Anthracycline derivatives having cytostatic activity

US4948880A · kind A · utility

Assignee

• Behringwerke Aktiengesellschaft · DE

Inventors

• Peter Hermentin · Marburg, DE
• Michael Paal · Hamburg, DE
• Hans Kraemer · Marburg, DE
• Cenek Kolar · Marburg, DE
• Dieter Hoffmann · Marburg, DE
• Manfred Gerken · Marburg, DE
• Hans G. Berscheid · Schwalbach am Taunus, DE
• Dirk Bottger · Liederbach, DE

Key dates

• Filing date: Dec 4, 1987
• Grant date: Aug 14, 1990
• Expiry date: Dec 4, 2007

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, which are optionally in the form of a salt of an inorganic or organic acid, ##STR1## in which the substituents have the following meaning: R.sup.1 is hydrogen or a hydroxyl group, PA0 R.sup.2 is hydrogen or a hydroxyl or a methoxy group, PA0 R.sup.3 is hydrogen or a hydroxyl group, PA0 R.sup.4 is hydrogen or a hydroxyl group, PA0 R.sup.5 is hydrogen, a hydroxyl or a methoxycarbonyl group, or a substituent of the general formula II, ##STR2## in which R.sup.8a has the meaning indicated for R.sup.8, or a substituent of the formula III, ##STR3## R.sup.6 is ethyl, methylcarbonyl, hydroxymethylcarbonyl, hydroxyalkyl or a dihydroxyalkyl, PA0 R.sup.7 is hydrogen or a substituent of the general formula IV, ##STR4## and R.sup.8 is hydrogen or a cyanomethyl group or a substituent of the general formula COR.sup.9 or CH.sub.2 R.sup.10, R.sup.9 being hydrogen, CH.sub.3, CF.sub.3 or CCl.sub.3, and R.sup.10 being C.sub.1 - to C.sub.8 -alkyl, substituted alkyl, phenyl or substituted phenyl, to a process for their preparation and to their use in pharmaceuticals.