Derivatives of doxorubicine, their preparation and use

US4296105A · kind A · utility

Assignee

• Institut International de Pathologie Cellulaire et Moleculaire · BE

Inventors

• Roger Baurain · Hamme-Mille, BE
• Andre Trouet · Winksele, BE

Key dates

• Filing date: Jul 5, 1979
• Grant date: Oct 20, 1981
• Expiry date: Jul 5, 1999

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

New derivatives of doxorubicine of the formula ##STR1## wherein R represents a radical of the formula ##STR2## wherein R.sub.1 represents hydrogen, alkyl (possibly substituted with amino, alkylamino, dialkylamino, hydroxy, mercapto or methylthio), phenyl, benzyl (possibly substituted with one or more hydroxy) and R.sub.2 represents hydrogen or forms with R.sub.1 an alkylene radical, the salts thereof and pharmaceutical compositions containing said compounds. They are prepared according to methods known in peptidic chemistry by reacting a reactive form of an aminoacid of the formula ##STR3## with doxorubicine.