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Extract from the Register of European Patents

EP About this file: EP2633856

EP2633856 - ATP citrate lyase inhibitors for treating cancer [Right-click to bookmark this link]
StatusThe application is deemed to be withdrawn
Status updated on  28.11.2014
Database last updated on 25.09.2024
Most recent event   Tooltip28.11.2014Application deemed to be withdrawnpublished on 31.12.2014  [2015/01]
Applicant(s)For all designated states
The Trustees of The University of Pennsylvania
3160 Chestnut Street, Suite 200
Philadelphia, PA 19104-6283 / US
[N/P]
Former [2013/36]For all designated states
The Trustees of The University of Pennsylvania
3160 Chestnut Street, Suite 200 Philadelphia
Pennsylvania 19104-6283 / US
Inventor(s)01 / Thompson, Craig B.
304 Mallwyd Road
Merion Station, PA 19066 / US
02 / Bauer, Daniel
251 South 22nd Street
Philadelphia, PA 19103 / US
03 / Hatzivassiliou, Georgia
2425 Lombard Street
Philadelphia, PA 19146 / US
 [2013/36]
Representative(s)Lau, Sarah Jane
Kilburn & Strode LLP
Lacon London
84 Theobalds Road
London WC1X 8NL / GB
[N/P]
Former [2013/36]Lau, Sarah Jane
Kilburn & Strode LLP 20 Red Lion Street
London WC1R 4PJ / GB
Application number, filing date13155657.307.05.2004
[2013/36]
Priority number, dateUS20030469233P09.05.2003         Original published format: US 469233 P
[2013/36]
Filing languageEN
Procedural languageEN
PublicationType: A2 Application without search report 
No.:EP2633856
Date:04.09.2013
Language:EN
[2013/36]
Type: A3 Search report 
No.:EP2633856
Date:01.01.2014
Language:EN
[2014/01]
Search report(s)(Supplementary) European search report - dispatched on:EP04.12.2013
ClassificationIPC:A61K31/34, A61P35/00, A61K51/04
[2013/37]
CPC:
A61K31/34 (EP,US); A61K51/0491 (EP,US); A61P35/00 (EP);
A61P43/00 (EP)
Designated contracting statesAT,   BE,   BG,   CH,   CY,   CZ,   DE,   DK,   EE,   ES,   FI,   FR,   GB,   GR,   HU,   IE,   IT,   LI,   LU,   MC,   NL,   PL,   PT,   RO,   SE,   SI,   SK,   TR [2013/36]
TitleGerman:ATP-Citrat-Lyasehemmer zur Behandlung von Krebs[2013/36]
English:ATP citrate lyase inhibitors for treating cancer[2013/36]
French:Inhibiteurs de lyase de citrate d'ATP pour le traitement du cancer[2013/36]
Examination procedure02.07.2014Application deemed to be withdrawn, date of legal effect  [2015/01]
07.08.2014Despatch of communication that the application is deemed to be withdrawn, reason: examination fee not paid in time  [2015/01]
Parent application(s)   TooltipEP04751597.8  / EP1626711
Fees paidRenewal fee
14.03.2013Renewal fee patent year 03
14.03.2013Renewal fee patent year 04
14.03.2013Renewal fee patent year 05
14.03.2013Renewal fee patent year 06
14.03.2013Renewal fee patent year 07
14.03.2013Renewal fee patent year 08
14.03.2013Renewal fee patent year 09
28.05.2013Renewal fee patent year 10
Penalty fee
Additional fee for renewal fee
31.05.201411   M06   Not yet paid
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Responsibility for the accuracy, completeness or quality of the data displayed under the link provided lies entirely with the Unified Patent Court.
