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US 9,309,513 B2Granted
MicroRNA compounds and methods for modulating miR-122
AssigneeRegulus Therapeutics Inc.
InventorsBalkrishen Bhat, Daniel Hogan
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Abstract
Described herein are compositions and methods for the inhibition of miR-122 activity. The compositions have certain nucleoside modifications that yield potent inhibitors of miR-122 activity. The compounds may comprise conjugates to facilitate delivery to the liver. The compositions may be administered to subjects infected with hepatitis C virus, as a treatment for hepatitis C virus and related conditions.
Claims15
A method of treating an HCV infection comprising administering to an HCV-infected human a therapeutically effective amount of a pharmaceutical composition comprising a compound of the structure:
- wherein X is a phosphodiester linkage;
- m is 1;
- N in Nm is a β-D-deoxyriboadenosine;
- Y is a phosphodiester linkage;
- and MO is a modified oligonucleotide having the structure AEMeCEAEMeCEMeCEAETETGUSCSACSACSTCSCS (SEQ ID NO:
- 4), wherein the superscript “Me” indicates 5-methylcytosine, wherein nucleosides not followed by a subscript are β-D-deoxyribonucleosides, nucleosides followed by a subscript “E” are 2′-MOE nucleosides, nucleosides followed by a subscript “S” are S-cEt nucleosides, and each internucleoside linkage is a phosphorothioate internucleoside linkage;
- and wherein Y is linked to the 3′ terminus of the modified oligonucleotide;
- and
- one or more pharmaceutically acceptable excipients.
6 more elements
Dependencies are inferred from the claim text.