14-AMINO STEROID DERIVATIVES,A PROCESS FOR THE PREPARATION THEREOF AND METHOD OF USE THEREOF

摘要

For the Contracting States BE, CH, LI, DE, FR, GB, IT, NL, SE 1. 14-amino steroid derivatives represented by general Formula (I) : see diagramm : EP0101659,P10,F1 wherein R represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R1 represents a substituted or unsubstituted sugar residue, and R2 represents a hydrogen atom, a hydroxyl group or an -OR3 group, wherein R3 is a substituted or unsubstituted sugar residue, and acid salts thereof. For the Contracting State : AT 1. A process for the preparation of 14-amino steroid derivatives represented by general Formula (I) : see diagramm : EP0101659,P10,F1 wherein R represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R1 represents a substituted or unsubstituted sugar residue, and R2 represents a hydrogen atom, a hydroxyl group or an -OR3 group, wherein R3 is a substituted or unsubstituted sugar residue characterized in that it comprises coupling the 14-amino steroid of general Formula II : see diagramm : EP0101659,P10,F2 wherein R is a hydrogen atom or a lower alkyl group, and R'2 is a hydrogen atom or a hydroxyl group, after preliminary protection of the -NH2 group at the 14-position and the -OH group at the 20-position, with an activated sugar of the formula R1 -X, wherein R1 is a sugar residue and X is a halogen atom or an acetylated group ; and, if desired, removing the protective groups.