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Title:
PRODRUG USING NITROIMIDAZOLE
Document Type and Number:
WIPO Patent Application WO/2013/122112
Kind Code:
A1
Abstract:
Provided is a prodrug of a therapeutically active organic compound having: an amino group, a cyclic amino group or a hydroxyl group in the molecule; and a 2-nitro-1-imidazole propionic acid. In particular, provided is a prodrug in which the therapeutic organic compound is selected from an antitumor agent. Said prodrug specifically cleaves at the low-oxygen site within a living body and exhibits an innate therapeutic activity.

Inventors:
NAGASAKI YUKIO (JP)
IKEDA YUTAKA (JP)
HISANO HIKARU (JP)
Application Number:
JP2013/053429
Publication Date:
August 22, 2013
Filing Date:
February 13, 2013
Export Citation:
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Assignee:
UNIVERSITY OF TSUKUBA (1-1-1, Tennodai Tsukuba-sh, Ibaraki 77, 〒3058577, JP)
International Classes:
C07D233/91; A61K31/4168; A61K31/7042; A61K47/48; A61P35/00; A61P43/00; C07D403/06; C07D475/08; C07H15/252; C07H19/06; C07J5/00
Domestic Patent References:
WO2009018163A12009-02-05
WO2000064864A12000-11-02
WO2004087075A22004-10-14
WO2009018163A12009-02-05
Foreign References:
JPH07101860A1995-04-18
JPH0466575A1992-03-02
US3679698A1972-07-25
JP2002543059A2002-12-17
JP2006521409A2006-09-21
JPH07101860A1995-04-18
Other References:
KUMAR, LALIT ET AL.: "Imidazole derivatives as possible microbicides with dual protection", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 45, no. 2, 2010, pages 817 - 824, XP026835712
BONNITCHA, PAUL D. ET AL.: "Nitroimidazole conjugates of bis(thiosemicarbazonato)64Cu (II) - Potential combination agents for the PET imaging of hypoxia", JOURNAL OF INORGANIC BIOCHEMISTRY, vol. 104, no. 2, 2010, pages 126 - 135, XP026808641
LI, ZEJUN ET AL.: "Synthesis and in vitro and in vivo evaluation of three radioiodinated nitroimidazole analogues as tumor hypoxia markers", NUCLEAR MEDICINE AND BIOLOGY, vol. 32, no. 3, 2005, pages 225 - 231, XP027674899
HAY, MICHAEL P. ET AL.: "Hypoxia-selective antitumor agents. 8. Bis(nitroimidazolyl) alkanecarboxamides: a new class of hypoxia- selective cytotoxins and hypoxic cell radiosensitizers", JOURNAL OF MEDICINAL CHEMISTRY, vol. 37, no. 3, 1994, pages 381 - 91, XP002122988
HAY, MICHAEL P. ET AL.: "Nitroimidazole-based 'extruded mustards' designed as reductively activated hypoxia-selective cytotoxins", ANTI- CANCER DRUG DESIGN, vol. LL, no. 5, 1996, pages 383 - 402, XP000909800
MEI, LEI ET AL.: "99mTc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 58, 2012, pages 50 - 63, XP055160634
See also references of EP 2816036A4
B.M SYKE ET AL., J. MED. CHEM., vol. 42, 1999, pages 345 - 355
J. DUAN ET AL., J. MED. CHEM., vol. 51, no. 8, 2008, pages 2412 - 2420
M.P. HAY ET AL., J. MED. CHEM., vol. 37, 1994, pages 381 - 391
Attorney, Agent or Firm:
PATENT PROFESSION CORPORATION ODAJIMA PATENT OFFICE (Nippon Jitensha Bldg, 9-15 Akasaka 1-chome, Minato-k, Tokyo 52, 〒1070052, JP)
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Claims: