155388-93-5Relevant articles and documents
4-substituted pyridine-2-formamide compound, preparation method thereof and application
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Paragraph 0059-0063, (2018/03/28)
The invention discloses a 4-substituted pyridine-2-formamide compound, a preparation method thereof and an application. The 4-substituted pyridine-2-formamide compound has a structure as shown in a formula I, and the chemical name of the compound is 4-{4-[3-(4-chlorine-3-trifluoromethyl-phenyl)-ureide]-3-carboxyl phenoxy}-N-picoline-2-carboxylic methylamine. According to the preparation method of the 4-substituted pyridine-2-formamide compound, 4-chlorine-2-picolinic acid serves as an initial raw material, and the compound in the formula I is prepared by acylating chlorination, amination, substitution reaction and condensation reaction. The 4-substituted pyridine-2-formamide compound retains a Sorafenib efficacy structure, 5-aminosalicylic acid or aminosalicylic acid ester achieving a positive pharmacological function in the metabolic process replaces p-aminophenol with large toxic and side effects, efficacy can be improved, and the toxic and side effects are reduced.
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.