EPOTHILONE DERIVATIVES

摘要

The present invention relates to compounds of the formula Q is selected from the group consisting of G is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo, W is O or NR₁₅; X is O or H,H; Y is selected from the group consisting of O; H,OR₁₆; OR₁₇,OR₁₇; NOR₁₈; H,NOR₁₉; H,NR₂₀R₂₁; H,H; or CHR₂₂; OR₁₇OR₁₇ can be a cyclic ketal; Z₁ and Z₂ are selected from the group consisting of CH₂, O, NR₂₃, S, or SO₂, wherein only one of Z and Z₂ is a heteroatom; B₁ and B₂ are selected from the group consisting of OR₂₄, or OCOR₂₅, or O₂CNR₂₆R₂₇; when B₁ is H and Y is OH, H they can form a six-membered ring ketal or acetal; D is selected from the group consisting of NR₂₈R₂₉, NR₃₀COR₃₁ or saturated heterocycle; R₁, R₂, R₃, R₄, R₅, R₆, R₇, R₁₃, R₁₄, R₁₈, R₁₉, R₂₀, R₂₁, R₂₂, R₂₆, and R₂₇ are selected from the group H, alkyl, substituted alkyl, or aryl and when R₁ and R₂ are alkyl can be joined to form a cycloalkyl; R₃ and R₄ are alkyl can be joined to form a cycloalkyl; R₉, R₁₀, R₁₆, R₁₇, R₂₄, R₂₅, and R₃₁ are selected from the group H, alkyl, or substituted alkyl; R₈, R₁₁, R₁₂, R₂₈, R₃₀, R₃₂, R₃₃, and R₃₀ are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; R₁₅, R₂₃ and R₂₉ are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R₃₂C-O, R₃₃SO₂, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds wherein W and X are both O; and R₁, R₂, R₇, are H; and R₃, R₄, R₆, are methyl; and R₈, is H or methyl; and Z₁, and Z₂, are CH₂; and G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; and Q is as defined above are excluded.