R¹ is -COR z in which R z is RO- or R; R g is C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ 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; R² is -OCOR, H, OH, -OR, -OSO₂R, -OCONR o R, -OCONHR, -OCOO(CH₂) t R, or -OCOOR; 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.
Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.
摘要:
The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.
摘要:
This invention relates to a fluorinated taxol of formula I
in which
R¹ is -COR z in which R z is RO- or R; R g is C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ 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, furyl, thienyl or phenyl, 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; R² is -OCOR, H, OH, -OR, -OSO₂R, -OCONR o R, -OCONHR, -OCOO(CH₂) t R, or -OCOOR; 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. Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.
摘要:
The present invention concerns novel water-soluble phosphonooxymethyl ethers of taxane derivatives, their use as antitumor agents, and pharmaceutical compositions containing the novel compounds.
摘要:
in which R¹ is -COR z in which R z is RO- or R; R g is C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ 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; R² is -OCOR, H, OH, -OR, -OSO₂R, -OCONR o R, -OCONHR, -OCOO(CH₂) t R, or -OCOOR; 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. Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.