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
Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula Iwherein: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; andn 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) reducechronic 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.
展开▼
机译:式I的苯基-3-氨基烷基-4-甲基-2,6-二氧杂哌啶 <图像文件=“ IMGA0001.GIF” he =“ 34” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 73” /> Chemistry>其中: R 1 Sub>代表甲氧基,乙氧基或羟基, ListItem> R 2 Sub>代表甲氧基,乙氧基。羟基或氢; ListItem> 每个R 3 Sub>分别代表甲基或乙基; ListItem> R 4 Sub>代表氢或甲基; ListItem> R 5 Sub>表示氢或甲基;并且 ListItem> n代表2或3, ListItem> UnorderedList>及其药理学上可接受的酸加成盐(a)具有抗焦虑活性,(b)拮抗苯并二氮杂in反向激动剂的抗焦虑活性。 (c)降低大脑中5-羟色胺或其代谢产物5-羟基-吲哚乙酸的异常异常高水平;(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。
展开▼