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    • 4. 发明授权
    • Aminosalicylate derivatives for treatment of inflammatory bowel disease
    • 氨基水杨酸衍生物用于治疗炎性肠病
    • US07157444B2
    • 2007-01-02
    • US10688585
    • 2003-10-18
    • Deanna Jean Nelson
    • Deanna Jean Nelson
    • A61K31/715C07H5/04C07H5/06C07H1/00C08B37/08
    • C07H5/04
    • Therapeutic 5-aminosalicylic acid derivative compositions having general formula (I), wherein R is a 1-deoxy sugar residue or a poly(ethylene glycol) chain-containing residue, are provided. The compositions enable topical delivery of 5-aminosalicylic acid to the gastrointestinal tract following oral administration in pharmaceutical preparations. According to the invention, the compositions stabilize pharmaceutical compositions containing therapeutic 5-aminosalicylic acid derivatives in a manner that enhances the retention of said compositions in the intestine, decreases the cellular absorption thereof, and decreases the transfer of said compositions or the 5-aminosalicylic acid derived therefrom to the systemic circulation
    • 提供具有通式(I)的治疗性5-氨基水杨酸衍生物组合物,其中R为1-脱氧糖残基或含聚乙二醇链的残基。 该组合物能够在药物制剂中口服给药后将5-氨基水杨酸局部递送至胃肠道。 根据本发明,组合物稳定含有治疗性5-氨基水杨酸衍生物的药物组合物,其方法是增强所述组合物在肠中的保留性,降低其细胞吸收,并降低所述组合物或5-氨基水杨酸的转移 从其衍生到体循环