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US 2019/0169185 A1Published application
Substituted 2-n-hydroxy-1,3-dioxo-1,2,3,4-tetrahydronaphthyridines, and methods of making and using same
AssigneeArbutus Biopharma Corporation
InventorsRAMESH D. KAKARLA, BRUCE D. DORSEY
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Abstract
The present invention includes novel substituted 2-N-hydroxy-1,3-dioxo-1,2,3,4-tetrahydronaphthyridines, which can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention inhibit HBV RNAse H activity.
Claims25
A compound of formula (I):
- wherein:
- R1 is selected from the group consisting of —OR′ and —NR′R′, wherein each occurrence of R′ is independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C8 cycloalkyl, optionally substituted benzyl, optionally substituted aryl, and optionally substituted heteroaryl;
- each of X1, X2, X3, and X4 is independently selected from the group consisting of N and CR3, with the proviso that 1-2 of X1, X2, X3, and X4 are N;
- R2 and R3 are independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, halo, —CN, —OR″, —NR″R″, —N(C0-C6 alkyl)C(═O)R″, —N(C0-C6 alkyl) S(═O)2R″, —NO2, —S(═O)2NR″R″, —OC(═O)R″, and —C(═O)O—C1-C6 alkyl, wherein each occurrence of R″ is independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, optionally substituted C3-C8 cycloalkyl, and optionally substituted phenyl;
- and
- n is 0, 1, 2, 3, or 4;
- or a salt, solvate, geometric isomer, stereoisomer, tautomer, or any mixtures thereof
4 more elements
Dependencies are inferred from the claim text.