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    • 3. 发明授权
    • Naphthalene derivatives
    • 萘衍生物
    • US07732622B2
    • 2010-06-08
    • US12111989
    • 2008-04-30
    • Miles Stuart CongreveGerard Martin Paul GiblinAndrew McMurtrie MasonNeil Derek MillerSusan RoomansAnn Louise Walker
    • Miles Stuart CongreveGerard Martin Paul GiblinAndrew McMurtrie MasonNeil Derek MillerSusan RoomansAnn Louise Walker
    • C07D209/60A61K31/40
    • C07D209/66C07D209/64
    • A compound of formula (I) wherein R1 and R3 are the same or different and represent ═O, hydrogen, C1-6alkyl, C1-6dialkyl, ═CHC1-C5alkyl, ═S, or a 5- or 6-membered aryl; R4 to R9 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or CF3; Q1 is hydrogen, C1-6alkyl, C1-6dialkyl, C1-6alkoxy, NHAc, NR210 where R10 is hydrogen or C1-6alkyl, difluoro, fluoro, ═O, or OH; Q2, Q3, Q4 and Q5 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or a 5- or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmaceutically acceptable derivatives thereof.
    • 式(I)的化合物,其中R 1和R 3相同或不同并且表示≡O,氢,C 1-6烷基,C 1-6二烷基,= CHCl-C 5烷基,= S或5或6元芳基; R4至R9相同或不同,表示氢,C1-6烷氧基,OCF3,OCH2CF3,O-环丙基,OCH2-环丙基,C1-C6烷基,S-烷基,NR210,其中R10为氢或C1-6烷基,卤素, OH,CH 2 OC 1 -C 6烷基,CH 2 OH或CF 3; Q1是氢,C1-6烷基,C1-6二烷基,C1-6烷氧基,NHAc,NR210,其中R10是氢或C1-6烷基,二氟,氟,= O或OH; Q2,Q3,Q4和Q5相同或不同,表示氢,C1-6烷氧基,OCF3,OCH2CF3,O-环丙基,OCH2-环丙基,C1-C6烷基,S-烷基,NR210,其中R10是氢或C1-6烷基, 卤素,NO 2,OH,CH 2 OC 1 -C 6烷基,CH 2 OH或5或6元芳基; 条件是化合物[4-(1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基)苯基] -2-丙酸钠盐和[4-(4,9 - 二乙氧基-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基)苯基]乙酸; 和它们的药用衍生物。