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Selectively substituted quinoline compounds
专利权人:
EISAI R & D MANAGEMENT CO.; LTD.
发明人:
HANS HANSEN,LYNN HAWKINS,SALLY ISHIZAKA,SHAWN SCHILLER,ERIC CARLSON,CHIKAKO OGAWA,MATTHEW MACKEY,HEATHER DAVIS
申请号:
ARP140103811
公开号:
AR098014A1
申请日:
2014.10.14
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
Quinine compounds, as antagonists or inhibitors of receptors such as methanol 7 and / or 8, are selectively substituted and used in the synthesis of effective drugs for the treatment of systemic lupus erythematosus (SLE) and lupus nephritis, in which methanol is a protein of innate immune system. 1. Requirement 1: a compound (1) with formula characteristics,where at least one of R¹ and R² is -H, methyl, or ethyl, and the other is -H; or the other is C₁₋₆ alkyl which is optionally substituted with: -OH, methoxy, ethoxy, -OCH (CH () ₂,-O (CH) CHPhenyl, furan-o (ch832222); phenyl, methyltetraethyl-f-n (ch832323) c833222;Cyanogen, pyridinedioxy, fluoronoxyl, isochrome, phenol, benzene, benzeneOxo...a. Amino acid, carbamate, 7-member helix, 3-6-member cyclopentadiene, saturated or unsaturated, or unsaturated or unsaturated, optionally including one or more heteroatoms selected from O and N, optionally replacing one or more C or N atoms with methyl, cyanogen, fluorine, methylamine or trifluoride, or c83318327cyclo; Saturated or unsaturated, or unsaturated, optionally including one or more heteroatoms selected from O, s, and N, optionally replacing one or more C or N atoms with methyl, ethyl, pyridine, azidine, acrylamide, aminomethylamine, carbamate, or trifluoromethyl; or R1 and R2,Together with the nitrogen atoms connected to them, they form 8 to 11 members of spirulina, an 8-member bike, a 7-member spirulina, an optional glycol substitute, or a 4 to 6-member cyclopentanediol substitute, but at least one anthrax substitute can be used, 1. Carbamate, methyl (ethylamine) methyl (dimethylamine) methyl, dimethylamine (methylamine) methyl and amino, wherein R3 cubic meter is - H or methyl; 6. Claim 6: a compound classified as formula (2), wherein r8308es-h or methyl; r8330925 is saturated, partially saturated or unsaturated tar;Optionally, change to: - H, - Cl, - F, - Oh, - nh832222,Oxo...-N (CH CH)Phenyl, cyclohexadiene, methyl phenyl tricarboxylate, cyclohexadiene acryloni
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