| abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to the field of organic chemistry, namely to selectively substituted quinoline compounds of formula (I), wherein R 8 is-H or methyl; R 9 is-H, methyl or hydroxyl; R 10 is methyl, hydroxyl or NR 11 R 12 ; and where R 11 and R 12 independently selected, and where R 11 is-H, methyl or -CH 2 -C(O)CH 2 CH 3 ; and R 12 is-H, oxopyrrolidinyl, dioxydothiopyranyl, isopropylsulfonyl, tetrahydropyranyl, oxetanyl, tetrahydrofuranyl, dimethylaminethanesulfonyl, aminoethanesulfonyl, dimethylaminopropanesulfonyl, C 1 -C 6 -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)R 13 , where R 13 is C 1 -C 7 -alkyl which is cyclic, branched or linear, optionally substituted with NR 13 R 14 , where R 13 and R 14 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)NH 2 ; 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). n n n n 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. n 11 cl, 37 dwg, 5 tbl |