Rapamycin carbohydrate derivatives
OwnerMark Abel, Roman Szweda +3inventors
InventorsMark Abel, Roman Szweda, Daniel Trepaier, Randall Yatscoff, Robert Foster
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Abstract
This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.
Claims21
1-24. (canceled)
A medical device comprising a rapamycin carbohydrate derivative having the structure of formula (I):
- wherein R1 and R2 are independently hydrogen or —X-Z;
- wherein n=0 or 1;
- and
- wherein each X is a linker selected from the group consisting of —C(O)— and —SO2—;
- wherein each Z is a carbohydrate moiety selected from the group consisting of fructose, fucitol and allose;
- wherein Z is attached to X through a hydroxyl oxygen atom of Z;
- with the proviso that R1 and R2 are not both hydrogen.
Dependencies are inferred from the claim text.