Oligonucleotides having site specific chiral phosphorothioate internucleoside linkages
First Claim
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1. An oligomeric compound comprising a plurality of covalently-bound nucleosides;
- said compound having the formula;
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Abstract
Novel chiral compounds that mimic and/or modulate the activity of wild-type nucleic acids are disclosed. In general, the compounds are phosphorothioate oligonucleotides wherein the 5′, and the 3′-terminal internucleoside linkages are chirally Sp and internal internucleoside linkages are chirally Rp.
164 Citations
63 Claims
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1. An oligomeric compound comprising a plurality of covalently-bound nucleosides;
- said compound having the formula;
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 46, 47, 48)
- said compound having the formula;
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17. A nucleoside having the formula:
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wherein; Bx is a heterocyclic base moiety;
R4 is a hydroxyl protecting group;
R1 is H, hydroxyl, a protected hydroxyl, a 2′
-substituent group or a protected 2′
-substituent group; and
R2 is an Sp chiral auxiliary group. - View Dependent Claims (18, 19, 20, 21, 22, 23, 24)
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- 25. A method of preparing an oligomeric compound of formula:
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49. A compound of formula:
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wherein; R62 is H or a hydroxyl protecting group;
R1 is H, hydroxyl, a protected hydroxyl, a 2′
-substituent group or a protected 2′
-substituent group;
B is a heterocyclic base moiety; and
R61 is a chiral auxiliary selected from formulas I-VI;
- View Dependent Claims (50, 51, 52, 53)
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54. A compound having the formula:
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wherein; B is a heterocyclic base moiety;
q is 0 to about 50;
R62 is H or a hydroxyl protecting group;
R1 is H, hydroxyl, a protected hydroxyl, a 2′
-substituent group or a protected 2′
-substituent group;
R64 is H, a hydroxyl protecting group, or a linker to a solid support;
R63 is a radical selected from the group consisting of - View Dependent Claims (55, 56, 57, 58, 59, 60, 61, 62, 63)
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Specification