公开(公告)号：EP0665226A4

公开(公告)日：1995-06-07

申请号：EP93923647

申请日：1993-10-27

申请人： TOYAMA CHEMICAL CO LTD

发明人： TAKEDA KENJI ,  TERASHIMA NOBUO ,  NAKANO JOJI ,  MINAMI HISASHI ,  KOBAYASHI TOYOKAZU ,  FURUHATA KUNIKAZU ,  TAKAKURA TADAKAZU ,  TAKATA MAKOTO ,  KAWAFUCHI HIROYO ,  HIRAIWA TORU

IPC分类号： C07D261/20 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535

CPC分类号： C07D413/04 ,  C07D261/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： A 1,2-benzisoxazole derivative represented by general formula (I) and a salt thereof, said compound (I) being excellent in the protection against cerebral hypoxia, having the macrobiotic effect on the animals suffering from cerebral ischemia and an antispasmodic effect, having reduced effect on the central nervous system, and having a high safety, thus being useful for treating not only the acute stage of cerebral circulation disorder but also the chronic stage thereof, sequelae of the trauma of the head and epilepsy. In formula (I), R represents hydrogen, halogen, nitro, cyano, hydroxy, optionally substituted lower alkyl, lower alkenyl, lower alkynyl, aralkyl, aryl, lower alkyloxy, cycloalkyl, aralkyloxy, aryloxy, amino, lower acyl, arylcarbonyl, lower alkanesulfonyl, arenesulfonyl, lower alkylthio, carbamoyl, heterocycle, lower alkylene or lower alkenylene; R1 and R2, which may be the same or different from each other, represent each hydrogen or optionally substituted lower alkyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl, aralkyl or heterocycle; R4 represents optionally substituted lower alkyl, aryl or heterocycle, or alternatively R3 and R4 may be combined together to represent lower alkylene; and R5 and R6, which may be the same or different from each other, represent each hydrogen, optionally substituted lower alkyl, lower alkenyl, lower alkynyl, lower acyl, lower alkyloxycarbonyl or aralkyl.