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    • 10. 发明授权
    • Therapeutic 1,4-thiazepines
    • 治疗性1,4-硫氮杂
    • US5580866A
    • 1996-12-03
    • US424464
    • 1995-05-03
    • John R. HousleyJames E. JefferyKenneth J. NicholBruce J. Sargent
    • John R. HousleyJames E. JefferyKenneth J. NicholBruce J. Sargent
    • A61K31/55A61K31/554A61P25/08C07D281/10
    • C07D281/10
    • Compounds of formula I ##STR1## in which n=0, 1 or 2;R.sub.1, R.sub.2, R.sub.6 and R.sub.7 independently represent H or alkyl (optionally substituted by one or more halo);R.sub.3 and R.sub.4 independently represent H or alkyl or together represent a group of formula .dbd.NR.sub.12 where R.sub.12 represents H, hydroxy, alkyl, phenyl or alkoxy; each alkyl, phenyl and alkoxy being optionally substituted with one or more halo;R.sub.5 represents: (a) H, (b) alkyl, (c) a group of formula --COR.sub.13 in which R.sub.13 is H, alkyl or phenyl, when R.sub.3 and R.sub.4 represent H or alkyl (optionally substituted with one or more halo), or (d) a group of formula --S(O).sub.p R.sub.14 in which p=1 or 2 and R.sub.14 is alkyl or phenyl, when R.sub.3 and R.sub.4 represent H or alkyl (optionally substituted with one or more halo); each alkyl and phenyl optionally substituted with one or more halo;and R.sub.8 to R.sub.11 independently represent H, halo, cyano, nitro, alkyl alkoxy, alkanoyl, carboxy, alkanoyloxy, carbamoyl (optionally substituted with alkyl or sulphamoyl (optionally substituted with alkyl of 1 to 4 carbon atoms); each alkyl, alkoxy, alkanoyl or alkanoyloxy optionally substituted with one or more halo;have utility in the treatment of seizures and/or neurological disorders such as epilepsy and/or as neuroprotective agents to protect against conditions such as stroke.
    • PCT No.PCT / EP93 / 03123 Sec。 371日期:1995年5月3日 102(e)日期1995年5月3日PCT提交1993年11月6日PCT公布。 第WO94 / 11360号公报 日期:1994年5月26日公式I I的化合物,其中n = 0,1或2; R1,R2,R6和R7独立地表示H或烷基(任选被一个或多个卤素取代); R3和R4独立地表示H或烷基或一起代表式= NR12的基团,其中R12表示H,羟基,烷基,苯基或烷氧基; 每个烷基,苯基和烷氧基任选被一个或多个卤素取代; R 5表示:(a)H,(b)烷基,(c)R 3为H,烷基或苯基的式-COR 13基团,当R 3和R 4表示H或烷基(任选被一个或多个卤素取代时) 或(d)当R 3和R 4表示H或烷基(任选被一个或多个卤素取代)时,其中p = 1或2且R 14为烷基或苯基的式-S(O)pR 14基团; 每个烷基和任选被一个或多个卤素取代的苯基; 并且R 8至R 11独立地表示H,卤素,氰基,硝基,烷基烷氧基,烷酰基,羧基,烷酰氧基,氨基甲酰基(任选被烷基或氨磺酰基(任选被1至4个碳原子的烷基取代)取代;各烷基,烷氧基,烷酰基 或任选被一个或多个卤素取代的烷酰氧基;可用于治疗癫痫发作和/或神经障碍,例如癫痫和/或作为神经保护剂以防止诸如中风的病症。