AMINO ACID DERIVATIVES FOR TREATING INFLAMMATORY DISEASES Russian patent published in 2025 - IPC C07D401/04 C07D401/14 C07D403/14 C07D405/14 C07D495/04 A61K31/444 A61K31/4709 A61P29/00 A61P37/06 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, which have inhibitory activity on nuclear factor-kappa B (NF-kB). In formula (I) n is equal to 0, 1 or 2; dotted line is an optional link; Het is pyridin-3-yl; R¹ is hydrogen; R² is hydrogen; R³ is hydrogen, alkyl, cycloalkylalkyl or aralkyl; R⁴ is hydrogen and R⁵ is -C(O)R⁶, R⁶ is aryl or heteroaryl, where aryl or heteroaryl is optionally substituted with R^g, R^h and/or Rⁱ independently selected from alkyl, C₁-C₆ alkoxy, halogen, halogen-C₁-C₆ alkyl, nitro, amino, C₁-C₆ alkylamino and acylamino; acylamino is -NR'C(O)R, where R' is hydrogen or alkyl and where R is C₁-C₆ alkyl or C₃-C₁₀ cycloalkyl, where C₁-C₆ alkyl can be substituted with amino or 2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl; or R⁴ and R⁵ together with the nitrogen atom to which they are attached form 1,3-dioxoisoindolin-2-yl. "Alkyl" denotes a linear saturated monovalent hydrocarbon radical of one to six carbon atoms or a branched saturated monovalent hydrocarbon radical of three to six carbon atoms; "alkylene" denotes a linear saturated divalent hydrocarbon radical of one to six carbon atoms or a branched saturated divalent hydrocarbon radical of three to six carbon atoms; "heteroaryl" denotes a monovalent monocyclic or bicyclic aromatic radical of 5-10 ring atoms, where one or two ring atoms are heteroatoms selected from N and O, and the remaining ring atoms are carbon; "aryl" denotes a monocyclic or bicyclic aromatic hydrocarbon radical of 6-10 ring atoms; "cycloalkyl" denotes a cyclic saturated monovalent hydrocarbon radical of three to ten carbon atoms; "cycloalkylalkyl" denotes a radical -(alkylene)-R, where R is cycloalkyl as defined above. Invention also relates to a pharmaceutical composition containing said compound and a method of treating a disease which can be treated by inhibiting NF-kB activation.

EFFECT: compound can be useful for treating inflammatory diseases.

21 cl, 3 tbl, 68 ex

(I)