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72 条记录 (耗时 0.034 秒)

    5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them
    7.
    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。

    Tripeptides acting on the central nervous system and a process for the preparation thereof
    8.
    发明授权
    Tripeptides acting on the central nervous system and a process for the preparation thereof 失效
    作用于中枢神经系统的三肽及其制备方法

    公开(公告)号：US4299821A

    公开(公告)日：1981-11-10

    申请号：US163829

    申请日：1980-06-27

    申请人： Lajos Kisfaludy ,  Tamas Szirtes ,  Lajos Balaspiri ,  Eva Palosi ,  Laszlo Szporny ,  Adam Sarkadi

    发明人： Lajos Kisfaludy ,  Tamas Szirtes ,  Lajos Balaspiri ,  Eva Palosi ,  Laszlo Szporny ,  Adam Sarkadi

    IPC分类号： C07K5/08 ,  A61K38/04 ,  A61K38/06 ,  A61P25/00 ,  C07K1/113 ,  C07K5/062 ,  C07K5/097 ,  C07K14/575 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/06034 ,  C07K5/06043 ,  C07K5/06104 ,  C07K5/0825

    摘要： The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),Glp--X--Y--NH--A (I)whereinX is L-norleucyl, L-leucyl, L-norvalyl, D-leucyl, L-prolyl, L-2-aminobutyryl, L-valyl, L-threonyl, L-isoleucyl, L-2-aminodecanoyl, L-cyclohexylalanyl or L-tert.-butyl-seryl group andY is L-prolyl group, orX is L-histidyl group andY is L-homoprolyl or D-pipecolyl group, furthermoreA is hydrogen, a C.sub.1-10 alkyl group or a C.sub.1-3 alkyl group having a dimethylamino substituent,with the proviso that if X is L-leucyl group, A is other than hydrogen, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.

    摘要翻译： 本发明涉及作用于中枢神经系统且对应于通式（I）的Glp-XY-NH-A（I）的新型肽衍生物，其中X为L-正亮氨酰基，L-亮氨酰，L-缬氨酰基，D -L-脯氨酰基，L-苏氨酸，L-异亮氨酰基，L-2-氨基十一烷酰基，L-环己基丙氨酰基或L-叔丁基 - 丝氨酰基，Y是L-脯氨酰基，L-脯氨酰基，L-2-氨基丁酰基， 基团，或X为L-组氨酰基，Y为L-顺式或D-哌啶基，此外A为氢，C1-10烷基或具有二甲基氨基取代基的C1-3烷基，条件是如果X 是L-亮氨酰基，A不是氢，和其药学上可接受的复合物。 这些化合物通过肽化学中常用的方法制备。