(19)
(11) EP 1 235 595 B8

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

(15) Correction information:
Corrected version no 1 (W1 B1)

(48) Corrigendum issued on:
07.10.2009 Bulletin 2009/41

(45) Mention of the grant of the patent:
05.08.2009 Bulletin 2009/32

(21) Application number: 00965901.2

(22) Date of filing: 28.08.2000
(51) International Patent Classification (IPC): 
A61K 47/48(2006.01)
(86) International application number:
PCT/EP2000/008361
(87) International publication number:
WO 2001/017563 (15.03.2001 Gazette 2001/11)

(54)

INTEGRIN-MEDIATED DRUG TARGETING

INTEGRIN-VERMITTELTE ARZNEIMITTEL-ZIELRICHTUNG

CIBLAGE DE MEDICAMENT INDUIT PAR L'INTEGRINE


(84) Designated Contracting States:
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

(30) Priority: 08.09.1999 US 392167
29.06.2000 US 606772

(43) Date of publication of application:
04.09.2002 Bulletin 2002/36

(73) Proprietor: Bayer Schering Pharma Aktiengesellschaft
13353 Berlin (DE)

(72) Inventors:
  • LERCHEN, Hans-Georg
    51375 Leverkusen (DE)
  • BAUMGARTEN, Jörg
    42115 Wuppertal (DE)
  • BRÜGGEMEIER, Ulf
    42799 Leichlingen (DE)
  • ALBERS, Markus
    51375 Leverkusen (DE)
  • SCHOOP, Andreas
    AT/1150 Wien (AT)
  • SCHULZE, Thomas-J
    Thousands Oaks, CA 91360 (US)


(56) References cited: : 
WO-A-93/20229
WO-A-97/39021
   
  • KERR J S ET AL: "NOVEL SMALL MOLECULE ALPHAV INTEGRIN ANTAGONISTS: COMPARATIVE ANTI-CANCER EFFICACY WITH KNOWN ANGIOGENESIS INHIBITORS" ANTICANCER RESEARCH,HELENIC ANTICANCER INSTITUTE, ATHENS,,GR, vol. 19, no. 2A, 1999, pages 959-968, XP000924849 ISSN: 0250-7005
  • FIELDS ET AL: "Integrins: cell adhesion molecules in cancer" EXPERT OPINION ON THERAPEUTIC PATENTS,GB,ASHLEY PUBLICATIONS, vol. 8, no. 6, August 1998 (1998-08), pages 633-644, XP002105988 ISSN: 1354-3776
  • CARRON C P ET AL: "A PEPTIDOMIMETIC ANTAGONIST OF THE INTEGRIN ALPHA V BETA 3 INHIBITS LEYDIG CELL TUMOR GROWTH AND THE DEVELOPMENT OF HYPERCALCEMIA OF MALIGNANCY" CANCER RESEARCH,US,AMERICAN ASSOCIATION FOR CANCER RESEARCH, BALTIMORE, MD, vol. 58, May 1998 (1998-05), pages 1930-1935, XP000915219 ISSN: 0008-5472
  • NICKOLS A ET AL: "ANTIANGIOGENIC AND ANTICANCER ACTIVITIES OF ANTAGONISTS OF INTEGRIN ALPHAVBETA3" PROCEEDINGS OF THE ANNUAL MEETING OF THE AMERICAN ASSOCIATION FOR CANCER RESEARCH,US,PHILADELPHIA, AACR, vol. 38, 1 March 1997 (1997-03-01), page 206, abstract no. 1389 XP002071773
  • T J MACDONALD ET AL: "Migration of human brain tumor cells and human brain endothelial cells on tenascin requires the integrin alphaVbeta3;a unifying model for brain tumor invasion and angiogenesis" PROC. ANNU MEET. AACR, vol. 39, 28 March 1998 (1998-03-28), page 497, abstract no. 3382 XP002141915 NEW ORLEANS, LA, MARCH 28 - APRIL 1, 1998,PHILADELPHIA, US
  • P C BROOKS ET AL: "Requirement of vascular integrin alphaV beta3 for angiogenesis" SCIENCE ,AAAS, LANCASTER, PA,US, vol. 264, 22 April 1994 (1994-04-22), pages 569-571, XP002138524 ISSN: 0036-8075
  • BROOKS P C ET AL: "INTEGRIN ALPHAVBETA3 ANTAGONISTS PROMOTE TUMOR REGRESSION BY INDUCING APOPTOSIS OF ANGIOGENIC BLOOD VESSELS" CELL,US,CELL PRESS, CAMBRIDGE, NA, vol. 79, no. 7, 30 December 1994 (1994-12-30), pages 1157-1164, XP000652129 ISSN: 0092-8674
  • VARNER J A ET AL: "TUMOR ANGIOGENESIS AND THE ROLE OF VASCULAR CELL INTEGRIN ALPHAVBETA3" IMPORTANT ADVANCES IN ONCOLOGY,LIPPINCOT-RAVEN, PHILADELPHIA,US, 1996, pages 69-87, XP000857371 ISSN: 0883-5896
  • VARNER J A ET AL: "INTEGRINS AND CANCER" CURRENT OPINION IN CELL BIOLOGY,GB,CURRENT SCIENCE, LONDON, vol. 8, no. 5, October 1996 (1996-10), pages 724-730, XP000857374 ISSN: 0955-0674
  • VARNER J A ET AL: "REVIEW: THE INTEGRIN ALPHAVBETA3: ANGIOGENESIS AND APOPTOSIS" CELL ADHESION AND COMMUNICATION,US,HARWOOD ACADEMIC PUBLISHERS, GMBH, YVERDON, vol. 3, no. 4, 1995, pages 367-374, XP000857373 ISSN: 1061-5385
  • GASPARINI G.: "The rationale and future potential of angiogenesis inhibitors in neoplasia" DRUGS, vol. 58, no. 1, July 1999 (1999-07), pages 17-38, XP001002355
  • DAMIANO JS ET AL: "Cell adhesion mediated drug resistance (CAM-DR): role of integrins and resistance to apoptosis in human myeloma cell lines." BLOOD, vol. 93, no. 5, 1 March 1999 (1999-03-01), pages 1658-1667, XP002168941
  • UHM, JOON H. ET AL: "Vitronectin, a glioma-derived extracellular matrix protein, protects tumor cells from apoptotic death" CLIN. CANCER RES., 06-1999, VOL. 5, NO. 6, PAGE(S) 1587-1594, XP002168942
  • MUELLER, B. M. ET AL: "Pre-clinical therapy of human melanoma with morpholino-doxorubicin conjugated to a monoclonal antibody directed against an integrin on melanoma cells" ANTIBODY, IMMUNOCONJUGATES, RADIOPHARM., 1991, VOL. 4, NO. 2, PAGE(S) 99-106, XP001002266
  • BITAN GAL ET AL: "Mapping the integrin alphaVbeta3-ligand interface by photoaffinity cross-linking." BIOCHEMISTRY, vol. 38, no. 11, 16 March 1999 (1999-03-16), pages 3414-3420, XP002168943 ISSN: 0006-2960
  • SHEU JOEN R ET AL: "Triflavin, an arg-gly-asp-containing peptide, inhibits the adhesion of tumor cells to matrix proteins via binding to multiple integrin receptors expressed on human hepatoma cells." PROCEEDINGS OF THE SOCIETY FOR EXPERIMENTAL BIOLOGY AND MEDICINE, vol. 213, no. 1, 1996, pages 71-79, XP001002230 ISSN: 0037-9727
  • Hart et al. (1994) JBC 269, 12468-12474.
   
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