申请人:Sfunga Therapeutics, Inc.
公开号:US10882883B2
公开(公告)日:2021-01-05
Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3′-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2′epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.
本发明公开了两性霉素B(AmB)的衍生物,其特点是与AmB相比,治疗指数有所提高。AmB衍生物包括根据式(I)的C16脲、氨基甲酸酯和酰胺;根据式(II)的C3′-取代的C16脲、氨基甲酸酯和酰胺;根据式(III)的C16酰基;根据式(IV)的C2′-环-C16脲、氨基甲酸酯和酰胺;以及根据式(V)的C16噁唑烷酮衍生物。还公开了包含AmB衍生物的药物组合物,以及使用AmB衍生物的治疗方法。