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6 条记录 (耗时 0.023 秒)

    Dibenz[b,e]oxepin derivatives and pharmaceutical composition containing the same
    2.
    发明授权
    Dibenz[b,e]oxepin derivatives and pharmaceutical composition containing the same 失效
    二苯并[b，e] oxepin衍生物和含有它们的药物组合物

    公开(公告)号：US4889858A

    公开(公告)日：1989-12-26

    申请号：US180104

    申请日：1988-02-17

    申请人： Hitoshi Uno ,  Mikio Kurokawa ,  Fuminori Sato ,  Shunsuke Naruto ,  Yoshinobu Masuda

    发明人： Hitoshi Uno ,  Mikio Kurokawa ,  Fuminori Sato ,  Shunsuke Naruto ,  Yoshinobu Masuda

    IPC分类号： C07D313/12 ,  C07D401/12 ,  C07D409/12

    CPC分类号： C07D401/12 ,  C07D313/12 ,  C07D409/12

    摘要： The present invention relates to compounds represented by the general formula (I): ##STR1## wherein R.sub.1 is H or methoxy, R.sub.2 is H, methoxy, OH or F, R.sub.3 is H or F, R.sub.4 is H or F at 7-, 8- or 9-position, and .circle.Ar is a benzene, thiophene or pyridine ring, provided that (i) at least two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, (ii) R.sub.2 or R.sub.3 is F when R.sub.4 is F, (iii) R.sub.1, R.sub.3 and R.sub.4 are H when R.sub.2 is methoxy or OH, (iv) R.sub.2 and R.sub.3 are not simultaneously F, and (v) R.sub.2 and R.sub.3 are H or F, and both R.sub.1 and R.sub.4 are H when .circle.Ar is a thiophene or pyridine ring, or a physiologically acceptable acid addition salt thereof. The compounds of the present invention have an excellent protective effect against cerebral anoxia and some of them have also an inhibitory effect on lipid peroxidation of mitochondrial membrane of brain and an anti-convulsant activity and are useful as an agent for prevention or treatment of cerebral diseases caused by hypoxia in mammals including human.

    Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
    3.
    发明授权
    Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same 失效
    甲磺酰胺衍生物，其制备方法和包含其的组合物

    公开(公告)号：US4172896A

    公开(公告)日：1979-10-30

    申请号：US912857

    申请日：1978-06-05

    申请人： Hitoshi Uno ,  Mikio Kurokawa ,  Yoshinobu Masuda

    发明人： Hitoshi Uno ,  Mikio Kurokawa ,  Yoshinobu Masuda

    IPC分类号： C07D261/20 ,  C07D263/56 ,  A61K31/42

    CPC分类号： C07D263/56 ,  C07D261/20

    摘要： Methane-sulfonamide derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group: --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y,and an alkali metal salt thereof, and a process for the preparation of said methane-sulfonamide derivatives. Said compounds have an excellent anticonvulsant activity and are useful as anticonvulsants for controlling convulsions and seizures in patients with epilepsy.

    摘要翻译： 下式的甲磺酰胺衍生物：其中R 1是氢或卤素原子，R 2和R 3相同或不同，各自为氢或具有1至3个碳原子的直链或支链烷基， 的X和Y是碳原子，另一个是氮原子，条件是：-CH 2 SO 2 NR 2 R 3基团与X和Y中的任一个的碳原子键合，及其碱金属盐，以及制备所述 甲磺酰胺衍生物。 所述化合物具有优异的抗惊厥活性，可用作控制癫痫患者惊厥和癫痫发作的抗惊厥药。

    Acetic acid derivatives and composition containing the same
    4.
    发明授权
    Acetic acid derivatives and composition containing the same 失效
    乙酸衍生物及含有其的组合物

    公开(公告)号：US4356186A

    公开(公告)日：1982-10-26

    申请号：US246114

    申请日：1981-03-20

    申请人： Hitoshi Uno ,  Mikio Kurokawa ,  Hideo Nakamura

    发明人： Hitoshi Uno ,  Mikio Kurokawa ,  Hideo Nakamura

    IPC分类号： A61K31/34 ,  A61K31/38 ,  A61P29/00 ,  C07D313/12 ,  C07D337/12 ,  C07D337/14 ,  C07D405/06 ,  C07D409/06 ,  A61K31/335

    CPC分类号： C07C323/00 ,  C07D313/12 ,  C07D337/12 ,  Y10S514/825 ,  Y10S514/916

    摘要： Novel acetic acid derivatives of the formula: ##STR1## wherein X is oxygen or sulfur; R.sub.1 is hydrogen or a lower alkyl; R.sub.2 is hydroxy, an alkoxy, an alkenyloxy, a cycloalkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-disubstituted amino-lower alkoxy, a lower alkoxycrbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group ##STR2## wherein R.sub.3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R.sub.4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R.sub.3 and R.sub.4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group --CH(R.sub.1)COR.sub.2 is joined to the carbon atom at 2- or 3-position, and pharmaceutically acceptable salts thereof, processes for their preparation, and pharmaceutical compositions containing these compounds. They have excellent anti-inflammatory, analgesic and antipyretic activities with weak ulcerogenicity in the gastrointestinal tract and toxicity.

    摘要翻译： 下式的新型乙酸衍生物：其中X是氧或硫; R1是氢或低级烷基; R2是羟基，烷氧基，烯氧基，环烷氧基，芳氧基，取代的芳氧基，芳基 - 低级烷氧基，取代的芳基 - 低级烷氧基，芳基 - 低级烯氧基，取代的芳基 - 低级烯氧基，ω-二取代 氨基 - 低级烷氧基，低级烷氧基羰基 - 低级烷氧基，低级烷氧基 - 低级烷氧基，羟基 - 低级烷氧基 - 低级烷氧基，酰基 - 低级烷氧基或基团，其中R3是氢，羟基，低级烷基 ，芳基 - 低级烷基，羟基 - 低级烷基或羧基 - 低级烷基，R 4是氢，低级烷基或羟基 - 低级烷基，或者R 3和R 4可以与它们所在的氮原子结合在一起 连接形成杂环基; 并且基团-CH（R 1）COR 2与2-或3-位的碳原子及其药学上可接受的盐连接，其制备方法和含有这些化合物的药物组合物。 它们具有优良的抗炎，止痛和解热活性，肠胃道溃疡性弱，毒性低。