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6-aryl-(methyl - or methylidone)-quinoline derivatives as voltage- gated potassium channel blockers

机译:6-芳基-(甲基或亚甲基酮)-喹啉衍生物作为电压门控钾通道阻滞剂

摘要

This invention concerns a compound of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,PPR.sup.3 is an optionally substituted C. sub.6 -C.sub.10 aryl or heteroaryl group; optionally substituted by one or more substituents the same or different,P PR' represents one or more optional substituents the same or different, selected from the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub. 2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6 )alkyl, carboxy, C.sub.2 -C.sub. 7 alkanoxylamino, optionally substituted C.sub.6 -C.sub.10 or heteroaryl or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; andPPR" represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions the same or different: monovalent substituents being selected from the following: C. sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkanoyloxy, hydroxy, amino, C. sub.2 -C.sub.7 alkanoylamino, C.sub.1 -C. sub.6 alkylamino, C.sub.1 -C. sub.6 hydroxalkyl, C.sub.7 -C.sub.17 aralkyloxyamino, R" can also represent hydroxy in the 6 position (when the optional bond is absent); the di-valent substituents being selected from oxo (i.e ═O) and methylene (i.e ═CH.sub.2);P P and the N-oxides thereof, which compounds have pharmaceutical uses conferred by their ability to block voltage gated potassium channels.
机译:本发明涉及一种通式为:的化合物或其药学上可接受的盐,其中虚线代表任选的键,P 3 R是任选取代的C.sub.6- C.sub.10芳基或杂芳基;任选地被一个或多个相同或不同的取代基取代,P> R'表示一个或多个相同或不同的可选取代基,其选自:卤素,C 1 -C 6烷基,C 2 -C 7烷氧羰基,C 1 -C 6羟烷基,CN,氨基羰基, 2 -C 7烷酰氧基(C 1 -C 6)烷基,羧基,C 2 -C 6。 7个烷氧基氨基,任选取代的C 6 -C 10或杂芳基或任选取代的(C 6 -C 10芳基)烷基或杂芳基烷基; “ P”和“ P”表示在5、7或8个相同或不同的位置上的一个或多个可选的单价或二价取代基:单价取代基选自:C.sub.1-C。 sub.6烷基,C.sub.2 -C.sub.7烷酰氧基,羟基,氨基,C.sub.2-C.sub.7烷酰基氨基,C.sub.C.sub.6烷基氨基,C。 sub.1-C.sub.6羟基烷基,C.sub.7-C.sub.17芳烷基氧基氨基,R“也可以在6位代表羟基(当不存在任选键时);化合物,其二价取代基选自氧代(即═ O)和亚甲基(即═ CH.sub.2);

及其N-氧化物,这些化合物因其能力而具有药物用途阻断电压门控钾通道。

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