Oligomeric compounds and methods
First Claim
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1. An oligomeric compound comprising an antisense oligonucleotide consisting of 16 to 30 linked nucleosides having the formula:
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5′
-Q-(E)w-(A)2-(B)x-(A)2-(C)y-(A)3-Dwherein;
each A is a 2′
-OCH3 modified nucleoside;
each E is, independently, a 2′
-F or a 2′
-OCH3 modified nucleoside wherein at least the E that is linked to the adjacent 5′
-A is a 2′
-F modified nucleoside;
each B and C is a 2′
-F modified nucleoside;
D is H or 3′
-terminal group;
Q is a 5′
-phosphate stabilizing nucleoside comprising;
i) a 5′
-terminal modified phosphate; and
ii) a 2′
-substituent group selected from F, O—
(CH2)2—
O—
CH3, and OCH3;
w is from about 4 to about 10;
x is from about 2 to about 4; and
y is from about 3 to about 8.
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Abstract
The present invention provides oligomeric compounds and uses thereof. In certain embodiments, such oligomeric compounds are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds or as RNAi compounds.
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Citations
21 Claims
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1. An oligomeric compound comprising an antisense oligonucleotide consisting of 16 to 30 linked nucleosides having the formula:
-
5′
-Q-(E)w-(A)2-(B)x-(A)2-(C)y-(A)3-Dwherein; each A is a 2′
-OCH3 modified nucleoside;each E is, independently, a 2′
-F or a 2′
-OCH3 modified nucleoside wherein at least the E that is linked to the adjacent 5′
-A is a 2′
-F modified nucleoside;each B and C is a 2′
-F modified nucleoside;D is H or 3′
-terminal group;Q is a 5′
-phosphate stabilizing nucleoside comprising;i) a 5′
-terminal modified phosphate; andii) a 2′
-substituent group selected from F, O—
(CH2)2—
O—
CH3, and OCH3;w is from about 4 to about 10; x is from about 2 to about 4; and y is from about 3 to about 8. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)
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Specification