1094772-18-5Relevant academic research and scientific papers
A class of intestinal lysis type co-drugs and their preparation and use
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, (2022/01/20)
The present invention relates to a class of intestinal cleavage type co-drugs (Codrug) and preparation and use thereof, in particular, the present invention provides a co-drug compound as shown in formula I. The present invention further provides a method
Oxidative cleavage of hydroxamic acid promoted by sodium periodate
Yuan, Changchun,Du, Biao,Xun, Miao-Miao,Liu, Bo
, p. 3622 - 3628 (2017/06/13)
A series of hydroxamic acids, involving aliphatic, aromatic and cyclic substrates, were transformed to the corresponding carboxylic acids through NaIO4-mediated oxidative cleavage in mild conditions. Esterification of these acids with TMSCHN2 could result in formation of the corresponding methyl ester. This methodology makes good compensation for the existing methods transforming amides to esters. Our results also pave the way to harness hydroxamic acids as useful synthetic building blocks.
TARGETING PRODRUGS AND COMPOSITIONS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES
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Page/Page column 24-25, (2010/07/09)
Provided herein are compounds, compositions and methods for preventing or treating gastrointestinal cancer in a mammal, wherein the method comprises delivering an effective amount of a COX-2 or a similar sulfonamide inhibitor as a prodrug or derivative thereof to the colon, wherein the COX-2 or similar inhibitor is released in- vivo.
Design, synthesis, and pharmacological effects of a cyclization-activated steroid prodrug for colon targeting in inflammatory bowel disease
Márquez Ruiz, Juan F.,Radics, Gabor,Windle, Henry,Serra, Hugo O.,Simplício, Ana Luísa,Kedziora, Kinga,Fallon, Padraic G.,Kelleher, Dermot P.,Gilmer, John F.
supporting information; experimental part, p. 3205 - 3211 (2010/03/24)
Glucocorticoids are used in the treatment of inflammatory bowel disease. A limitation to their use is that they undergo absorption from the GIT before reaching the colon causing severe systemic side effects. We report here on a novel prodrug approach to targeting corticosteroids to the colon. The design involves attaching a 21-ester group that suppresses absorption during transit to the colon. The prodrug is designed to be primed by colonic microflora liberating an amino ester that cyclizes releasing the steroid. One of the prodrugs 5b was as efficacious as prednisolone in the murine DSS model but did not cause thymic atrophy, a marker for systemic steroid effects.
TARGETING DIAZO PRODRUGS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES
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Page/Page column 33-34, (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).
