Tripeptide derivatives with central nervous system activity and preparation thereof

USRE30496E · kind E · reissue

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: Feb 26, 1979
• Grant date: Jan 27, 1981
• Expiry date: Feb 26, 1999

Classification

• Technology area (CPC —): General

Abstract

The tripeptide derivatives of formula 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' 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, .Iadd.and with the further proviso that when R.sup.1 is hydrogen, R.sup.2 is hydrogen or lower alkyl and Y is Gly then R.sup.3 is amino(lower)alkylamino, .Iaddend.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.