Documents cited:Search[Y]WO02070676  (MERCK PATENT GMBH [DE], et al) [Y] 1-11 * page 10, line 32 - page 11, paragraph 1 *;
 [AD]WO9322304  (SMITHKLINE BEECHAM PLC [GB], et al) [AD] 1-11 * claims 1-17 * * page 1, paragraph 3 *;
 [AD]US5447954  (GRIBBLE ANDREW D [GB], et al) [AD] 1-11 * column 1 - lines 24-62 *
 [Y]  - SULLIVAN A C ET AL, "Reactivity and inhibitor potential of hydroxycitrate isomers with citrate synthase, citrate lyase, and ATP citrate lyase", vol. 252, no. 21, ISSN 0021-9258, (19771110), pages 7583 - 7590, JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY FOR BIOCHEMISTRY AND MOLECULAR BIOLOGY, US, URL: http://www.jbc.org/content/252/21/7583.abstract, XP008163761 [Y] 1-11 * abstract *
 [Y]  - SZUTOWICZ A ET AL, "Effect of (-)hydroxycitrate on the activities of ATP citrate lyase and the enzymes of acetyl CoA metabolism in rat brain", ACTA BIOCHIMICA POLONICA, POLSKIE TOWARZYSTWO BIOCHEMICZNE, PL, (19760101), vol. 23, no. 2-3, ISSN 0001-527X, pages 227 - 234, XP008163764 [Y] 1-11 * abstract *
 [A]  - KARZEL K ET AL, "[The effect of benzenecarboxylic acids--in particular mellitic acid--in in vitro biological system]", ARZNEIMITTEL-FORSCHUNG JAN 1989 LNKD- PUBMED:2719744, (198901), vol. 39, no. 1, ISSN 0004-4172, pages 6 - 11, XP008125960 [A] 1 * abstract * * page 7; table 1 *
by applicantUS5447954
 US6414002
 US2003087935
 US2003069275
    - CZEMIN, J., ACTA MEDICA AUSTRIACA, (2002), vol. 29, pages 162 - 170
    - VANDER HEIDEN, M. G. ET AL., CELL, (1997), vol. 91, pages 627 - 637
    - ELSHOURBAGY, N. A. ET AL., J BIOL CHEM, (1990), vol. 265, pages 1430 - 1435
    - ELSHOURBAGY, N. A. ET AL., BUR J BIOCHEM, (1992), vol. 204, pages 491 - 499
    - FUKUDA, H. ET AL., J BIOCHEM (TOKYO, (1999), vol. 126, pages 437 - 444
    - BARROW ET AL., "Antimycins, Inhibitors of ATP-Citrate Lyase, from a Streptomyces sp.", JOURNAL OF ANTIBIOTICS, (1997), vol. 50, no. 9, page 729
    - HOFFINANN GE ET AL., BIOCHIM BIOPHYS ACTA, (19801006), vol. 620, no. 1, pages 151 - 8
    - SZUTOWICZ A ET AL., ACTA BIOCHIM POL, (1976), vol. 23, no. 2-3, pages 227 - 34
    - SULLIVAN AC ET AL., J BIOL CHEM, (19771110), vol. 252, no. 21, pages 7583 - 90
    - KAPLAN ET AL., J BIOL CHEM, (19900805), vol. 265, no. 22, pages 13379 - 85
    - ZARA V ET AL., BIOCHEM BIOPHYS RES COMMUN, (19960625), vol. 223, no. 3, pages 508 - 13
    - STIPANI, I ET AL., FEBS LETT, (19830919), vol. 161, no. 2, pages 269 - 74
    - LAW D ET AL., AM J PHYSIOL, (199207), vol. 263, no. 1, pages C220 - 5
    - PARADIES G ET AL., ARCH BIOCHEM BIOPHYS, (19900501), vol. 278, no. 2, pages 425 - 30
    - SIMPSON W. J. ET AL., "Influence of location and extent of surgical resection on survival of patients with glioblastoma multiforms: Results of three consecutive Radiation Therapy Oncology Group (RTOG) clinical trials", INT J RADIAT ONCOL BIOL PHYS, (1993), vol. 26, pages 239 - 244, XP026848892
    - BORGELT ET AL., "The palliation of brain metastases: Final results of the first two studies of the Radiation Therapy Oncology Group", INT J RADIAT ONCOL BIOL PHYS, (1980), vol. 6, pages 1 - 9
    - BERKHOUT, T.A. ET AL., BIOCHEM J., (1990), vol. 272, pages 181 - 186
