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    Substituted nitrobenzophenone derivatives and a process for the preparation thereof
    91.
    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 。

    N-substituted isoquinoline derivatives and pharmaceutical compositions containing them
    98.
    发明授权
    N-substituted isoquinoline derivatives and pharmaceutical compositions containing them 失效
    N-取代的异喹啉衍生物和含有它们的药物组合物

    公开(公告)号：US4668688A

    公开(公告)日：1987-05-26

    申请号：US664770

    申请日：1984-10-25

    申请人： Gabor Bernath ,  Jeno Kobor ,  Ferenc Fulop ,  Pal Perjesi ,  Elemer Ezer ,  Gyorgy Hajos ,  Eva Palosi ,  Laszlo Denes ,  Laszlo Szporny

    发明人： Gabor Bernath ,  Jeno Kobor ,  Ferenc Fulop ,  Pal Perjesi ,  Elemer Ezer ,  Gyorgy Hajos ,  Eva Palosi ,  Laszlo Denes ,  Laszlo Szporny

    IPC分类号： A61K31/47 ,  A61K31/472 ,  A61P1/04 ,  A61P25/04 ,  A61P29/00 ,  A61P37/06 ,  C07D217/16

    CPC分类号： C07D217/16

    摘要： The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof. Processes for the preparation of these compounds and pharmaceutical compositions are also within the scope of the invention.

    摘要翻译： 本发明涉及式（I）的新的N-取代双（羟甲基） - 甲基 - 异喹啉衍生物，其中R1和R2代表羟基或具有1-6个碳原子的烷氧基，虚线是 在1,2-位上的任选的双键，R3是具有1至6个碳原子的烷基或在烷基部分含有1至4个碳原子的芳烷基，或 - 如果1,2-二烷基中存在单键， 位置 - 表示如果R 4是具有1至5个碳原子的烷基，具有1至4个碳原子的烷氧基，羟基，苯基或取代的苯基，其中X是氧的式“IMAGE”的基团; 如果R 4是-NH 2，-NH-C 1-4 - 烷基，-NH-C 3-6 - 环烷基，-NH-苯基或-NH-C 1-4 - 烷基 - 苯基，则X是氧或硫; 并且R 5和R 6独立地代表氢，具有1至4个碳原子的烷基或苯基，条件是它们中的至少一个不是苯基，及其盐。 用于制备这些化合物和药物组合物的方法也在本发明的范围内。