1-cyclohexyl-3,4-dihydroisoquinoline derivatives and pharmaceutical
compositions containing them
    1.
    发明授权
    1-cyclohexyl-3,4-dihydroisoquinoline derivatives and pharmaceutical compositions containing them 失效
    1-环己基-3,4-二氢异喹啉衍生物和含有它们的药物组合物

    公开(公告)号:US4622329A

    公开(公告)日:1986-11-11

    申请号:US721880

    申请日:1985-04-10

    CPC分类号: C07D217/14

    摘要: The invention relates to new 1-cyclohexyl-3,4-dihydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen, hydroxyl or alkoxy having from 1 to 6 carbon atoms,X is oxygen andZ is a .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is hydrogen or alkyl having from 1 to 6 carbon atoms; orX represents an .dbd.NR.sup.4 group, in which R.sup.4 is hydrogen or hydroxyl, andZ is a .dbd.CH--CN, .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is as defined above,and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular show antispasm, analgesic, gastric acid secretion inhibiting, sedative and hypnotic activity and effectively reduce the alcoholic narcosis time. According to a further aspect of the invention there is provided a process for the preparation of these compounds. The invention further relates to pharmaceutical compositions containing them as active ingredient.

    摘要翻译: 本发明涉及式(I)的新的1-环己基-3,4-二氢异喹啉衍生物其中R 1和R 2各自独立地表示氢,羟基或具有1至6个碳原子的烷氧基,X是氧 Z为a = CH 2或= CH-COOR 3基团,其中R 3为氢或具有1至6个碳原子的烷基; 或X表示= NR4基团,其中R4为氢或羟基,Z为a = CH-CN,= CH2或= CH-COOR3基团,其中R3如上定义,及其酸加成盐。 式(I)的化合物是药学活性的,特别是表现出痉挛,镇痛,胃酸分泌抑制,镇静和催眠活性,并有效降低酒精性麻醉时间。 根据本发明的另一方面,提供了制备这些化合物的方法。 本发明还涉及含有它们作为活性成分的药物组合物。

    [1,3]oxazino[4,3-a]-isoquinoline derivatives and pharmaceutical
compositions containing them
    4.
    发明授权
    [1,3]oxazino[4,3-a]-isoquinoline derivatives and pharmaceutical compositions containing them 失效
    [1,3]恶嗪并[4,3-a] - 异喹啉衍生物和含有它们的药物组合物

    公开(公告)号:US4623647A

    公开(公告)日:1986-11-18

    申请号:US664844

    申请日:1984-10-25

    CPC分类号: C07D498/04 C07D498/10

    摘要: The invention relates to new [1,3]oxazino[4,3-a]-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,R.sup.3 is hydrogen, alkyl having from 1 to 8 carbon atoms, cycloakyl or cycloalkenyl having from 3 to 6 carbon atoms, optionally substituted phenyl, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or heteroaryl,R.sup.4 is hydrogen or alkyl having from 1 to 4 carbon atoms, orR.sup.3 and R.sup.4 together form a --(CH.sub.2).sub.n -- group, in which n is an integer from 3 to 7,R.sup.5 is hydroxyl, halogen or an ##STR2## group, in which R.sup.6 is optionally substituted phenyl,X is oxygen or sulfur,and salts thereof.According to another aspect of the invention there is provided a process for the preparation of these compounds. Compounds of formula (I) are pharmaceutically active. Pharmaceutical compositions containing them are also within the scope of the invention.

    摘要翻译: 本发明涉及式(I)的新的[1,3]恶嗪并[4,3-a] - 异喹啉衍生物其中R 1和R 2表示羟基或具有1至6个碳原子的烷氧基,R 3 是氢,具有1至8个碳原子的烷基,具有3至6个碳原子的环烷基或环烯基,任选取代的苯基,在烷基部分或杂芳基具有1至4个碳原子的芳烷基,R 4是氢或具有1 至4个碳原子,或者R 3和R 4一起形成 - (CH 2)n - 基团,其中n为3-7的整数,R 5为羟基,卤素或基团,其中R 6为任选取代的苯基 X是氧或硫,及其盐。 根据本发明的另一方面,提供了一种制备这些化合物的方法。 式(I)的化合物是药学活性的。 含有它们的药物组合物也在本发明的范围内。

    N-substituted isoquinoline derivatives and pharmaceutical compositions
containing them
    7.
    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。