PAN-GENOMIC INHIBITORS OF THE HEPATITIS C VIRUS PROTEIN NS5A, PHARMACEUTICAL COMPOSITIONS, INTERMEDIATES FOR THE SYNTHESIS OF INHIBITORS, AND METHODS FOR THEIR PREPARATION AND USE Russian patent published in 2018 - IPC C07D403/04 C07D403/14 A61K31/4178 A61P31/12 A61P31/20 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a novel compound of Formula 1, or a pharmaceutically acceptable salt or stereoisomer thereof. Compounds possess the properties of the NS5A inhibitor of hepatitis C virus and can be used in the treatment of hepatitis C. In the compound of the general formula 1

R1 is hydrogen, tert-butoxycarbonyl, or

where R11 is unsubstituted C₁-C₆ alkyl, unsubstituted C₃-C₆ cycloalkyl or unsubstituted C₁-C₆ alkyloxy, and arrows (←) indicate the place of addition of substituents; R2 is hydrogen, halogen or C₁-C₄ alkyl; R3 is optionally substituted phenyl, optionally substituted phenyloxy, optionally substituted phenylsulfanyl, optionally substituted phenyl (N-C₁-C₄alkyl)amino, naphthyl or 6-membered nitrogen-containing hetaryl, wherein the phenyl in each of said groups may be substituted with halogen, C₁-C₄ alkyl, nitro, N-mono- or N, N-dialkylamine, phenyl, 6-membered heterocycle with 2 nitrogen atoms in the ring which is substituted by C₁-C₄ alkyl; R4 is

,

where R41 is unsubstituted C₁-C₆ alkyloxy; X is but-1,3-dinylene or 1,4-phenylene; arrows (←) indicate the place of addition of substituents. Invention also relates to intermediates of formulas 3 and 4 for the preparation of a compound of formula 1

,

where W is iodine, 4-trimethylsilanyl-buta-1,3-diynyl and buta-1,3-diynyl; R43 has the values corresponding to R1; R1, R2, R3 are as defined above.

EFFECT: pharmaceutically acceptable salt is provided.

9 cl, 27 ex, 3 tbl