Amphotericin B derivatives with improved therapeutic index

Attorney Docket No. UIX-014.25 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 ofAmB. Certain of the derivatives are C3, C5, C8, C9, C1I, C13, or C15 5 deoxy derivatives...

Full description

Saved in:
Bibliographic Details
Main Authors Davis, Stephen, Uno, Brice E, Knapp, David M, Struble, Justin, Burke, Martin D, Dailey, Ian, Gray, Kaitlyn C, Wang, Pulin, Palyam, Nagarjuna
Format Patent
LanguageEnglish
Published 16.01.2020
Subjects
CHEMISTRY
DERIVATIVES THEREOF
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SUGARS
Online AccessGet full text

Cover

More Information
Summary:Attorney Docket No. UIX-014.25 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 ofAmB. Certain of the derivatives are C3, C5, C8, C9, C1I, C13, or C15 5 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. - 65- Figure 1 HO OH OH OHOHOH HO /'MeO OH OH OH OH O,,,16R OR' 0 Me amphotericin B (AmB) COOH OH 0 Me amphotericin B methyl ester (AmBME) COOMe OH amphoternolide (AmdeB) COOH H 0 Me C2'deoxy amphotericin B (C2'deOAmB) COOH OH
Bibliography:Application Number: AU20190279928