| abstract |
REFERS TO THE USE OF PURINE AND PYRIMIDINE NUCLEOSIDE DERIVATIVES OF FORMULA I WHERE R IS H, [P (O) (OH) -O] nH; n IS 1-3; R1 IS ALKYL, ALKENYL, ALKINYL, HALOALKYL, ALKYLCARBONYL, ALCOXYCARBONYL, HYDROXYALKYL, ALCOXYALKYL, AMONG OTHERS; R2 IS H, HYDROXYL, AMINE, ALKYL, HYDROXYALKYL, ALCOXYL, HALOGEN, CYANE, AZIDO; R3 AND R4 ARE H, OH, ALCOXYL, HALOGEN, HYDROXYALKYL; ONE OF R3 AND R4 IS H; OR TOGETHER THEY ARE = CH2, = NOH, X IS O, S, CH2; B IS FORMULA B1 9-PURINYL; R5 IS H, OH, ALKYL, ALCOXYL, ALKYLTIO, NHR8, HALOGEN, SH; R6 IS HYDROXYL, NHR8, NHOR9, NHNR8, NHCOOR9 ', SH; R7 IS H, HYDROXYL, ALKYL, ALCOXYL, ALKYLTIO, NHR8, HALOGEN, SH, CYANE; R8 IS H, ALKYL, HYDROXYALKYL, ARYLCARBONYL, ALKYLCARBONYL; R9 IS H, ALKYL; R9 'IS ALKYL; B IS 1-PYRIMIDYL B2; Z IS O, S; R10 IS HYDROXYL, NHR8, NHOR9, NHNR8; NHCOOR9 ', SH; R11 IS H, ALKYL, HYDROXYL, HYDROXYALKYL, ALCOXYALKYL, HALOALKYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE 4'-C-ETHINYLCITIDINE; 4'-C-ETHOXICITIDINE; 4'-C-ACETYL CYTIDINE, 4'-C-AZIDOCITIDINE, 4'-CYANOCITIDINE, AMONG OTHERS. COMPOUNDS I ARE REPLICATION INHIBITORS OF THE SUBGENOMIC RNA OF THE HEPATITIS C VIRUS AND MAY BE USEFUL FOR THE TREATMENT OF HEPATITIS C |