TRICYCLO-PHOSPHOROTHIOATE DNA
First Claim
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1. A nucleic acid molecule comprising tricyclo-nucleosides joined by internucleoside phosphorothioate linkages (3′
- -OPS-O-5′
linkages).
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Abstract
The present invention relates to a nucleic acid molecule containing a sequence of tricyclo nucleosides joined by internucleoside phosphorothioate linkage. The invention also relates to synthetic antisense oligonucleotides and to methods employing the same.
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Citations
21 Claims
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1. A nucleic acid molecule comprising tricyclo-nucleosides joined by internucleoside phosphorothioate linkages (3′
- -OPS-O-5′
linkages). - View Dependent Claims (2, 3, 4, 5, 7, 8, 15, 16, 17, 18, 19, 20, 21)
- -OPS-O-5′
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6. A method for synthesizing a tricyclo-phosphorothioate DNA molecule, the method comprising:
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a) providing a first tricyclo-nucleoside bound to a solid phase support, said first nucleotide having a protected 5′
-OH group;b) deprotecting the 5′
group to form a free 5′
-OH group;c) reacting the free 5′
-OH group with a 5′
-protected tricyclonucleoside-3′
-O-cyanoethyl-N,N-diisopropylaminophosphoramidite monomer to form an internucleoside phosphoramidite linkage between the first and a second tricyclo-nucleosides; andd) sulfurizing the internucleoside phosphoramidite group to form a phosphorothioate internucleoside linkage between the first and second tricyclo-nucleosides.
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9. (canceled)
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10. (canceled)
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11. (canceled)
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12. (canceled)
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13. (canceled)
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14. (canceled)
Specification