6,7-epoxy paclitaxels

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 493/04 (2006.01) A61K 31/33 (2006.01) C07D 493/08 (2006.01)

Patent

CA 2143013

The present invention provides paclitaxel derivatives of formula I Image I in which R1 is -CORz, in which Rz is RR°N-, RHN-, RO- or R; R2 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, or a radical of the formula -W-Rx in which W is a bond, C2-6 alkenediyl, or -(CH2)t-, in which t is one to six; and Rx is naphthyl, phenyl, or heteroaryl, and furthermore Rx can be optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups; 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.

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