RAMOT AT TEL-AVIV UNIVERSITY LTD.;TECHNION RESEARCH & DEVELOPMENT FOUNDATION LTD.
发明人:
Itai BENHAR,Nir OSHEROV,Vladimir DERGACHEV,Alex Martin SZPILMAN
申请号：
US15657649
公开号：
US20170319705A1
申请日:
2017.07.24
申请国别(地区):
US
年份:
2017
代理人:
摘要：
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, C1-4 alkyl or phenyl； R2 is (CH2)m wherein m is between 0 and 4； R3 and R4 are each independently H or C1-4 alkyl, R5 is or OH, R6 is selected from a group consisting of: amide and alkyl, and R7 is a water-soluble polymer, and pharmaceutically acceptable salts, solvates, hydrates, diastereomers, and prodrugs of the compound of Formula [I].
