USE OF EPOTHLONE DERIVATIVES FOR PREPARATION OF PHARMACEUTICAL COMPOSITION SUITABLE FOR TREATMENT OF REFRACTORY TUMORS

摘要

The present invention relates to the use of epothilone derivatives of the general formula wherein B1, B2, G, Q, X, Y, Z1, Z2 and R1-R7 are various simple or complex organic groups as defined below for the manufacture of a medicament for the treatment of macular tumors. Q is selected from the group consisting of; G is selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, heterocyclic, and groups; W is O or R15N; X is oxygen or hydrogen and hydrogen Y is oxygen, hydrogen and R16O; R17O and R17O; R18ON and hydrogen; hydrogen and R20R21N; hydrogen and hydrogen; R22HC = selected from the group consisting of R17O and R17O may be a cyclic ketal; Z1 and Z2 are independently selected from the group consisting of methylene, oxygen, R23N-, sulfur, and -SO2-, wherein only one of Z1 and Z2 can be a heteroatom; B1 and B2 are independently selected from R24O, R25OCO and R27R26N- (O =) C-O, and when B1 is hydrogen and Y is hydroxy and hydrogen, they may form a 6-membered ketal or acetal ring; D is selected from the group consisting of R28R29N, R31OCR30N and saturated heterocyclic; R1, R2, R3, R4, R5, R6, R7, R13, R14, R18, R19, R20, R21, R22, R26 and R27 are independently selected from hydrogen, alkyl, substituted alkyl and aryl, and if R1 and R2 is alkyl, they may be attached to form a cycloalkyl group, and when R3 and R4 are alkyl, they may be attached to form a cycloalkyl group. SHE