155388-63-9Relevant articles and documents
BIFUNCTIONAL COMPOUNDS AND USE FOR REDUCING URIC ACID LEVELS
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Paragraph 00185, (2015/09/22)
Bifunctional compounds that increase uric acid excretion and reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders of uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are provided. Pharmaceutical compositions comprising the bifunctional compounds are also provided.
Azo-reductase activated budesodine prodrugs for colon targeting
Marquez Ruiz, Juan F.,Kedziora, Kinga,O'Reilly, Mary,Maguire, Jacqueline,Keogh, Brian,Windle, Henry,Kelleher, Dermot P.,Gilmer, John F.
, p. 7573 - 7577 (2013/02/23)
Budesodine is a synthetic glurocorticoid that undergoes substantial first pass metabolism, limiting systemic exposure. Its use in treatment of inflammatory bowel disease would benefit from a targeting strategy that could lead to a local topical effect, improving safety and increasing anti-inflammatory efficacy. A two-step prodrug strategy involving azoreduction/cyclization that we developed previously for prednisolone is here applied with some variations to budesonide. The budesodine prodrugs were tested using an in vitro azoreductase assay simulating human colonic microflora. The kinetics of amino steroid ester cyclization and its pH dependence was also evaluated. The stability of the prodrugs systems in simulated human duodenal and gastric fluid was evaluated to determine the likelihood of intact intestinal transit. The propionic acid derived prodrug 3 undergoes rapid activation by Clostridium perfingens and its putative reduction product cyclizes with acceptable rapidity when synthesized independently. These properties of 3 suggest that it has potential in management of ulcerative colitis.
TARGETING DIAZO PRODRUGS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES
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Page/Page column 29; 33-35, (2009/03/07)
Provided herein are compounds, compositions and methods for decreasing NFkB DNA-binding activity in a patient comprising administering of a therapeutically effective amount of a compound or composition of the application to the patient to reduce, alleviate or treat various gastrointestinal diseases, such as inflammatory bowel disease (IBD).