AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX
    1.
    发明申请
    AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX 审中-公开
    AMPHOTERICIN B衍生物与改进的治疗指数

    公开(公告)号:US20160215012A1

    公开(公告)日:2016-07-28

    申请号:US15026520

    申请日:2014-10-06

    IPC分类号: C07H17/08 A01N43/90

    CPC分类号: C07H17/08 A01N43/90

    摘要: Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3′ or C4′ modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

    摘要翻译: 提供两性霉素B(AmB)的某些衍生物,其特征在于毒性降低并保留抗真菌活性。 某些衍生物是AmB的C16脲衍生物。 某些衍生物是AmB的C3,C5,C8,C9,C11,C13或C15脱氧衍生物。 某些衍生物包括AmB的霉菌素附属物的C3'或C4'修饰物。 还提供了制备本发明的AmB衍生物的方法,包含本发明的AmB衍生物的药物组合物和本发明的AmB衍生物的使用方法。