SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS Russian patent published in 2016 - IPC C07D223/16 C07D401/04 C07D401/10 C07D401/14 C07D403/04 C07D403/10 C07D403/14 A61K31/55 A61P9/00 A61P29/00 A61P31/00 A61P35/00 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to formula compounds, where Y stands for 6-membered heteroaryl, containing 1-2 nitrogen atoms; R² is selected from OR¹⁴ and NR⁶R⁷; each of R⁶ and R⁷ is independently selected from H, C₁-C₁₂ alkyl, C₃-C₁₂ cycloalkyl, 6-membered heterocycle, containing 1 nitrogen atom, or benzyl, where said alkyl, cycloalkyl or benzyl are optionally substituted with one or more groups, independently selected from -F, -OR⁸, -NR¹²SO₂R¹³, -C(=O)NR¹²R¹³, or R⁶ and R⁷, together with nitrogen atom, which they are bound to, form 5-6-membered heterocylic ring, containing 1 nitrogen atom, and said 5-6-membered heterocyclic ring is optionally substituted with one or more -OH; R⁸ is selected from hydrogen and C₁-C₁₂ alkyl, and each of R¹², R¹³ and R¹⁴ is independently selected from H and C₁-C₁₂ alkyl, where said alkyl is optionally substituted with -OH; or their tautomers, enantiomers or pharmaceutically acceptable salts. The invention also relates to particular derivatives of benzo[b]azepine, given on i. 3, to set for treating TLR7- and/or TLR8-mediated condition, pharmaceutical composition and methods for treating TLR7- and/or TLR8-mediated conditions.

EFFECT: derivatives, possessing agonistic activity with respect to TLR7 or TLR8 receptor.

14 cl, 3 tbl, 222 ex