Technion Research & Development Foundation Ltd

Tel Aviv University

Nir Osherov

Itai Benhar

Alex Martin Szpilman

Vladimir Dergachev

Embodiments of the invention provide derivatives of Amphotericin B having increased solubility and reduced toxicity relative to AMB, while retaining antifungal activity against multiple clinical fungal isolates. Derivatives of AMB are provided comprising a polymer group having an amine group, the polymer linked to mycosamine via a relatively stable linker such as an amide linker. The derivatives may be of the general formula [I]: wherein R is H, Calkyl or phenyl; Ris (CH)wherein m is between 0 and 4; Rand Rare each independently H or Calkyl, Ris or OH, Ris selected from a group consisting of: amide and alkyl, and Ris a water-soluble polymer, and pharmaceutically acceptable salts, solvates, hydrates, diastereomers, and prodrugs of the compound of Formula [I].

Amphotericin B derivatives

Embodiments of the invention provide derivatives of Amphotericin B having increased solubility and reduced toxicity relative to AMB, while retaining antifungal activity against multiple clinical fungal isolates. Derivatives of AMB are provided comprising a polymer group having an amine group, the polymer linked to mycosamine via a relatively stable linker such as an amide linker. The derivatives may be of the general formula [I]: wherein R is H, Calkyl or phenyl; Ris (CH)wherein m is between 0 and 4; Rand Rare each independently H or Calkyl, Ris H or OH, Ris selected from a group consisting of: amide and alkyl, and Ris a water-soluble polymer, and pharmaceutically acceptable salts, solvates, hydrates, diastereomers, and prodrugs of the compound of Formula [I].

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Nir Osherov