Tripeptide derivatives with central nervous system activity and preparation thereof

US4018912A · kind A · utility

Assignee

• Ayerst, McKenna & Harrison, Inc. · CA

Inventors

• Amedeo A. Failli · Princeton Junction, US
• Hans U. Immer · Mount Royal, CA
• Manfred Götz · Brakel, DE

Key dates

• Filing date: Jul 28, 1975
• Grant date: Apr 19, 1977
• Expiry date: Jul 28, 1995

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

The tripeptide derivatives of formula 1 EQU H--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1) in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R.sup.1 is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.