New epothilone derivatives, useful for treating malignant tumors such as ovarian, stomach, colon, breast and lung carcinoma, acute lymphocytic and myelocytic leukemia and chronic inflammatory diseases such as psoriasis

摘要

Epothilone derivatives (I) and their stereoisomers and mixtures are new Epothilone derivatives of formula (I) and their stereoisomers and mixtures are new. R4, R5 = H, 1-10C alkyl, aryl or 7-20C aralkyl; R6, R7 = H; or R6+R7 = a bond or O; R8 = Me or H; (i) R1a+R1b = trimethylene; R2 = phenyl or benzyl; and X = 2-pyridyl, 2-methyl-4-thiazolyl or 2-methyl-4-oxazolyl; (ii) R1a+R1b = trimethylene; R2 = Me, Et, or Pr; and X = 2-pyridyl, 2-methyl-4-thiazolyl or 2-methyl-4-oxazolyl; or (iii) R1a, R1b = Me; R2 = Me, Et, or Pr; and X = 2-pyridyl, 2-methyl-4-thiazolyl or 2-methyl-4-oxazolyl; the N and/or S in X may be in the oxidized form; provided that when R2 and R8 are Me, then X can only be a 2-pyridyl having an optionally oxidized N.