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US 2006/0040890 A1Published application
Anti-viral nucleosides
AssigneeRoche Palo Alto LLC
InventorsJoseph Martin, Keshab Sarma, David Smith
Life of this patent
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Abstract
4-Amino-1-((2R,3S,4S,5R)-5-azido-3,4-dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (I:R1=R2=R3=R4=H) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.
Claims23
A compound of formula I
- wherein:
- R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, COR5, C(═O)OR5, C(═O)SR5, C(═O)NHR5 and COCH(R6)NHR7;
- R5 is independently selected from the group consisting of C1-8 unbranched or branched alkyl, C1-18 unbranched or branched alkenyl, C1-18 unbranched or branched alkynyl, C1-18 lower haloalkyl, C3-8 cycloalkyl, C3-8 cycloalkyl-C1-3 alkyl, phenyl optionally substituted with one to three substituents independently selected from the group consisting of halo, C1-6 alkyl, C1-6 lower alkoxy, C1-6 lower thioalkyl, C1-6 lower alkyl sulfinyl, C1-6 lower alkyl sulfonyl, nitro and cyano, CH2Ph wherein in phenyl ring is optionally substituted as described above, and CH2OPh wherein in phenyl ring is optionally substituted as described above;
- R6 is independently selected from the group consisting of the side chains of naturally occurring amino acids and C1-5 unbranched or branched alkyl;
- R7 is selected from the group consisting of hydrogen and R5OCO;
- or,
- R6 and R7 taken together are (CH2)3;
- and,
- hydrates, solvates, clathrates and acid addition salts thereof.
6 more elements
Dependencies are inferred from the claim text.