Pharmaceutical compositions and medical uses of...

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A - Human Necessities

61

K

167/232

A61K 31/445 (2006.01)

Patent

CA 1273879

ABSTRACT PHARMACEUTICAL COMPOSITIONS AND MEDICAL USES OF DIOXOPIPERIDINE DERIVATIVES Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I Image 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.

518034

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