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
Authors
Dates
2020-09-02—Published
2017-08-23—Filed