5,6,6a,7-Tetrahydro-4H-dibenz(de,g)-isoquinoline derivatives, and their
use for treating central nervous system disorders
    23.
    发明授权
    5,6,6a,7-Tetrahydro-4H-dibenz(de,g)-isoquinoline derivatives, and their use for treating central nervous system disorders 失效
    5,6,6a,7-四氢-4H-二苯并(de,g) - 异喹啉衍生物及其用于治疗中枢神经系统疾病的用途

    公开(公告)号:US4425350A

    公开(公告)日:1984-01-10

    申请号:US251000

    申请日:1981-04-03

    CPC分类号: C07D491/06 C07D221/18

    摘要: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and are hydroxy, straight or branched-chain alkoxy of from 1 to 5 carbon atoms, phenoxy, benzyloxy, two adjacent groups may be methylenedioxy, or hydrogen provided R.sub.4 and R.sub.5 are not simultaneously hydrogen; R.sub.6 is hydrogen, straight or branched-chain alkyl of from 1 to 5 carbon atoms, straight or branched-chain alkenyl of from 2 to 5 carbon atoms, cycloalkylalkyl of from 4 to 7 carbon atoms, alkoxy carbonyl of from 2 to 6 carbon atoms, trifluoroacetyl, aralkyl of from 5 to 11 carbon atoms, or acyl which is derived from an aliphatic, araliphatic or aromatic carboxylic acid of from 1 to 11 carbon atoms; and the pharmaceutically acceptable salts thereof; excluding 5,6,6a,7-tetrahydro-1-hydroxy-2,9,10trimethoxy-5-methyl-4H-dibenz(de,g)-isoquinoline and 5,6,6a,7-tetrahydro-1,2,9,10-tetramethoxy-5-methyl-4H-dibenz(de,g)isoquinoline.The present invention also provides a process for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for treating diseases of the central nervous system.

    摘要翻译: 本发明提供以下通式的化合物:其中R 1,R 2,R 3,R 4和R 5可以相同或不同,为1至5个碳原子的羟基,直链或支链烷氧基,苯氧基,苄氧基 ,两个相邻的基团可以是亚甲二氧基,或者提供的氢,R4和R5不同时为氢; R 6是氢,具有1至5个碳原子的直链或支链烷基,2至5个碳原子的直链或支链烯基,4至7个碳原子的环烷基烷基,2至6个碳原子的烷氧基羰基 具有5至11个碳原子的三氟乙酰基,芳烷基或衍生自具有1至11个碳原子的脂族,芳脂族或芳族羧酸的酰基; 及其药学上可接受的盐; 不包括5,6,6a,7-四氢-1-羟基-2,9,10-三甲氧基-5-甲基-4H-二苯并(de,g) - 异喹啉和5,6,6a,7-四氢-1,2, 9,10-四甲氧基-5-甲基-4H-二苯并(de,g)异喹啉。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。 此外,本发明涉及这些化合物用于治疗中枢神经系统疾病的用途。

    Process for the preparation of 1-hydroxyaporphine-derivatives
    25.
    发明授权
    Process for the preparation of 1-hydroxyaporphine-derivatives 失效
    1-羟基萘酚衍生物的制备方法

    公开(公告)号:US4202980A

    公开(公告)日:1980-05-13

    申请号:US971142

    申请日:1978-12-19

    CPC分类号: C07D491/06 C07D221/18

    摘要: A process for the preparation of 1-hydroxyaporphine derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.3 and R.sub.4, which are the same or different, are lower alkyl, aryl or aralkyl radicals or R.sub.3 and R.sub.4 can together form a lower alkylene bridge member and R.sub.2 is a hydrogen atom or a lower alkyl, aralkyl or alkoxycarbonyl radical or an acyl radical derived from an aliphatic, aromatic or araliphatic carboxylic acid.

    摘要翻译: 制备以下通式的1-羟基萘酚衍生物的方法:其中R1,R3和R4相同或不同,为低级烷基,芳基或芳烷基或R3和R4可以一起形成低级 亚烷基桥构件和R 2是氢原子或低级烷基,芳烷基或烷氧基羰基或衍生自脂族,芳族或芳脂族羧酸的酰基。