA inhibitory activity, and further exhibit improved therapeutic index. Further provided are methods for selectively modulating miRNA activity in a cell.
Claims34
An oligomeric compound comprising an oligonucleotide consisting of 17 to 29 nucleosides linked by internucleoside linking groups, said oligonucleotide having an internal region located between two external regions, wherein each external region independently comprises from 1 to about 3 nucleosides, each external region comprises a stabilizing modification, and the internal region comprises at least 10-D-2′-deoxy-2′-fluororibofuranosyl nucleosides.
-13. (canceled)
An oligomeric compound comprising an oligonucleotide having the formula:
- 5′-T1-(Nu1-L1)n1-(Nu2-L2)n2-Nu2-(L3-Nu3)n3-T2-3′
- wherein:
- each Nu1 and Nu3 is, independently, a stabilizing nucleoside;
- at least 10 Nu2 are -D-2′-deoxy-2′-fluororibofuranosyl nucleosides;
- each L1, L2 and L3 is, independently, an internucleoside linking group;
- each T1 and T2 is, independently, H, a hydroxyl protecting group, an optionally linked conjugate group or a capping group;
- n1 is from 0 to about 3;
- n2 is from about 14 to about 22;
- n3 is from 0 to about 3;
- and
- provided that if n1 is 0 then T1 is not H or a hydroxyl protecting group, and if n3 is 0, then T2 is not H or a hydroxyl protecting group.
15-71. (canceled)
An oligomeric compound comprising an oligonucleotide having the formula I:
- T1-(Nu1)n1-(Nu2)n2-(Nu3)n3-(Nu4)n4-(Nu5)n5-T2, wherein:
- Nu1 and Nu5 are, independently, 2′ stabilizing nucleosides;
- Nu2 and Nu4 are -D-2′-deoxy-2′-fluororibofuranosyl nucleosides;
- Nu3 is a 2′-modified nucleoside;
- each of n1 and n5 is, independently, from 0 to 3;
- the sum of n2 plus n4 is between 10 and 25;
- n3 is from 0 and 5;
- and
- each T1 and T2 is, independently, H, a hydroxyl protecting group, an optionally linked conjugate group or a capping group.
77-78. (canceled)
(canceled)
85-86. (canceled)
(canceled)
Dependencies are inferred from the claim text.