A class of 2-fluoro-nucleoside compounds are disclosed which are useful
in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal
cellular proliferation, including tumors and cancer. The compounds have the general
formulae:
##STR1##
wherein
- Base is a purine or pyrimidine base;
- R1 is OH, H, OR3, N3, CN, halogen,
including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino,
or alkoxy, and base refers to a purine or pyrimidine base;
- R2 is H, phosphate, including monophosphate, diphosphate,
triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically
acceptable leaving group which when administered in vivo, is capable of providing
a compound wherein R2 is H or phosphate; sulfonate ester including alkyl
or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group
is optionally substituted with one or more substituents as described in the definition
of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and
- R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable
leaving group which when administered in vivo, is capable of being cleaved to the
parent compound, or a pharmaceutically acceptable salt thereof.
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