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    • 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
    • 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
    • US4425350A
    • 1984-01-10
    • US251000
    • 1981-04-03
    • Johannes HartensteinEdgar Fritschi
    • Johannes HartensteinEdgar Fritschi
    • A61K31/47A61K31/473A61P25/00A61P25/18A61P25/24A61P25/26C07D221/18C07D491/06C07D217/04C07D217/06
    • C07D491/06C07D221/18
    • 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.
    • 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。