CARBOHYDRATE CONJUGATES AS DELIVERY AGENTS FOR OLIGONUCLEOTIDES
First Claim
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1. An iRNA agent comprising a compound having the structure shown in formula (I)
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Abstract
The present invention provides iRNA agents comprising at least one subunit of the formula (I):
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- wherein:
- A and B are each independently for each occurrence O, N(RN) or S;
- X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z′)(Z″)O-nucleoside, —P(Z′)(Z″)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z′)(Z″)O-Linker-OP(Z′″)(Z″″)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z′)(Z″)-formula (I), —P(Z′)(Z″)— or -Linker-R;
- R is LG, -Linker-LG, or has the structure shown below:
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- LG is independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide;
- RN is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and
- Z′, Z″, Z′″ and Z″″ are each independently for each occurrence O or S.
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Citations
19 Claims
- 1. An iRNA agent comprising a compound having the structure shown in formula (I)
- 2. An iRNA agent comprising a compound having the structure shown in formula (I′
Specification