Esters of glucuronide prodrugs of anthracyclines and method of preparation and use in tumor-selective chemotherapy

The invention relates to novel esters and in particular to novel water soluble esters of glucuronide prodrugs of anthracyclines their synthesis and use in tumor-selective chemotherapy. It appeared that in the final step in the synthesis of these prodrugs, i.e. the coupling of the glucuronide spacer...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Hauptverfasser:	HAISMA, HIDDE JACOB, DE VOS, DICK, CORNELISSEN, JEROEN JOHANNES, LAMBERUTS, MARIA, SCHEEREN, JOHAN WILHELM, ABEN, RENE WILHELMUS MARIE
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	CHEMISTRY DERIVATIVES THEREOF HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SUGARS
Online-Zugang:	Volltext bestellen
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The invention relates to novel esters and in particular to novel water soluble esters of glucuronide prodrugs of anthracyclines their synthesis and use in tumor-selective chemotherapy. It appeared that in the final step in the synthesis of these prodrugs, i.e. the coupling of the glucuronide spacer moiety to the parent drug molecule, protection of the sugar hydroxyls is, surprisingly, no longer required. A process for the preparation of these unprotected sugar spacer moieties is also disclosed.