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COMPOSITIONS OF HYDROPHOBIC DERIVATIVES OF TAXANA AND THEIR APPLICATION
COMPOSITIONS OF HYDROPHOBIC DERIVATIVES OF TAXANA AND THEIR APPLICATION
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机译:塔克萨纳州疏水衍生物的组成及其应用
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1. The composition containing nanoparticles, in which the nanoparticles contain a hydrophobic derivative of taxane and a carrier protein. ! 2. The composition according to claim 1, where the hydrophobic derivative of a taxane is a prodrug of a taxane. ! 3. The composition according to claim 1 or 2, where the carrier protein is albumin. ! 4. The composition according to claim 3, where the albumin is human serum albumin. ! 5. The composition according to claim 1, where the composition contains a carrier protein both in the form of nanoparticles and in the form of non-nanoparticles, and where about less than 25% of the carrier protein is in the form of nanoparticles. ! 6. The composition according to claim 1, where the average diameter of the nanoparticles in the composition is approximately less than 200 nm. ! 7. The composition according to claim 1, where the average diameter of the nanoparticles in the composition is approximately less than 100 nm. ! 8. The composition according to claim 1, where more than 80% of the nanoparticles in the composition have a diameter of approximately less than 100 nm. ! 9. The composition according to claim 1, where more than 90% of the nanoparticles in the composition have a diameter of approximately less than 100 nm. ! 10. The composition according to claim 1, where the hydrophobic derivative of taxane is a compound of the formula:! ! where R1 represents phenyl or -OtBu; ! R2, R3, R4 and R5 independently represent H or a hydrophobic group; ! and where at least one of R2, R3, R4 and R5 is not H; ! with the proviso that when R1 is phenyl and R2, R3 and R5 are each H, then R4 is not an acyl group; ! or a pharmaceutically acceptable salt, isomer or solvate thereof. ! 11. The composition of claim 10, where the hydrophobic group is —C (O) R6; and! each R6 independently represents a substituted or unsubstituted group selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl alkyl, aryl, get�
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