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US 8,569,478 B2Granted
Modified 4′-nucleosides as antiviral agents
AssigneeGilead Pharmasset LLC
InventorsJinfa Du, Phillip Furman, Michael Joseph Sofia
Life of this patent
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Abstract
Compounds, methods and compositions for treating a host infected with human immunodeficiency virus and hepatitis B virus comprising administering an effective amount of a described 4′-C-substituted β-D- and β-L-nucleoside or a pharmaceutically acceptable salt or prodrug thereof, are provided.
Claims7
A compound which is a β-D- and β-L-nucleoside or a pharmaceutically acceptable salt thereof, having a structure defined by formula (I) or by formula (II):
- wherein:
- X is hydrogen, F, Cl, Br, I, NH2, NHR4, NR4R5, NHOH, NHOR4, NHNH2, NR4NH2, NHNHR4, SH, SR4, S(O)bR4, OH, OR4, N3, CN, or CF3;
- Y is hydrogen, F, Cl, Br, I, NH2, NHR4, NR4R5, NHOH, NHOR4, NHNH2, NR4NH2, NHNHR4, SH, SR4, S(O)bR4, OH, OR4, N3, CN, CF3, hydroxymethyl, methyl, substituted or unsubstituted ethyl, substituted or unsubstituted vinyl, substituted or unsubstituted 2-bromovinyl, or substituted or unsubstituted ethynyl;
- R1 is F or N3;
- R2 is OH, OR4, OC(O)R4, —OP(O)(OQ)a(NHR4)b, SH, SR4, S(O)bR4, SC(O)R4, NH2, NHC(O)R4, NHR4, NR4R5, NHOH, NHOR4, NHNH, NR4NH2, or NHNHR4;
- R3 is F, cyano, azido, ethynyl, chlorovinyl, fluorovinyl, alkyl (C2-6), one to three halogen substituted alkyl (C1-6), alkenyl or alkynyl (C2-6);
- Z is O, S, CH2 or C═CH2;
- A is N, CH, or CF;
- and
- R4 and R5 are the same or different and are lower alkyl, lower alkenyl, acyl of carbon 1-17, aryl, or aralkyl;
- M is at least one member selected from the group consisting of H+, Na+, and K+;
- and
- a has a value of 0 or 1, b has a value of 1 or 2, and Q is M or R4.
10 more elements
Dependencies are inferred from the claim text.