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US 7,833,992 B2Granted
Conjugates and compositions for cellular delivery
AssigneeMerck Sharpe & Dohme Ltd.
InventorsChandra Vargeese, Peter Haeberli, Weimin Wang, Tongqian Chen
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Abstract
This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol 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.
Claims3
A compound having Formula 107:
- wherein X comprises a short interfering RNA (siRNA) comprising 2′-fluoro pyrimidines and 2′-O-methyl purines;
- each W independently comprises a linker molecule selected from the group consisting of amide, phosphate, phosphate ester, phosphoramidate, thiophosphate ester linkage, and R3(CH2)2O(CH2)2(OCH2CH2)nO(CH2)2NHC(=0)—, where n is independently an integer from about 1 to about 20;
- 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, or N;
- and Cholesterol comprises cholesterol.
2 more elements
Dependencies are inferred from the claim text.