7,8-cyclopropataxanes

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 305/14 (2006.01) A61K 31/335 (2006.01) A61K 31/38 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2099211

ABSTRACT An antitumor compound of formula I Image 1 in which R1 is -CORz in which Rz is t-butyloxy, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, or phenyl, optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups; 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, furyl, thienyl or phenyl, and furthermore Rx can be optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups; R3 is -OCOR, -OCOOR, H, or OH; R4 is hydrogen; or R3 and R4 jointly form a carbonyl group; and R is C1-6 alkyl. 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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