AMIDES OF QUINOLINE AND QUINAZOLINE, USEFUL AS A SODIUM CHANNEL MODULATORS Russian patent published in 2019 - IPC C07D215/54 C07D241/44 C07D401/12 C07D403/12 C07D413/12 C07D417/12 A61K31/465 A61K31/4709 A61K31/498 A61P25/00 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of the formula I, where Y is CH or N; Ar¹ is a 5–6 membered aromatic monocyclic ring containing 0–4 heteroatoms, independently selected from nitrogen, oxygen and sulphur, where said ring is optionally condensed with a 5-membered monocyclic aromatic ring containing 2–3 heteroatoms, independently selected from nitrogen, where Ar¹ contains m substituents, each of which is independently selected from -WR^W, or Ar¹ is , or ; m is an integer from 0 to 1 inclusive; W is a bond or C₁C₂alkyl, where is one element CH₂ mentioned C₁C₂alkyl may be replaced by -CO- or -SO₂-; R^W absent, represents H, OH, NH₂, NHR′, CN or 5-membered fully unsaturated monocyclic ring containing 4 heteroatoms, independently selected from nitrogen; R′ is a C₁C₆alkyl; R¹ R², R³, R⁴ R⁵, R^6′ represent H; R⁵ R⁶, R⁷ are H, halogen r-XR^X; X is C₁C₃alkyl, where said C₁C₃alkyl is substituted with 0–3 halogen, where one element is CH₂ mentioned C₁-C₃alkyl may be replaced by -O-; and R^X missing; or 3-(4-fluorophenoxy)-N-(2-oxo-1,2-dihydropyridin-4-yl)quinoxaline-2-carboxamide; or 3-(4-fluoro-2-methoxyphenoxy)-N-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)quinoxaline-2-carboxamide. Invention also relates to a pharmaceutical composition based on a compound of the formula I, a method for inhibiting a voltage-dependent sodium channel, and a method for treating or alleviating the severity of pain. I.

EFFECT: new heterocyclic compounds with the ability to inhibit sodium channels are obtained.

42 cl, 3 tbl, 13 ex