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US 8,569,466 B2Granted
Aromatic carboxylic acid derivatives for treatment and prophylaxis of gastrointestinal diseases including colon cancers
OwnerNnochiri Ekwuribeinventor
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Abstract
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.
Claims4
A compound of one of the formulas:
- wherein:
- R is selected from the group consisting of —OH, —HNCH2CH2SO3H, —HNCH2CH2SO2N3, —HNCH2CH2SO2NHR6, —HNCH2CO2H and —HNCH(CO2H)CH2COOH;
- Z is selected from the group consisting of H, C1-6 alkyl (including cycloalkyl), alkenyl, heterocyclyl, aryl, heteroaryl, F, Cl, Br, I, —OR′, —NR′R″, —CF3, —CN, —NO2, —C2R′, —SR', —N3, —C(═O)NR′R″, —NR′C(═O)R″, —C(═O)R′, —C(═O)OR′, —OC(═O)R′, —OC(═O)NR′R″, —NR′C(═O)O R″, —SO2R′, —SO2NR′R″, and —NR′SO2R″,
- R′ and R″ are individually hydrogen, C1-6 alkyl, cycloalkyl, heterocyclyl, aryl, or arylalkyl;
- J is selected from the group consisting of —SO3H, SO2N3, SO2NHR6, and CO2H;
- and
- R6 is H or C1-8 alkyl,
- and pharmaceutically acceptable salts and esters thereof.
5 more elements
A compound is presented by the formula:
Dependencies are inferred from the claim text.