    - BARTH, C.; HACKENSCHMIDT, J.; ULMANN, H.; DECKER, K., "Inhibition of cholesterol synthesis by (-)-hydroxycitrate in perfused rat liver. Evidence for an extramitochondrial mevalonate synthesis from acetyl coenzyme A", FEBS LETT, (1972), vol. 22, doi:doi:10.1016/0014-5793(72)80266-7, pages 343 - 346, XP025600375

DOI:   http://dx.doi.org/10.1016/0014-5793(72)80266-7
    - BENJAMIN, W. B.; PENTYALA, S. N.; WOODGETT, J. R.; HOD, Y.; MARSHAK, D., "ATP citrate lyase and glycogen synthase kinase-3 beta in 3T3-Ll cells during differentiation into adipocytes", BIOCHEM J, (1994), vol. 300, pages 477 - 482
    - BERKHOUT, T.A.; HAVEKES, K. M.; PEARCE, N. J.; GROOT, P. H., "The effect of (-)-hydroxycitrate on the activity of the low-density-lipoprotein receptor and 3-hydroxy-3-methylglutaryl-CoA reductase levels in the human hepatoma cell line Hep G2", BIOCHEM J., (1990), vol. 272, pages 181 - 186, XP008125901
    - BERWICK, D. C.; HERS, I.; HEESOM, K. J.; MOULE, S. K.; TAVARE, J. M., "The identification of ATP-citrate lyase as a protein kinase B (Akt) substrate in primary adipocytes", JBIOL CHEM, (2002), vol. 277, pages 33895 - 33900
    - DOLLE, R. E.; MCNAIR, D.; HUGHES, M. J.; KRUSE, L. I.; EGGELSTON, D.; SAXTY, B. A.; WELLS, T. N.; GROOT, P. H., "ATP-citrate lyase as a target for hypolipidemic intervention. Sulfoximine and 3-hydroxy-beta-lactam containing analogues of citric acid as potential tight- binding inhibitors", J MED CHEM, (1992), vol. 35, pages 4875 - 4884
    - DOLLE, R. E.; GRIBBLE, A.; WILKES, T.; KRUSE, L. I.; EGGLESTON, D.; SAXTY, B. A.; WELLS, T. N.; GROOT, P. H., "Synthesis of novel thiol-containing citric acid analogues. Kinetic evaluation of these and other potential active-site-directed and mechanism-based inhibitors of ATP citrate lyase", J MED CHEM, (1995), vol. 38, doi:doi:10.1021/jm00003a016, pages 537 - 543, XP009059143

DOI:   http://dx.doi.org/10.1021/jm00003a016
    - ELSHOURBAGY, N. A.; NEAR, J. C.; KMETZ, P. J.; SATHE, G. M.; SOUTHAN, C.; STRICKLER, J. E.; GROSS, M.; YOUNG, J. F.; WELLS, T. N.;, "Rat ATP citrate lyase. Molecular cloning and sequence analysis of a full-length cDNA and mRNA abundance as a function of diet, organ, and age", J BIOL CHEM, (1990), vol. 265, pages 1430 - 1435
    - ELSHOURBAGY, N. A.; NEAR, J. C.; KMETZ, P. J.; WELLS, T. N.; GROOT, P. H.; SAXTY, B. A.; HUGHES, S. A.; FRANKLIN, M.; GLOGER, 1. S, "Cloning and expression of a human ATP-citrate lyase cDNA", EUR J BIOCHEM, (1992), vol. 204, pages 491 - 499
    - FANG, M.; LOWENSTEIN, J. M., "Citrate and the conversion of carbohydrate into fat. The regulation of fatty acid synthesis by rat liver extracts", BIOCHEM J, (1967), vol. 105, pages 803 - 811
    - FRAUWIRTH, K. A.; RILEY, J. L.; HARRIS, M. H.; PARRY, R. V.; RATHMELL, J. C.; PLAS, D. R.; ELSTROM, R. L.; JUNE, C. H.; THOMPSON,, "The CD28 signaling pathway regulates glucose metabolism", IMMUNITY, (2002), vol. 16, pages 769 - 777
    - FUKUDA, H.; IRITANI, N., "Regulation of ATP citrate lyase gene expression in hepatocytes and adipocytes in normal and genetically obese rats", J BIOCHEM (TOKYO, (1999), vol. 126, pages 437 - 444
    - GRIBBLE, A. D.; DOLL, R. E.; SHAW, A.; MCNAIR, D.; NOVELLI, R.; NOVELLI, C. E.; SLINGSBY, B. P.; SHAH, V. P.; TEW, D.; SAXTY, B. A, "ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme", J MED CHEM, (1996), vol. 39, doi:doi:10.1021/jm960167w, pages 3569 - 3584, XP055135333

