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    N-substituted isoquinoline derivatives and pharmaceutical compositions containing them
    2.
    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。

    2,3-Polymethylene-4-oxo-4H-pyrido[1,2-a]pyrimidines
    7.
    发明授权
    2,3-Polymethylene-4-oxo-4H-pyrido[1,2-a]pyrimidines 失效
    2,3-二亚甲基-4-氧代-4H-吡啶并[1,2-a]嘧啶

    公开(公告)号：US4220771A

    公开(公告)日：1980-09-02

    申请号：US935071

    申请日：1978-08-18

    申请人： Istvan Hermecz ,  Ferenc Fulop ,  Zoltan Meszaros ,  Gabor Bernath ,  Jozsef Knoll

    发明人： Istvan Hermecz ,  Ferenc Fulop ,  Zoltan Meszaros ,  Gabor Bernath ,  Jozsef Knoll

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61K31/55 ,  A61P7/02 ,  A61P9/10 ,  A61P11/00 ,  A61P25/04 ,  A61P29/00 ,  A61P31/04 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Pharmaceutical intermediates, morphine potentiators and other compounds have the formula ##STR1## wherein R is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy, nitro, amino, carboxy or a carboxylic acid derivate radical, R.sup.1 is hydrogen or a C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 is hydrogen, R.sup.4 is hydrogen or C.sub.1-4 alkyl, R.sup.5 is hydrogen R.sup.6 is hydrogen or R.sup.3 and R.sup.4 and/or R.sup.5 and R.sup.6 form a chemical bond, X is oxygen or imino, m is 1, 2, 3 or 4, n is 0, 1, 2 or 3, and if n is 1, then the dotted lines can stand for bonds, with the proviso that if m=1 and n=1 and if in the 2,3-, 6,7-, 8,9- and 1,10-positions double bonds are present, and R.sup.1 and R.sup.2 are hydrogen, then R is other than 9-hydroxy or 9-methyl; if m=2 and n=1 and R.sup.2 is hydrogen, then at least one of R and R.sup.1 is other than hydrogen; and if m=2 and n=2 and R.sup.2 is hydrogen and the molecule is a 2,3,4,6,7,8,9,10-octahydro derivative, then at least one of R and R.sup.1 is other than hydrogen or an acid-addition or quaternary salt thereof.

    摘要翻译： 药物中间体，吗啡增效剂和其它化合物具有式“IMAGE”，其中R是氢，卤素，C 1-4烷基，羟基，硝基，氨基，羧基或羧酸衍生物基团，R 1是氢或C 1-4烷基， R2是氢或C1-4烷基，R3是氢，R4是氢或C1-4烷基，R5是氢R6是氢或R3和R4和/或R5和R6形成化学键，X是氧或亚氨基，m 是1,2,3或4，n是0,1,2或3，如果n是1，则虚线可以代表键，条件是如果m = 1且n = 1，如果在 存在2,3,6,7,8,9和1,10-位双键，R1和R2是氢，则R不是9-羟基或9-甲基; 如果m = 2且n = 1且R2是氢，则R和R1中的至少一个不是氢; 并且如果m = 2且n = 2且R 2是氢并且该分子是2,3,4,6,7,8,9,10-八氢衍生物，则R和R 1中的至少一个不是氢或 其加酸或季盐。