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US 10,329,542 B2Granted
HBV RNAse H purification and enzyme inhibitors
AssigneeSaint Louis University
InventorsJohn Tavis, Yuan Hu
Life of this patent
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Abstract
Provided herein are methods for the obtention of an active HBV RNaseH preparation and its use in screening methods to identify potential inhibitors of the enzyme for possible use as therapeutic agents. Also provided are methods of treatment using agents identified according to the screen.
Claims20
A method of inhibiting a hepatitis B virus (HBV) RNAseH comprising contacting said enzyme with a compound having the formula:
- wherein:
- R11 is hydrogen, —OR17, hydroxy, or halo, wherein R17 is C1-C8 acyl, C1-C8 alkyl, or a substituted version of either of these groups;
- R12 is hydrogen, hydroxy or halo;
- R13 and R14 are each independently hydrogen, hydroxy, nitroso, C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, C1-C12 aryl, C1-C12 aralkyl, C1-C12 amido, a substituted version of any of these groups, or R13 is taken together with R14 as provided below;
- R15 is hydrogen, C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, C1-C12 aryl, C1-C12 aralkyl,
- or a substituted version of any of these groups;
- and
- R16 is hydrogen, unsubstituted C1-C6 alkyl, substituted C1-C6 alkyl, or hydroxyl;
- provided that when R13 and R14 are taken together as further defined by FORMULA IV:
- R18 and R19 are each independently hydrogen, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl.
7 more elements
Dependencies are inferred from the claim text.