DOI:   http://dx.doi.org/10.1021/jm960167w
    - GRIBBLE, A. D.; IFE, R. J.; SHAW, A.; MCNAIR, D.; NOVELLI, C. E.; BAKEWELL, S.; SHAH, V. P.; DOLLE, R. E.; GROOT, P. H.; PEARCE, N, "ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3- carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo", J MED CHEM, (1998), vol. 41, pages 3582 - 3595
    - INOUE, J.; SUZUKI, F.; FUKUNISHI, K.; ADACHI, K.; TAKEDA, Y., "Studies on ATP citrate lyase of rat liver", J BIOL CHEM, (1966), vol. 60, pages 543 - 553
    - LOWENSTEIN, J. M., "Effect of (-)-hydroxycitrate on fatty acid synthesis by rat liver in vivo", J BIOL CHEM, (1971), vol. 246, pages 629 - 632
    - MORIKAWA, J.; NISHIMURA, Y.; UCHIDA, A.; TANAKA, T., "Molecular cloning of novel mouse and human putative citrate lyase beta-subunit", BIOCHEM BIOPHYS RES COMMUN, (2001), vol. 289, pages 1282 - 1286
    - PEARCE, N. J.; YATES, J. W.; BERKHOUT, T. A.; JACKSON, B.; TEW, D.; BOYD, H.; CAMILLERI, P.; SWEENEY, P.; GRIBBLE, A. D.; SHAW, A., "The role of ATP citrate lyase in the metabolic regulation of plasma lipids. Hypolipidaemic effects of SB-204990, a lactone prodrug of the potent ATP citrate lyase inhibitor SB-201076", BIOCHEM J, (1998), vol. 334, pages 113 - 119, XP008125902
    - PLAS, D. R.; TALAPATRA, S.; EDINGER, A. L.; RATHMELL, J. C.; THOMPSON, C. B., "Akt and Bel-XL promote growth factor-independent survival through distinct effects on mitochondrial physiology", J BIOL CHEM, (2001), vol. 276, pages 12041 - 12048
    - SAXTY, B. A.; NOVELLI, R.; DOLLE, R. E.; KRUSE, L. I.; REID, D. G.; CAMILLERI, P.; WELLS, T. N., "Synthesis and evaluation of (+) and (-)-2,2-difluorocitrate as inhibitors of rat- liver ATP-citrate lyase and porcine-heart aconitase", EUR J BIOCHEM, (1991), vol. 202, pages 889 - 896
    - SULLIVAN, A. C.; TRISCARI, J.; HAMILTON, J. G.; MILLER, O. N.; WHEATLEY, V. R., "Effect of (-)-hydroxycitrate upon the accumulation of lipid in the rat. I. Lipogenesis", LIPIDS, (1974), vol. 9, pages 121 - 128
    - SULLIVAN, A. C.; TRISCARI, J.; HAMILTON, J. G.; MILLER, O. N., "Effect of (-)-hydroxycitrate upon the accumulation of lipid in the rat. II", APPETITE. LIPIDS, (1974), vol. 9, pages 129 - 134
    - SULLIVAN, A. C.; DAIRMAN, W.; TRISCARI, J., "threo-Chlorocitric acid: a novel anorectic agent", PHARMACOL BIOCHEM BEHAV, (1981), vol. 15, pages 303 - 310
    - VANDER HEIDEN, M. G.; CHANDEL, N. S.; WILLIAMSON, E. K.; SCHUMACKER, P. T.; THOMPSON, C. B., "Bel-xL regulates the membrane potential and volume homeostasis of mitochondria", CELL, (1997), vol. 91, pages 627 - 637
    - VANDER HEIDEN, M. G.; PLAS, D. R.; RATHMELL, J. C.; FOX, C. J.; HARRIS, M. H.; THOMPSON, C. B., "Growth factors can influence cell growth and survival through effects on glucose metabolism", MOL CELL BIOL, (2001), vol. 21, pages 5899 - 5912
    - WATSON, J. A.; LOWENSTEIN, J. M., "Citrate and the conversion of carbohydrate into fat. Fatty acid synthesis by a combination of cytoplasm and mitochondria", J BIOL CHEM, (1970), vol. 245, pages 5993 - 6002
The EPO accepts no responsibility for the accuracy of data originating from other authorities; in particular, it does not guarantee that it is complete, up to date or fit for specific purposes.