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    • 8. 发明申请
    • Reducing tetracycline resistance in living cells
    • 减少活细胞中四环素的耐药性
    • US20030153537A1
    • 2003-08-14
    • US09504697
    • 2000-02-16
    • Stuart B. Levy
    • A61K031/65A61K031/41
    • C07D295/13A61K31/65C07C237/26C07C323/29C07C2601/08A61K2300/00
    • The present invention provides an improved methodology by which therapeutically to overcome resistance to tetracycline in living cells including bacteria, parasites, fungi, and rickettsiae. The methodology employs a blocking agent such as C5 ester derivatives, or 6-deoxy 13-(substituted mercapto) derivatives of tetracycline, in combination with other tetracycline-type antibiotics as a synergistic combination of compositions to be administered simultaneously, sequentially or concurrently. In another embodiment, certain novel compositions are provided which may be administered alone against, for example, a sensitive or resistant strain of gram positive bacteria such as S. aureus and E. faecalis. The concomitantly administered compositions effectively overcome the tetracycline resistant mechanisms present such that the cell is effectively converted from a tetracycline-resistant state to a tetracycline-sensitive state.
    • 本发明提供了一种改进的方法,其通过其治疗来克服包括细菌,寄生虫,真菌和立克次体在内的活细胞中对四环素的抗性。 该方法采用封闭剂如C5酯衍生物或四环素的6-脱氧13-(取代的巯基)衍生物与其他四环素型抗生素组合,作为同时,顺序或同时施用的组合物的协同组合。 在另一个实施方案中,提供某些新的组合物,其可以针对例如革兰氏阳性细菌如金黄色葡萄球菌和粪肠球菌的敏感或抗性菌株单独施用。 伴随施用的组合物有效克服存在的四环素抗性机制,使得细胞有效地从四环素抗性状态转变为四环素敏感状态。