摘要 |
The present invention relates to 2′-Fluoro-6′-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses. |
主权项 |
1. A nucleoside compound according to the structure: Where B is Wherein R is H, F, Cl, Br, I, C1-C4 alkyl (preferably CH3), —C≡N, —C≡C—Ra, X is H, C1-C4 alkyl (preferably, CH3), F, Cl, Br or I; Ra is H or a —C1-C4 alkyl group; R1 and R1a are each independently, H, an acyl group, a C1-C20 alkyl or ether group, an amino acid residue (D or L), a phosphate, diphosphate, triphosphate, phosphodiester or phosphoramidate group or together R1 and R1a form a carbodiester or phosphodiester group with the oxygen atoms to which they are bonded; R2 is H, an acyl group, a C1-C20 alkyl or ether group or an amino acid residue (D or L); Or a pharmaceutically acceptable salt, or enantiomer thereof. |