USE OF CONJUGATES OF DOXORUBICIN WITH LACTOSAMINATED ALBUMIN

(19)

(11)

EP 1 937 310 B8

(12)	CORRECTED EUROPEAN PATENT SPECIFICATION
	Note: Bibliography reflects the latest situation

(15)	Correction information:
	Corrected version no 2 (W2 B1)

(48)	Corrigendum issued on:
	13.07.2011 Bulletin 2011/28

(45)	Mention of the grant of the patent:
	24.11.2010 Bulletin 2010/47

(21)	Application number: 06793626.0

(22)	Date of filing: 19.09.2006

(51)

International Patent Classification (IPC):

A61P 35/00^(2006.01)

A61K 47/48^(2006.01)

(86)	International application number:
	PCT/EP2006/066489

(87)	International publication number:
	WO 2007/039448 (12.04.2007 Gazette 2007/15)

(54)	USE OF CONJUGATES OF DOXORUBICIN WITH LACTOSAMINATED ALBUMIN VERWENDUNG VON KONJUGATEN VON DOXORUBICIN MIT LACTOSAMINIERTEM ALBUMIN UTILISATION DE CONJUGUES DE DOXORUBICINE ET D'ALBUMINE LACTOSAMINEE

(84)	Designated Contracting States:
	AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR

(30)

Priority:

20.09.2005 IT MI20051743

(43)	Date of publication of application:
	02.07.2008 Bulletin 2008/27

(73)	Proprietor: Universita' di Bologna - Dipartimento di Patologia Sperimentale
	40126 Bologna (IT)

(72)	Inventors:
	FIUME, Luigi I-40125 Bologna (IT) DI STEFANO, Giuseppina I-40068 San Lazzaro Di Savena (BO) (IT)

(74)	Representative: Pistolesi, Roberto et al
	Dragotti & Associati Srl Via Marina 6 20121 Milano 20121 Milano (IT)

(56)

References cited: :

WO-A-93/25239
WO-A2-2006/074272

WO-A2-2005/107814

STEFANO DI G ET AL: "Doxorubicin coupled to lactosaminated human albumin remains confined within mouse liver cells after the intracellular release from the carrier" DIGESTIVE AND LIVER DISEASE, W.B. SAUNDERS, vol. 35, no. 6, June 2003 (2003-06), pages 428-433, XP002361079 ISSN: 1590-8658
STEFANO G D ET AL: "A novel method for coupling doxorubicin to lactosaminated human albumin by an acid sensitive hydrazone bond: synthesis, characterization and preliminary biological properties of the conjugate" EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, ELSEVIER, AMSTERDAM, NL, vol. 23, no. 4-5, December 2004 (2004-12), pages 393-397, XP004658708 ISSN: 0928-0987
KRATZ F: "Drug conjugates with albumin and transferrin" EXPERT OPINION ON THERAPEUTIC PATENTS, ASHLEY PUBLICATIONS, GB, vol. 12, no. 3, 2002, pages 433-439, XP002337252 ISSN: 1354-3776
SEOW Y-Y T ET AL: "Expression of a functional asialoglycoprotein receptor in human renal proximal tubular epithelial cells" NEPHRON, XX, XX, vol. 91, no. 3, 2002, pages 431-438, XP008066266 ISSN: 0028-2766
TRERÈ D ET AL: "THE ASIALOGLYCOPROTEIN RECEPTOR IN HUMAN HEPATOCELLULAR CARCINOMAS: ITS EXPRESSION ON PROLIFERATING CELLS" BRITISH JOURNAL OF CANCER, LONDON, GB, vol. 81, no. 3, 1999, pages 404-408, XP008075840 ISSN: 0007-0920
SAXENA A. ET AL: "H2, the minor subunit of the human asialoglycoprotein receptor, traffics intracellularly and forms homo-oligomers, but does not bind asialo-orosomucoid" JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 277, no. 38, 2002, pages 35297-35304, XP002423100
FIUME ET AL: "Doxorubicin coupled to lactosaminated albumin inhibits the growth of hepatocellular carcinomas induced in rats by diethylnitrosamine" JOURNAL OF HEPATOLOGY, MUNKSGAARD INTERNATIONAL PUBLISHERS, COPENHAGEN, DK, vol. 43, no. 4, October 2005 (2005-10), pages 645-652, XP005058385 ISSN: 0168-8278
DI STEFANO G ET AL: "ENHANCED UPTAKE OF LACTOSAMINATED HUMAN ALBUMIN BY RAT HEPATOCARCINOMAS: IMPLICATIONS FOR AN IMPROVED CHEMOTHERAPY OF PRIMARY LIVER TUMORS" LIVER INTERNATIONAL, BLACKWELL MUNKSGAARD, OXFORD, GB, vol. 25, no. 4, 2005, pages 854-860, XP008075833 ISSN: 1478-3223
DI STEFANO ET AL: "Doxorubicin coupled to lactosaminated albumin: Enhanced drug levels in rat hepatocarcinomas" DIGESTIVE AND LIVER DISEASE, W.B. SAUNDERS, vol. 38, no. 4, April 2006 (2006-04), pages 284-285, XP005347320 ISSN: 1590-8658
DI STEFANO G ET AL: "A CONJUGATE OF DOXORUBICIN WITH LACTOSAMINATED ALBUMIN ENHANCES THE DRUG CONCENTRATIONS IN ALL THE FORMS OF RAT HEPATOCELLULAR CARCINOMAS INDEPENDENTLY OF THEIR DIFFERENTIATION GRADE" LIVER INTERNATIONAL, BLACKWELL MUNKSGAARD, OXFORD, GB, vol. 26, no. 6, 2006, pages 726-733, XP008075839 ISSN: 1478-3223
HARRIS L ET AL: "Patterns of ligand binding to normal, regenerating, preneoplastic, and neoplastic rat hepatocytes" CANCER RESEARCH 1987 US, vol. 47, no. 15, 1987, pages 3954-3958, ISSN: 0008-5472
ASHWELL G ET AL: "CARBOHYDRATE SPECIFIC RECEPTORS OF THE LIVER" SNELL, E. E. (ED.). ANNUAL REVIEW OF BIOCHEMISTRY, VOL. 51. XII+1055P. ANNUAL REVIEWS INC.: PALO ALTO, CALIF., USA. ILLUS SERIES : ANNUAL REVIEW OF BIOCHEMISTRY (ISSN 0066-4154), 1982, pages P531-554,
FIUME L ET AL: "Lactosaminated human serum albumin as hepatotropic drug carrier. Rate of uptake by mouse liver" FEBS LETTERS 1982 NL LNKD- DOI:10.1016/0014-5793(82)80701-1, vol. 146, no. 1, 1982, pages 42-46, ISSN: 0014-5793

Note: Within nine months from the publication of the mention of the grant of the European patent, any person may give notice to the European Patent Office of opposition to the European patent granted. Notice of opposition shall be filed in a written reasoned statement. It shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention).