MACROHETEROCYCLIC NUCLEOSIDE DERIVATIVES AND ANALOGUES THEREOF, PRODUCTION AND USE Russian patent published in 2020 - IPC C07H19/10 C07H19/20 A61K31/7064 A61K31/7068 A61K31/7072 A61P1/16 A61P31/12 A61P31/18 A61P35/00 

FIELD: medicine.

SUBSTANCE: present invention relates to a derivative applicable in medicine, a composition based thereon and preparation thereof. Disclosed is a derivative of formula 1 or 2, their stereoisomer

where Ar is phenyl; R¹ and R² are selected from H, F, Cl, CH₃, OH; R³ represents H or CH₃; X is oxygen or ethanediyl-1,1(C=CH₂); Y is CH(R⁴)(CH₂)_k, CH(R⁴)(CH₂)_mC(O)O(CH₂)_n; R⁴ denotes H or CH₃; k has value from zero to six; m has a value from zero to two; n has value from one to four; Q is a radical selected from Q1–Q4;

where R⁵ is a substitute selected from H, F, Cl, CH₃, OH; arrow (→) indicates connection point Q1–Q4. Disclosed process for producing compounds according to claim 1 or 2 includes cyclisation of acid of formula 3 or 16

where Ar, R¹, R², R³, X, Y and Q are defined above. What is presented is a novel effective derivative for treating hepatitis C and an effective process for preparing it, as well as a pharmaceutical composition based thereon.

EFFECT: disclosed derivative is a pro-drug for treating viral diseases and is an inhibitor of HCV NS5B polymerase, HBV DNA polymerase and HIV-1 reverse transcriptase.

10 cl, 19 ex