5-PIPERIDIN-8-CYANOCHINOLINE DERIVATIVES Russian patent published in 2018 - IPC C07D401/04 C07D401/02 C07D401/14 C07D413/14 C07D417/14 C07D471/04 A61K31/422 A61K31/427 A61K31/4545 A61K31/4709 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to selectively substituted quinoline compounds of formula (I), wherein R₈ is-H or methyl; R₉ is-H, methyl or hydroxyl; R₁₀ is methyl, hydroxyl or NR₁₁R₁₂; and where R₁₁ and R₁₂ independently selected, and where R₁₁ is-H, methyl or -CH₂-C(O)CH₂CH₃; and R₁₂ is-H, oxopyrrolidinyl, dioxydothiopyranyl, isopropylsulfonyl, tetrahydropyranyl, oxetanyl, tetrahydrofuranyl, dimethylaminethanesulfonyl, aminoethanesulfonyl, dimethylaminopropanesulfonyl, C₁-C₆-alkyl, which is linear, branched or cyclic, optionally substituted with methoxy, -F, ≡N, methyl oxetanyl, oxo, methyl imidazolyl, oxazolyl, optionally substituted methyl, pyrazolyl optionally substituted with methyl or cyano , C(O)R₁₃, where R₁₃ is C₁-C₇-alkyl which is cyclic, branched or linear, optionally substituted with NR₁₃R₁₄, where R₁₃ and R₁₄ are independently selected from methyl and -H; methoxy, hydroxyl, methylthio, ethylthio, methylsulfonyl, oxo, thiazolidinyl, pyridinyl, pyrazolopyridinyl, methyl amino, thiazolyl, -F, morpholinyl, methylisoxazolyl, methyl oxetanyl, aminooxetanyl, phenyl optionally substituted with hydroxyl, -C(O)NH₂; five-membered cycloalkyl, saturated or unsaturated, in which 1 or 2 carbon atoms are replaced by nitrogen atoms, wherein cycloamine or cyclodiamine is optionally substituted with hydroxyl or methyl; or a pharmaceutically acceptable salt thereof. Invention also relates to particular compounds, a method of treating said diseases, methods for antagonizing TLR7 and TLR8, a pharmaceutical composition and pharmaceutically acceptable salts based on a compounds of formula (I).

EFFECT: compounds that act as an antagonist or inhibitor for Toll-like receptors (TLRs) 7 and 8 are obtained and are effective for treatment of systemic lupus erythematosus and lupus nephritis.

11 cl, 37 dwg, 5 tbl