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    • 23. 发明授权
    • Nitrogen heterocycles
    • 氮杂环
    • US5681839A
    • 1997-10-28
    • US448453
    • 1995-12-07
    • Roger CrossleyAlbert OpalkoBarry John Langham
    • Roger CrossleyAlbert OpalkoBarry John Langham
    • C07C217/74C07C229/46C07D215/22C07D215/227C07D215/56A61K31/47
    • C07D215/227C07C217/74C07C229/46C07D215/56C07C2101/14
    • This invention concerns a compound of generic formula ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds, R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl C.sub.6 -C.sub.10 aryl, heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl; R' represents one or more optional substituents the same or different, selected from 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, C.sub.6 -C.sub.10 or heteroaryl or an (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; R" represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions selected from 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 hydroxyalkyl, and R" can also represent hydroxy in the 6 position when the optional bond is absent; oxo and methylene; which compounds have pharmaceutical uses conferred by their ability to block voltage gated potassium channels.
    • PCT No.PCT / GB95 / 00278 Sec。 371 1995年12月7日第 102(e)1995年12月7日,PCT提交1995年2月10日PCT公布。 公开号WO95 / 21824 日期1995年8月17日本发明涉及通式(1)的化合物或其药学上可接受的盐,其中虚线表示任选的键,R 3是任选取代的C 6 -C 10芳基或杂芳基; R4代表氢或式-CRaRbRc基团,其中Ra,Rb和Rc独立地选自氢,C1-C6烷基C6-C10芳基,杂芳基,被任意取代的C6-C10芳基或杂芳基取代的C1-C6烷基; R'表示选自卤素,C 1 -C 6烷基,C 2 -C 7烷氧基羰基,C 1 -C 6羟基烷基,CN,氨基羰基,C 2 -C 7烷酰氧基(C 1 -C 6)烷基,羧基,C 2 -C 7烷氧基氨基,C 6 -C 10或杂芳基或(C 6 -C 10芳基)烷基或杂芳基烷基; R“表示选自C 1 -C 6烷基,C 2 -C 7烷酰氧基,羟基,氨基,C 2 -C 7烷酰基氨基,C 1 -C 6烷基氨基,C 1 -C 6烷基氨基, C6羟基烷基,当不含任选的键时,R“也可以表示6位的羟基; 氧代和亚甲基; 哪些化合物具有通过其阻断电压门控钾通道的能力而赋予的药物用途。