Condensed quinolinium and isoquinolinium derivatives
    1.
    发明授权
    Condensed quinolinium and isoquinolinium derivatives 失效
    浓缩的喹啉和异喹啉衍生物

    公开(公告)号:US4994448A

    公开(公告)日:1991-02-19

    申请号:US251445

    申请日:1988-09-30

    CPC分类号: C07D471/04

    摘要: The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-4 alkyl or aralkyl; andR.sub.2 represents hydroxy; orR.sub.1 and R.sub.2 together form a valency bond;R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, amino, alkylthio or a group of the Formula --NR.sub.7 R.sub.8 in which R.sub.7 and R.sub.8 may be the same or different and stand for hydrogen, C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl or di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl or together with the nitrogen atom they are attached to form a 6-membered heterocyclic ring which may optionally contain a further nitrogen, oxygen or sulfur atom; orR.sub.2 and R.sub.3 together form an oxo (.dbd.O) or thixo (.dbd.S) group;R.sub.4 represents hydrogen, C.sub.1-4 alkyl or phenyl which may optionally bear one or two halogen or nitro substituent(s);Z is a group of the Formula (a) or (b) ##STR2## A.sup.- represents an anion) and isomers thereof possess useful local anaesthetic, antidepressant, tranquillo-sedative and smooth muscle relaxant properties accompanied by a weaker analgesic effect and are useful in therapy.

    摘要翻译: 通式I的新化合物Ⅰ(其中R1代表C1-4烷基或芳烷基,R2代表羟基;或R1和R2一起形成价键; R3是氢,C1-4烷基,C1- 烷氧基,苯基,氨基,烷硫基或式-NR7R8的基团,其中R 7和R 8可以相同或不同,代表氢,C 1-4烷基,苯基-C 1-4烷基,羟基-C 1-4烷基 或二 - (C 1-4烷基) - 氨基-C 1-4烷基或与它们连接的氮原子一起形成可任选地含有另外的氮,氧或硫原子的6元杂环;或R 2和R 3 一起形成氧代(= O)或触变(= S)基团; R4代表氢,C1-4烷基或苯基,其可任选地带有一个或两个卤素或硝基取代基; Z是式(a )或(b)和A-表示阴离子)及其异构体具有有用的局部麻醉剂,抗抑郁药,镇痛镇痛和平滑肌松弛剂性质,伴随较弱的镇痛剂 c效应,可用于治疗。