| abstract |
2'-Fluoronucleoside compounds are described, which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cell proliferation, including tumors and cancer. The compounds have the general formula (I), (II), (III), (IV) where the base is a purine or pyrimidic base, R1 is OH, H, OR 3, n3, CN, halogen, including F or CF3, lower alkyl, amino, lower alkylamino, dialkylamino (lower) or alkoxy and the base refers to a pure or pyrimidic 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 where R2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl, including methanesulfonyl, benzyl, where the phenyl group is optionally substituted with one or more substituents as described in the definition of the aryl given above, a lipid, an amino acid, peptide or cholestereol, and R2 is acyl, alkyl, phosphate or other pharmaceutically acceptable leaving group, which when administered in vivo can be cleaved to the original compound or a pharmaceutically acceptable salt thereof. |