Patent · US Expired

Pharmaceutical compositions and medical uses of dioxopiperidine derivatives

US4738973A · kind A · utility

7Cited by
2References
4Claims
0Family size

Assignee

Inventor

Key dates

Filing dateSep 10, 1986
Grant dateApr 19, 1988
Priority date
Expiry dateSep 10, 2006

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61P25/30
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents methoxy, ethoxy or hydroxy, PA1 R.sub.2 represents methoxy, ethoxy, hydroxy or hydrogen; PA1 each R.sub.3 independently represents methyl or ethyl; PA1 R.sub.4 represents hydrogen or methyl; PA1 R.sub.5 represents hydrogen or methyl; and PA1 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 depolarization activation of tryptophan hydroxylase. Novel compositions comprise the compounds with a benzodiazepine agonist or benzodiazepine inverse agonist.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.