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US 2010/0305148 A1Published application
Di-ester prodrugs of camptothecin, process for their preparation and their therapeutical applications
AssigneeAbraxis BioScience, LLC
InventorsPatrick Soon-Shiong, Neil P. Desai, Chunlin Tao, Cheng Zhi Yu
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Abstract
The present invention is related to 10,20-di-O ester derivatives of camptothecin and pharmaceutical formulations thereof. The compounds and pharmaceutical formulations of the present invention possess increased biological life span and bioavailability and reduced toxicity, while maintaining anti-cancer activity.
Claims13
-54. (canceled)
A di-ester compound having the following structure:
- wherein
- R1, R2, R3, and R4, which can be the same or different, are hydrogen, halogen, C1-C20 alkyl, C1-C8 alkoxyl, C4-C20 aryl or C1-C20 silyl,
- R, which can be the same or different, is C2-C30 alkyl, C2-C22 alkenyl, C4-C30 aryl, (CH2)nOR5, (CH2)nSR5, (CH2)nNR5R6 or (CH2)nCOR7,
- R5 and R6, which can be the same or different, are C1-C8 alkyl or C2-C6 alkenyl,
- R7 is hydroxy, C1-C20 alkyl, C1-C6 alkenyl, C1-C6 alkoxy, C4-C20 aryl, or NR8R9,
- R8 and R9, which can be the same or different, are C1-C6 alkyl,
- and n is an integer of 1 to 8,
- or a pharmaceutically acceptable salt thereof.
5 more elements
Dependencies are inferred from the claim text.