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Title:
TARGETING PRODRUGS AND COMPOSITIONS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES
Document Type and Number:
WIPO Patent Application WO/2010/072734
Kind Code:
A3
Abstract:
Provided herein are compounds of formula (I) as well as compounds of formula (I) which are prodrugs in which the (R7)a-phenyl-S(O)2NH group represents a sulphonamide-bond compound, compositions and methods for preventing or treating gastrointestinal diseases such as inflammatory bowel disease and colorectal cancer, wherein the method comprises delivering an effective amount of a COX-2 or a similar sulphonamide inhibitor as a prodrug or a derivative thereof to the colon, wherein the COX-2 or similar inhibitor is released in vivo.

Inventors:
GILMER JOHN FRANCIS (IE)
RUIZ JUAN FRANCISCO MARQUEZ (ES)
KELLEHER DERMOT (IE)
Application Number:
PCT/EP2009/067689
Publication Date:
August 19, 2010
Filing Date:
December 21, 2009
Export Citation:
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Assignee:
TRINITY COLLEGE DUBLIN (IE)
GILMER JOHN FRANCIS (IE)
RUIZ JUAN FRANCISCO MARQUEZ (ES)
KELLEHER DERMOT (IE)
International Classes:
C07C311/51; A61K31/18; A61K31/415; A61P29/00; A61P35/00; C07D231/12
Domestic Patent References:
WO2009003970A12009-01-08
Foreign References:
JPH07120877A1995-05-12
Other References:
V.R. SINHA, ET AL.: "Colonic drug delivery: prodrug approach", PHARMACEUTICAL RESEARCH, vol. 18, no. 5, May 2001 (2001-05-01), SPRINGER, NEW YORK, NY, US, pages 557 - 564, XP002501855, ISSN: 0724-8741
V. HAGEN, ET AL.: "Quantitative Struktur-Wirkungs-Beziehungen bei antikonvulsiv wirksamen Benzensulfonamiden", DIE PHARMAZIE, vol. 35, no. 3, March 1980 (1980-03-01), GOVI VERLAG PHARMAZEUTISCHER VERLAG, pages 183 - 185, XP001249175, ISSN: 0031-7144
G.M. BLACKBURN, ET AL.: "Synthesis of [alpha]-fluoro- and [alpha],[alpha]-difluoro- benzenemethanesulphonamides: New inhibitors of carbonic anhydrase", ORGANIC AND BIOMOLECULAR CHEMISTRY, vol. 3, no. 2, 21 January 2005 (2005-01-21), ROYAL SOCIETY OF CHEMISTRY LETCHWORTH, GB, pages 225 - 226, XP002580730, ISSN: 1477-0520
Attorney, Agent or Firm:
EARNSHAW, Mark (Scotland House165-169 Scotland Street, Glasgow Strathclyde G5 8PL, GB)
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