AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX

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 derivativ...

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Bibliographische Detailangaben
Hauptverfasser: Davis, Stephen, Uno, Brice E, Knapp, David M, Struble, Justin, Burke, Martin D, Dailey, Ian, Gray, Kaitlyn C, Wang, Pulin, Palyam, Nagarjuna
Format: Patent
Sprache:eng
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Zusammenfassung: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.