| abstract |
The present invention provides paclitaxel derivatives of formula I (see fig. I) in which R1 is -COR z in which R z is RO- or R; R2 is C1-6 alkyl, C2-6 alkenyl, C-26 alkynyl, C3-6 cycloalkyl, or a radical of the formula -W-R x in which W is a bond, C2-6 alkenediyl, or -(CH2)t-, in which t is one to six; and R x is naphthyl, phenyl, or heteroaryl, and furthermore R x can be optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups; R a is OCOR, H, OH, -OR, -OSO2R, -OCONR o R, -OCONHR, -OCOO(CH2)t R, or -OCOOR; R b and R c are both hydroxy or together form a bond with the carbon atoms to which they are attached; and R and R o 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. |