发明名称 SELECTIVELY SUBSTITUTED QUINOLINE COMPOUNDS
摘要 Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
申请公布号 US2016176841(A1) 申请公布日期 2016.06.23
申请号 US201414908164 申请日期 2014.10.14
申请人 EISAI R&D MANAGEMENT CO., LTD. 发明人 BOIVIN Roch;HANSEN Hans;ISHIZAKA Sally;MACKEY Matthew;SCHILLER Shawn;OGAWA Chikako;NARAYAN Sridhar;BERTINATO Peter;BERGER Gregory;ENDO Atsushi;YU Robert T.;HAWKINS Lynn
分类号 C07D401/02;C07D413/14;C07D471/04;C07D401/14;C07D417/14 主分类号 C07D401/02
代理机构 代理人
主权项 1. A compound of Formula (I): wherein R5 is H or methyl; R9 is —H, methyl, or hydroxyl; R10 is —H, methyl, hydroxyl, or NR11R12, and wherein R11 and R12 are independently selected, and wherein R11 is —H, methyl, or —CH2—C(O)CH2CH3; and R12 is —H, oxopyrrolidinyl, dioxidothiopyranyl, isopropylsulfonyl, tetrahydropyranyl, oxetanyl, tetrahydrofuranyl, hydroxyl, dimethylaminethanesulfonyl, aminethanesulfonyl, dimethylaminpropanesulfonyl,C1-C6 alkyl that is linear, branched, or cyclic, optionally substituted with methoxy, —F, ≡N, methyl oxetanyl, ethoxy, oxo-, methyl imidazolyl, methylthio piperazinyl optionally substituted with methyl or —CF3, acetamidyl optionally substituted with methyl or ethyl,oxazolyl optionally substituted with methyl,pyrazolyl optionally substituted with methyl, cyano, or hydroxyl,—C(O)R13, wherein R13 is C1 to C7 alkyl that is cyclic, branched, or linear, optionally substituted with NR13R14, wherein 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;a five membered cycloalkyl, saturated or unsaturated, in which 1 or 2 carbon atoms are replaced by nitrogen atoms, wherein the cycloamine or cyclodiamine is optionally substituted with hydroxyl or methyl.
地址 Bunkyo-ku, Tokyo JP