NUCLEOTIDES INCLUDING N-[(S)-1-CYCLOBUTOXYCARBONYL]PHOSPHORAMIDATE FRAGMENT, THEIR ANALOGS AND THEIR APPLICATION Russian patent published in 2018 - IPC C07H19/10 C07H19/20 C07F9/36 C07F9/44 C07F9/6561 A61K31/7076 A61K31/7072 A61K31/708 A61K31/664 A61K31/675 A61P31/20 A61P31/18 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to prodrug corresponding to the general formula 1, its stereoisomer, a pharmaceutically acceptable salt, optionally in crystalline and polycrystalline form, which has antiviral activity. In general formula 1 n has the value 1 or 0; Nuc is or , R¹ is hydrogen or methyl; R², R³ are optionally identical substituents selected from H, F, Cl, CH₃ if the solid line and the dotted line accompanying it () together represent a single carbon-carbon bond (C-C), or R² and R³ are hydrogen, when the solid line and the accompanying dotted line () together represent a carbon-carbon double bond (C=C); R⁴ is substituent selected from R^4.1–R^4.5: ; R^3.6 is substituent selected from H, F, Cl, CH₃ or CF₃; R^3.7 is hydrogen, C₁-C₄-alkyl or C₃-C₆-cycloalkyl; X is O, CH₂ or C=CH₂; Y represents S, CH₂ or HO-CH-group provided that the continuous line and the accompanying dotted line ( ) together represent a single carbon-carbon bond (C-C), or Y is CH-group provided that the solid line and the accompanying dotted line ( ) together represent a carbon-carbon double bond (C=C).

EFFECT: prodrug can be used in treatment of viral diseases mediated by the activity of NS5B HCV polymerase HBV, DNA polymerase and HIV-1 reverse transcriptase (RT), in particular for treatment of hepatitis B and C-infection.

4 cl, 6 tbl, 14 ex