(19)
(11) EP 3 351 246 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:
18.09.2019 Bulletin 2019/38

(45) Mention of the grant of the patent:
22.05.2019 Bulletin 2019/21

(21) Application number: 18155644.0

(22) Date of filing: 18.02.2002
(51) International Patent Classification (IPC): 
A61K 31/436(2006.01)
A61P 35/04(2006.01)
A61P 35/00(2006.01)

(54)

RAPAMYCIN DERIVATIVE FOR THE TREATMENT OF A SOLID TUMOR ASSOCIATED WITH DEREGULATED ANGIOGENESIS

RAPAMYCIN-DERIVAT ZUR BEHANDLUNG EINES SOLIDEN TUMORS, DER MIT DEREGULIERTER ANGIOGENESE ASSOZIIERT IST

DÉRIVÉ DE RAPAMYCINE POUR LE TRAITEMENT D'UNE TUMEUR SOLIDE ASSOCIÉE À UNE ANGIOGENÈSE DÉRÉGULÉE


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

(30) Priority: 19.02.2001 GB 0104072
17.10.2001 GB 0124957

(43) Date of publication of application:
25.07.2018 Bulletin 2018/30

(62) Application number of the earlier application in accordance with Art. 76 EPC:
16186041.6 / 3143995
14164259.5 / 2783686
02719864.7 / 1363627

(73) Proprietors:
  • Novartis Pharma AG
    4056 Basel (CH)
  • Novartis International Pharmaceutical AG
    4056 Basel (CH)

(72) Inventors:
  • Lane, Heidi
    4106 Therwill (CH)
  • O`Reilly, Terence
    4057 Basel (CH)
  • Wood, Jeanette Marjorie
    4105 Biel-Benken (CH)

(74) Representative: Carpmaels & Ransford LLP 
One Southampton Row
London WC1B 5HA
London WC1B 5HA (GB)


(56) References cited: : 
WO-A1-01/51049
WO-A1-97/47317
WO-A1-94/09010
US-A- 5 206 018
   
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  • SHAH SHIMUL A ET AL: "FRAP-p70s6K Signaling Is Required for Pancreatic Cancer Cell Proliferation", JOURNAL OF SURGICAL RESEARCH, ACADEMIC PRESS INC., SAN DIEGO, CA, US, vol. 97, no. 2, 2 November 2000 (2000-11-02), pages 123-130, XP029590080, ISSN: 0022-4804, DOI: 10.1006/JSRE.2001.6145
  • HIDALGO M ET AL: "THE RAPAMYCIN-SENSITIVE SIGNAL TRANSDUCTION PATHWAY AS A TARGET FOR CANCER THERAPY", ONCOGENE, NATURE PUBLISHING GROUP UK, LONDON, vol. 19, no. 56, December 2000 (2000-12), pages 6680-6686, XP009002368, ISSN: 0950-9232, DOI: 10.1038/SJ.ONC.1204091
  • SEUFFERLEIN T ET AL: "Constitutive activation of p70s6k in human pancreatic cancer cell lines bearing activating Ki-ras mutations", GASTROENTEROLOGY, W.B. SAUNDERS CO, US, vol. 114, 15 April 1998 (1998-04-15), page A496, XP027466913, ISSN: 0016-5085, DOI: 10.1016/S0016-5085(98)82012-X [retrieved on 1998-04-15]
  • SEUFFERLEIN THOMAS ET AL: "Rapamycin inhibits constitutive p70-s6k phosphorylation, cell proliferation, and colony formation in small cell lung cancer cells", CANCER RESEARCH, AACR - AMERICAN ASSOCIATION FOR CANCER RESEARCH, US, vol. 56, no. 17, 1996, pages 3895-3897, XP002766076, ISSN: 0008-5472
  • HIDALGO M ET AL: "A phase I and pharmacological study of CCI-779, a rapamycin ester cell cycle inhibitor. ADIS TITLE: CCI 779: therapeutic use Solid tumours Phase I trial", ANNALS OF ONCOL, KLUWER, DORDRECHT, NL, vol. 11, no. Suppl. 4, 2000, page 133, XP009193116, ISSN: 0923-7534
  • HIDALGO M ET AL: "CCI-779, a rapamycin analog and multifaceted inhibitor of signal transduction: a phase I study. ADIS TITLE: CCI 779: therapeutic use Solid tumours Phase I trial", PROGRAM/PROCEEDINGS - AMERICAN SOCIETY OF CLINICAL ONCOLOGY, THE SOCIETY, US, vol. 19, 2000, page 187, XP009193117, ISSN: 1081-0641
  • TSUCHIYA N ET AL: "EFFECTS OF FADROZOLE AND LEUPRORELIN ACETATE ON AROMATASE ACTIVITY AND CELL PROLIFERATION IN A HUMAN BREAST CANCER CELL LINE (SK-BR-3)", INTERNATIONAL JOURNAL OF CLINICAL ONCOLOGY, CHURCHILL LIVINGSTONE JAPAN, TOKYO, GB, vol. 5, 1 January 2000 (2000-01-01), pages 183-187, XP001069645, ISSN: 1341-9625
  • BUZDAR A ET AL: "Advances in aromatase inhibition: clinical efficacy and tolerability in the treatment of breast cancer", CLINICAL CANCER RESEARCH, THE AMERICAN ASSOCIATION FOR CANCER RESEARCH, US, vol. 7, no. 9, 1 September 2001 (2001-09-01), pages 2620-2635, XP002784456, ISSN: 1078-0432
  • CLEMETT DELYTH ET AL: "Exemestane: A review of its use in postmenopausal women with advanced breast cancer", DRUGS, ADIS INTERNATIONAL LTD, NZ, vol. 59, no. 6, 1 June 2000 (2000-06-01), pages 1279-1296, XP002784405, ISSN: 0012-6667
  • GOSS P E ET AL: "Aromatase inhibitors in the treatment and prevention of breast cancer", JOURNAL OF CLINICAL ONCOLOGY, AMERICAN SOCIETY OF CLINICAL ONCOLOGY, US, vol. 19, no. 3, 1 February 2001 (2001-02-01), pages 881-894, XP003022842, ISSN: 0732-183X
  • YU K ET AL: "MTOR, A NOVEL TARGET IN BREAST CANCER: THE EFFECT OF CCI-779, AN MTOR INHIBITOR, IN PRECLINICAL MODELS OF BREAST CANCER", ENDOCRINE - RELATED CANCER, BIOSCIENTIFICA LTD, GB, vol. 8, no. 3, 1 September 2001 (2001-09-01), pages 249-258, XP001079023, ISSN: 1351-0088, DOI: 10.1677/ERC.0.0080249
   
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).