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US 2018/0023081 A1Published application
Lna oligonucleotides with alternating flanks
AssigneesBristol-Myers Squibb Company, Roche Innovation Center Copenhagen A/S
InventorsPeter HAGEDORN, Richard E. OLSON, Anja Mølhart HØG, Marianne Lerbech JENSEN, Dong LI, Niels Fisker NIELSEN
Life of this patent
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Abstract
The present invention relates to LNA oligomers having two flanks, wherein one or both flanks comprise alternating LNA and DNA nucleosides.
Claims18
An oligomer of at least 10 contiguous nucleotides in length, comprising region A, region B, and region C (A-B-C),
- wherein region B comprises at least 5 consecutive nucleoside units and is flanked at 5′ by region A of 1-8 contiguous nucleoside units and at 3′ by region C of 1-8 contiguous nucleoside units, wherein region B, when formed in a duplex with a complementary RNA, is capable of recruiting RNaseH, and
- wherein region A and region C are selected from the group consisting of:
- (i) region A comprises a 5′ LNA nucleoside unit and a 3′ LNA nucleoside unit, and at least one DNA nucleoside unit between the 5′ LNA nucleoside unit and the 3′ LNA nucleoside unit, and, region C comprises at least two 3′ LNA nucleosides;
- or
- (ii) region A comprises at least one 5′ LNA nucleoside and region C comprises a 5′ LNA nucleoside unit, at least two terminal 3′ LNA nucleoside units, and at least one DNA nucleoside unit between the 5′ LNA nucleoside unit and the 3′ LNA nucleoside units, and
- (iii) region A comprises a 5′ LNA nucleoside unit and a 3′ LNA nucleoside unit, and at least one DNA nucleoside unit between the 5′ LNA nucleoside unit and the 3′ LNA nucleoside unit;
- and region C comprises a 5′ LNA nucleoside unit, at least two terminal 3′ LNA nucleoside units, and at least one DNA nucleoside unit between the 5′ LNA nucleoside unit and the 3′ LNA nucleoside units.
4 more elements
A conjugate comprising the oligomer according to any one 1-12 covalently attached to at least one non-nucleotide or non-polynucleotide moiety.
Dependencies are inferred from the claim text.