Benzodiazepine antagonistic .beta.-carboline derivatives and compositions thereof

US4600715A · kind A · utility

Assignee

• Shering Corporation · DE

Inventors

• Andreas Huth · Berlin, DE
• Ralph Schmiechen · Berlin, DE
• Dieter Seidelmann · Berlin, DE
• Dieter Rahtz · Berlin, DE
• Mogens Engelstoft
• Claus T. Braestrup · Copenhagen, DK

Key dates

• Filing date: Jun 22, 1984
• Grant date: Jul 15, 1986
• Expiry date: Jun 22, 2004

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/18
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

.beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.3 is ##STR2## wherein R.sup.5 is C.sub.1-5 alkyl, R.sup.6 is lower alkyl, aralkyl, or alkoxyalkyl of up to 7 carbon atoms, and R.sup.7 and R.sup.8 are hydrogen C.sub.1-5 alkyl, or, collectively with the amido nitrogen atom, piperidino, PA0 R.sup.4 is hydrogen, C.sub.1-3 alkyl, or CH.sub.2 OR.sup.9 wherein R.sup.9 is C.sub.1-3 alkyl, atoms, and PA0 R.sup.A is --COOR.sup.10 ##STR3## wherein R.sup.10 is hydrogen, lower alkyl, alkoxyalkyl or alkenyl of up to 5 carbon atoms, or benzyl, or X is oxygen or sulfur, and R.sup.11 and R.sup.12 each are hydrogen, lower alkyl or alkenyl or, collectively with the amido nitrogen atom, represent a hetero ring, are prepared by conventional methods and exhibit, inter alia, an effect on the central nervous system and are suitable for use as psychopharmaceuticals.