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COMPOSITIONS OF HYDROPHOBIC DERIVATIVES OF TAXANA AND THEIR APPLICATION

机译:塔克萨纳州疏水衍生物的组成及其应用

摘要

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�
机译:1.包含纳米颗粒的组合物,其中所述纳米颗粒包含紫杉烷的疏水性衍生物和载体蛋白。 ! 2.根据权利要求1的组合物,其中紫杉烷的疏水衍生物是紫杉烷的前药。 ! 3.根据权利要求1或2的组合物,其中所述载体蛋白是白蛋白。 ! 4.根据权利要求3的组合物,其中白蛋白是人血清白蛋白。 ! 5.根据权利要求1所述的组合物,其中所述组合物包含纳米颗粒形式和非纳米颗粒形式的载体蛋白,并且其中少于约25%的载体蛋白为纳米颗粒形式。 ! 6.根据权利要求1的组合物,其中所述组合物中纳米颗粒的平均直径约小于200nm。 ! 7.根据权利要求1的组合物,其中所述组合物中纳米颗粒的平均直径约小于100nm。 ! 8.根据权利要求1的组合物,其中组合物中超过80%的纳米颗粒具有约小于100nm的直径。 ! 9.根据权利要求1的组合物,其中组合物中多于90%的纳米颗粒具有约小于100nm的直径。 ! 10.根据权利要求1的组合物,其中紫杉烷的疏水衍生物是下式的化合物: !其中R1代表苯基或-OtBu; ! R2,R3,R4和R5独立地代表H或疏水基团; !并且R2,R3,R4和R5中至少一个不是H时; !前提是当R1是苯基并且R2,R3和R5各自是H时,则R4不是酰基。 !或其药学上可接受的盐,异构体或溶剂化物。 ! 11.根据权利要求10所述的组合物,其中所述疏水基团为-C(O)R 6;和!每个R 6独立地表示选自烷基,烯基,炔基,环烷基,环烷基烷基,芳基的取代或未取代的基团。

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