SODIUM CHANNEL BLOCKERS, PREPARATION METHOD THEREOF AND USE THEREOF Russian patent published in 2018 - IPC C07D417/14 C07D417/12 A61K31/427 A61K31/443 A61P29/00 

FIELD: biochemistry.

SUBSTANCE: invention relates to a compound represented by formula 1 or a pharmaceutically acceptable salt thereof, where R₁ – aryl or heteroaryl selected from the group consisting of phenyl, pyridinyl, pyrimidinyl, furanyl, isoxazolyl, pyrazolyl and thienyl, wherein aryl or heteroaryl is unsubstituted or substituted by one or two substituents independently selected from the group consisting of halogen, consisting of C_1–4alkyl, C_1–4haloalkyl and halogen; R₂ – heteroaryl selected from the group consisting of furanyl, imidazolyl, isoxazolyl, pyrazolyl, pyridinyl, pyrimidinyl, thiazolyl and thienyl, wherein heteroaryl is unsubstituted or substituted with one or two substituents independently selected from the group consisting of halogen, consisting of C_1–4alkyl, C_3–6cycloalkyl, halogen, morpholino, piperazinyl, piperidinyl, pyridinyl and pyrrolidinyl; R₃ – thiazolyl or thiadiazolyl; X₁ – CH; X₂ – N or X₁ – N; X₂ – CH; Y – O; Z – CR₄, and R₄ – H, halogen or CN; R₅ – H or halogen. Invention also relates to a compound represented by formula 1, or a pharmaceutically acceptable salt thereof, where R₁ – hydrogen, halogen or aryl or heteroaryl, selected from the group consisting of phenyl, pyridinyl and furanyl, wherein aryl or heteroaryl is unsubstituted or substituted by halogen; R₂ – aryl or heteroaryl, selected from the group consisting of furanyl, phenyl, pyrazolyl and pyridinyl, where aryl or heteroaryl is unsubstituted or substituted by C_1–4alkyl; R₃ – thiazolyl; X₁ – CH or N; X₂ – CH or N with the proviso that at least one of X₁ and X₂ is CH; Y – CH(OH); Z – CR₄, where R₄ is H or halogen; R₅ – H. Invention relates to a pharmaceutical composition for preventing or treating a disease, associated with sodium channel blocker Nav1.7, and to relieve pain, associated with sodium channel blocker Nav1.7 containing a compound or a pharmaceutically acceptable salt thereof of formula (1) as an active ingredient and a pharmaceutically acceptable carrier, adjuvant or diluent. Technical result – compounds having a blocking effect on sodium channels Nav1.7. [Formula 1].

EFFECT: compounds that have a blocking effect on sodium channels.

11 cl, 158 ex, 4 tbl