.alpha.-ACETYLENIC DERIVATIVES OF AMINES

US4139563A · kind A · utility

Assignee

• Merrell Toraude et Compagnie · FR

Inventors

• Brian W. Metcalf · Moraga, US
• Michel Jung · Illkirch-Graffenstaden, FR

Key dates

• Filing date: Jul 1, 1977
• Grant date: Feb 13, 1979
• Expiry date: Jul 1, 1997

Classification

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

Abstract

Novel acetylenic derivatives of amines of the following general structure: ##STR1## WHEREIN Z is .beta.-methylthioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, or ##STR2## WHEREIN N IS 2 OR 3 AND R.sub.1 is hydrogen or lower alkyl of from 1 to 4 carbon atoms with the proviso that when R.sub.1 is other than hydrogen, n is 2; and each of R.sub.a and R.sub.b is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; with the provisos that when Z is .beta.-benzylthioethyl or S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, R.sub.b is hydrogen, and when Z is ##STR4## EACH OF R.sub.a and R.sub.b can be the same or different; and pharmaceutically acceptable salts and individual optical isomers thereof.