Aromatic carboxylic acid derivatives for treatment and prophylaxis of gastrointestinal diseases including colon cancers

摘要

Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

主权项

1. A method of treating gastrointestinal disorders, comprising administering to a patient in need of treatment or prevention thereof an effective amount of a compound selected from the group consisting of: wherein: R is selected from the group consisting of —OH, —HNCH2CH2SO3H, —HNCH2CH2SO2N3, —HNCH2CH2SO2NHR6, —HNCH2CO2H, and —HNCH(CO2H)CH2COOH, and analogs thereof wherein any one or more sulfonic acid group (—SO3H) in the compound is replaced with an —SO2N3 or —SO2NHR6 group, where R6 is H or C1-8 alkyl, and pharmaceutically acceptable salts and esters of such compounds and analogs wherein the gastrointestinal disorder is colon cancer, Crohn's disease, or ulcerative colitis.