5,6,6a,7-Tetrahydro-4H-dibenz(de,g)-isoquinoline derivatives, and their
use for treating central nervous system disorders
    22.
    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。

    Antispasmodic substituted sulphoximides
    25.
    发明授权
    Antispasmodic substituted sulphoximides 失效
    解痉取代的磺酰亚胺

    公开(公告)号:US4105795A

    公开(公告)日:1978-08-08

    申请号:US719970

    申请日:1976-09-02

    摘要: This invention provides compounds of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 independently represent groups selected from the group consisting of straight chain alkyl groups; branched chain alkyl groups; aryl groups; optionally substituted aryl groups and the groups required to complete a ring system together with the sulphur atom;R.sup.3 and R.sup.4 independently represent groups selected from the group consisting of hydrogen; straight chain alkyl groups; branched chain alkyl groups and optionally substituted aryl groups;R.sup.5 and R.sup.6 independently represent groups selected from the group consisting of alkyl groups and the groups required to complete a heterocyclic ring together with the nitrogen atom; the groupR.sup.7 represents a group selected from the group consisting of hydrogen; straight chain alkyl groups and branched chain alkyl groups;X represents an anion of a physiologically acceptable acid andn represents a number selected from the group consisting of 0 and 1.The compounds show pharmacological activity, for example, as spasmolytics and broncholytics.

    摘要翻译: 本发明提供通式I(I)的化合物,其中R 1和R 2独立地表示选自直链烷基的基团; 支链烷基; 芳基; 任选取代的芳基和与硫原子一起完成环系所需的基团; R3和R4独立地表示选自氢, 直链烷基; 支链烷基和任选取代的芳基; R5和R6独立地表示选自烷基和与氮原子一起完成杂环所需的基团的基团; 基团R7表示选自氢的基团; 直链烷基和支链烷基; X表示生理上可接受的酸的阴离子,N表示从0和1组所选择的数字。