6,7-Modified paclitaxels.

摘要

The present invention provides paclitaxel derivatives of formula I in which R<1> is -COR in which R is RO- or R; R<2> is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, or a radical of the formula -W-R in which W is a bond, C2-6 alkenediyl, or -(CH2)t-, in which t is one to six; and R is naphthyl, phenyl, or heteroaryl, and furthermore R can be optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups; R is -OCOR, H, OH, -OR, -OSO2R, -OCONRR, -OCONHR, -OCOO(CH2)tR, or -OCOOR; R and R are both hydroxy or together form a bond with the carbon atoms to which they are attached; and R and R are independently C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups. Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.