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150 条记录 (耗时 0.028 秒)

    5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them
    14.
    发明授权
    5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them 失效
    5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-和含有它们的药物组合物

    公开(公告)号：US4329341A

    公开(公告)日：1982-05-11

    申请号：US178679

    申请日：1980-11-26

    申请人： Julianna Rochricht ,  Lajos Kisfaludy ,  Marton Kajtar ,  Eva Palosi ,  Laszlo Szporny

    发明人： Julianna Rochricht ,  Lajos Kisfaludy ,  Marton Kajtar ,  Eva Palosi ,  Laszlo Szporny

    IPC分类号： C07D243/24 ,  A61K31/55

    CPC分类号： C07D243/24

    摘要： The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen, halogen, trifluoromethyl or a nitro group;R.sup.2 stands for hydrogen or alkyl having 1 to 6 carbon atoms;R.sup.3 represents a group conventionally attached to the --CH(NH.sub.2)--COOH group of the known optically active or racemic .alpha.-amino-acids, preferably an optionally substituted lower alkyl group;R.sup.4 is hydrogen, chlorocarbonyl or carbamoyl; andX is hydrogen, halogen or trifluoromethyl, with the proviso that if in the racemic compounds R.sup.4 stands for hydrogen R.sup.3 is other than alkyl having 1 to 6 carbon atoms, in which the centers of asymmetry in the 3- and 5-positions have the same absolute configuration, and pharmaceutically acceptable acid addition salts thereof, and a process for their preparation. The new compounds show valuable enzyme inducing activity and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.

    摘要翻译： 本发明涉及通式（I）的新的光学活性或外消旋的5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-酮衍生物，其中R 1 代表氢，卤素，三氟甲基或硝基; R2代表氢或具有1至6个碳原子的烷基; R3表示通常与已知光学活性或外消旋的α-氨基酸的-CH（NH 2）-COOH基团连接的基团，优选任选取代的低级烷基; R4是氢，氯代羰基或氨基甲酰基; 并且X是氢，卤素或三氟甲基，条件是如果在外消旋化合物中R4代表氢，R3不是具有1至6个碳原子的烷基，其中3-和5-位的不对称中心具有 相同的绝对构型及其药学上可接受的酸加成盐及其制备方法。 新化合物显示有价值的酶诱导活性，因此可用作药物组合物的活性成分，其也在本发明的范围内。

    Substituted nitrobenzophenone derivatives and a process for the preparation thereof
    20.
    发明授权
    Substituted nitrobenzophenone derivatives and a process for the preparation thereof 失效
    取代的硝基二苯甲酮衍生物及其制备方法

    公开(公告)号：US4064121A

    公开(公告)日：1977-12-20

    申请号：US603855

    申请日：1975-08-12

    申请人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaboles Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

    发明人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaboles Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

    IPC分类号： C07D295/10 ,  C07D225/02 ,  C07D211/14

    CPC分类号： C07D295/10

    摘要： New compounds of the general formula (I), ##STR1## wherein R.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl, are prepared by reacting a compound of the general formula ##STR2## wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.

    摘要翻译： 通式（I）的新化合物，其中R 1和R 2各自表示饱和或不饱和的直链或支链烷基，芳烷基，饱和或不饱和环烷基或芳基 ，或R1和R2与相邻的氮原子一起可以形成任选地含有另外的氧或氮杂原子的任选取代的杂环基团，但是，R 1表示甲基，R 2可以仅代表甲基以外的基团，其通过使 通式（II）的化合物，其中X表示卤素，具有通式（III）的仲胺，R1-NH-R2（Ⅲ）其中R1和R2各自具有与上述相同的含义 。