1,2,5-OXADIAZOLE DERIVATIVES, HAVING ANTI-HIV ACTIVITY, PHARMACEUTICAL COMPOSITION, METHOD OF INHIBITING HIV-1 INTEGRASE Russian patent published in 2014 - IPC C07D271/08 C07D271/12 C07D413/04 C07D498/04 A61K31/4245 A61K31/443 A61P31/18 

FIELD: chemistry.

SUBSTANCE: invention relates to use of nucleoside derivatives - 1,2,5-oxadiazoles of general structural formula I where R¹ and R² are selected from phenylsulphonyl, substituted with one or more halogen atoms, nitro groups, carboxy groups, alkyl halides, CH₃, OCH₃, OCF₃; X is selected from N or N→O; or R¹ and R² form a group, where R', R", R'" and R'''' are independently selected from hydrogen; halogens; nitro groups, hydroxy group, carboxy group, CH₃; CH₂Br; OCH₃; phenylsulphonyl; phenylthio group; or the following groups: R' and R" can also be merged into one of the following common rings for inhibiting human immunodeficiency virus (HIV) replication. The invention also relates to a pharmaceutical composition based on compounds of formula I and a method of inhibiting HIV-1 subtypes A and B integrase, including forms which are resistant to raltegravir.

EFFECT: detecting novel activity in compounds of formula I, which can be used in medicine as HIV replication inhibitors.

3 cl, 5 tbl, 4 ex