首页> 外国专利> USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT.

USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT.

机译:细胞特异性缀合物用于治疗胃肠道炎的疾病。

摘要

The present invention is directed to methods for the prevention and treatment ofinflammatory diseases, disorders, and conditions of gastrointestinal tract byadministering to a patient in need of such treatment, conjugate compounds ofFormula (VII) having low oral ibioavailability, or pharmaceutically acceptablesalts, prodrugs, or solvate thereof: wherein M represents a macrolide subunitpossessing the property of accumulation in inflammatory cells, T represents ananti-inflammatory subunit that can be a steroid or nonsteroid (nonsteroidal moiety)derived from a non-steroid drug with anti iinflammatory, analgesic and/orantipyretic activity (NSAID) and L represents a linker covalently linking Mand T. The present disclosure is also directed to pharmaceutical compositions containingconjugate compounds of Formula (VII) having low oral-bioavailability.
机译:本发明涉及预防和治疗炎症性疾病,病症和胃肠道疾病的方法,其通过向需要这种治疗的患者给药具有低口服生物利用度的式(VII)的缀合物或药学上可接受的盐,前药或其溶剂化物:其中M代表具有在炎性细胞中积累性质的大环内酯亚单位,T代表抗炎亚单位,其可以是源自具有抗炎,镇痛和/或解热活性的非甾体药物的甾体或非甾体(非甾体部分)。 (NSAID)和L表示共价连接Mand T的连接基。本发明还涉及包含具有低口服生物利用度的式(VII)的缀合物的药物组合物。

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