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5-PIPERIDIN-8-CYANOCHINOLINE DERIVATIVES
专利权人:
EJSAJ Ar END Di MENEDZHMENT KO.; LTD.
发明人:
BUAVEN Rosh (US),БУАВЕН Рош (US),KHANSEN Khans (US),ХАНСЕН Ханс (US),ISIZAKA Salli (US),ИСИЗАКА Салли (US),MAKKI Mettyu (US),МАККИ Мэттью (US),SHILLER Shon (US),ШИЛЛЕР Шон (US),OGAVA Tikako (CH),ОГАВА
申请号:
RU2016118624
公开号:
RU0002671496C2
申请日:
2014.10.14
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
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 tblИзобретение относится к области органической химии, а именно к селективно замещенным соединениям хинолина формулы (I),
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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