| abstract |
The present invention relates to a prodrug and application thereof in the treatment of viral and cancerous diseases. Said prodrug inhibits HCV NS5B of HBV polymerase, DNA polymerase, and HIV-1 of reverse transcriptase (RT) and is used for the treatment of hepatitis B and C infection in mammals. n The present invention also relates to the prodrugs of general formula 1 and stereoisomers thereof and their isotopically enriched analogs, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polycrystalline forms of the prodrugs of general formula 1 and stereoisomers thereof, n n n n n n n n n n wherein n is 1 or 0; n Nuc is n n n n n n n n n n n n R 1 is hydrogen or methyl; n R 2 , R 3 are optionally identical substituents selected from H, F, Cl, CH 3 , OH provided that a solid line together with a dashed line above thereof ( ) denote a carbon-carbon single bond (C—C), or R 2 and R 3 denote hydrogen provided that a solid line together with a dashed line above thereof ( ) denote a carbon-carbon double bond (C═C); X is O, CH 2 or C═CH 2 ; Y is O, S, CH 2 or a HO—CH group provided that a solid line together with a dashed line above thereof ( ) denote a carbon-carbon single bond (C—C), or Y is a CH group provided that a solid line together with a dashed line above thereof ( ) denote a carbon-carbon double bond (C═C). |