N-substituted isoquinoline derivatives and pharmaceutical compositions
containing them
    9.
    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

    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。