首页> 外国专利> Use of dioxopiperidine derivatives in the treatment of anxiety, for the reduction of chronic abnormally high brain levels of serotonin or 5-hydroxy-indoleacetic acid, and in the treatment of bacterial or viral infections

Use of dioxopiperidine derivatives in the treatment of anxiety, for the reduction of chronic abnormally high brain levels of serotonin or 5-hydroxy-indoleacetic acid, and in the treatment of bacterial or viral infections

机译:二氧哌啶衍生物在治疗焦虑症,减少慢性异常高脑水平的血清素或5-羟基吲哚乙酸以及治疗细菌或病毒感染中的用途

摘要

Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I …CHEM… wherein:… R1 represents methoxy, ethoxy or hydroxy,… R2 represents methoxy, ethoxy, hydroxy or hydrogen;… each R3 independently represents methyl or ethyl;… R4 represents hydrogen or methyl;… R5 represents hydrogen or methyl; and… n represents 2 or 3,… and a pharmacologically acceptable acid addition salt thereof (a) have anxiolytic activity, (b) antagonize the anxiogenic activity of benzodiazepine inverse agonists, (c) reduce chronic abnormally high brain levels of serotonin or its metabolite 5-hydroxy-indoleacetic acid and (d) have antibacterial and antiviral activity. These activities are believed to be related to a reduction in serotonin turnover caused by blocking the depolarisation activation of tryptophan hydroxylase. Novel compositions comprise the compounds with a benzodiazepine agonist or benzodiazepine inverse agonist.
机译:式I的苯基-3-氨基烷基-4-甲基-2,6-二氧杂哌啶……:CHEM>…:…R1代表甲氧基,乙氧基或羟基,…R2代表甲氧基,乙氧基,羟基或氢;…每个R3独立地代表甲基或乙基;…R4代表氢或甲基;…R5代表氢或甲基;和…n代表2或3,…及其药理学上可接受的酸加成盐(a)具有抗焦虑活性,(b)拮抗苯二氮卓类反向激动剂的抗焦虑活性,(c)降低慢性异常高血清素或其代谢产物的大脑水平5-羟基吲哚乙酸和(d)具有抗菌和抗病毒活性。据信这些活性与通过阻断色氨酸羟化酶的去极化激活引起的5-羟色胺更新有关。新的组合物包含具有苯并二氮杂激动剂或苯并二氮杂in反向激动剂的化合物。

著录项

  • 公开/公告号EP0216555B1

    专利类型

  • 公开/公告日1992-09-02

    原文格式PDF

  • 申请/专利权人 BRITISH TECHNOLOGY GROUP LTD;

    申请/专利号EP19860306920

  • 发明设计人 GITTOS MAURICE WARD;

    申请日1986-09-08

  • 分类号A61K31/445;

  • 国家 EP

  • 入库时间 2022-08-22 05:30:31

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