Anthracycline conjugates with acetalic linker their preparation and pharmaceutical compositions containing them

A conjugate of formula (1), wherein the moiety A-O- is the residue of any anthracycline of formula A-O-H bearing at least one primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a residue of formula (2), wherein B represents a C1-C6 alkylene group optionally hetero interrupted...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser:	ANGELUCCI FRANCESCO, BERSANI LAURA, RUGGIERI DANIELA, STEFANELLI STEFANIA, SUARATO ANTONINO
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY DERIVATIVES THEREOF HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SUGARS
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Beschreibung
Zusammenfassung:	A conjugate of formula (1), wherein the moiety A-O- is the residue of any anthracycline of formula A-O-H bearing at least one primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a residue of formula (2), wherein B represents a C1-C6 alkylene group optionally hetero interrupted and m is 0 or 1; Z is a spacer group and T is a carrier moiety. The conjugates of formula (1) of the present invention are useful antitumor agents since they contain an acetalic bond which releases the parent drug A-O-H upon hydronium-ion-catalyzed hydrolysis or ''in vivo'' enzymatic cleavage.