IP Library › Granted Patent US 7,964,578
Granted Patent B2
US 7,964,578 · App. 12/253,156 · Granted Jun 21, 2011

Conjugates and compositions for cellular delivery

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Quick Facts
Patent No.
US 7,964,578
App. No.
12/253,156
Granted
Jun 21, 2011
Kind
B2
Abstract

This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol, folate, galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.

Claims (12)

1. A compound having Formula 107:

wherein X comprises a short interfering nucleic acid (siNA) molecule; each W independently comprises a linker molecule or chemical linkage selected from the group consisting of amide, phosphate, phosphate ester, phosphoramidate, or thiophosphate ester linkage, Y comprises a linker molecule that can be present or absent; each R1, R2, R3, and R4 independently comprises O, OH, H, alkyl, alkylhalo, O-alkyl, O-alkylcyano, S, S-alkyl, S-alkylcyano, N, amide, alkylamine, aminoacid, polyamine, cyclic amine or heterocyclic amine, and Cholesterol comprises cholesterol.

2. A compound having the formula below:

wherein X comprises a short interfering nucleic acid (siNA) molecule; each W independently comprises a linker molecule or chemical linkage selected from the group consisting of amide, phosphate, phosphate ester, phosphoramidate, or thiophosphate ester linkage, Y comprises a linker molecule that can be present or absent; each R1, R2, R3, and R4 independently comprises O, OH, H, alkyl, alkylhalo, O-alkyl, O-alkylcyano, S, S-alkyl, S-alkylcyano, N, amide, alkylamine, aminoacid, polyamine, cyclic amine or heterocyclic amine; and n is independently an integer from about 1 to about 20.

3. A compound having Formula 111:

wherein X comprises a short interfering nucleic acid (siNA) molecule capable of mediating RNA interference (RNAi); W comprises a linker molecule or chemical linkage that can be present or absent, and when present, forms only one covalent bond to the siNA molecule; and n is an integer from about 1 to about 20.

4. The compound of claim 1 , wherein W comprises a linker molecule or chemical linkage selected from the group consisting of amide, phosphate, phosphate ester, phosphoramidate, or thiophosphate ester linkage.

5. The compound of claim 3 , wherein W comprises a linker molecule or chemical linkage selected from the group consisting of amide, phosphate, phosphate ester, phosphoramidate, or thiophosphate ester linkage.

6. The compound of claim 1 , wherein said siNA molecule comprises a sense strand and an antisense strand, and wherein said sense strand is conjugated with a compound comprising Formula 107.

7. The compound of claim 3 , wherein said siNA molecule comprises a sense strand and an antisense strand, and wherein said sense strand is conjugated with a compound comprising Formula 107.

8. The compound of claim 2 , wherein W comprises a linker molecule or chemical linkage selected from the group consisting of amide, phosphate, phosphate ester, phosphoramidate, or thiophosphate ester linkage.

9. The compound of claim 2 , wherein the siNA molecule comprises a sense strand and an antisense strand, and wherein the sense strand is conjugated with a compound of claim 2 .