| 摘要 |
An anticancer combination which comprises a mitotic inhibitor (such as paclitaxel, docetaxel, vincristine, vinblastine, vinorelbine, and vinflunine) and a MEK inhibitor for treating cancer. The MEK inhibitor is a phenyl amine compound of Formula I where: R1 is hydrogen, hydroxy, C1-C8 alkyl, C1-C8 alkoxy, halo, trifluoromethyl, or CN; R2 is hydrogen; R3, R4, and R5 independently are hydrogen, hydroxy, halo, trifluoromethyl, C1-C8 alkyl, C1-C8 alkoxy, nitro, CN, or -(O or NH)m- (CH2)n-R9, where R9 is hydrogen, hydroxy, COOH, or NR10R11 ; n is 0-4; m is 0 or 1; R10 and R11 independently are hydrogen or C1-C8 alkyl, or taken together with the nitrogen to which they are attached can complete a 3-10 member cyclic ring optionally containing 1,2, or 3 additional heteroatoms selected from O, S, NH, or N-C1-C8 alkyl; Z is COOR7, tetrazolyl,CONR6R7, CONHNR10R11, or CH2OR7; R6 and R7 independently are hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, (CO)-C1-C8 alkyl, aryl, heteroaryl, or C3-C10(cycloalkyl optionally containing 1, 2, or 3 heteroatoms selected from O, S, NH, or N alkyl); and where any of the foregoing alkyl, alkenyl, aryl, heteroaryl, heterocyclic and alkynyl groups can be unsubstituted or substituted by halo, hydroxy, C1-6 alkoxy, amino, nitro, C1-4 alkylamino, di(C1-4)alkylamino, C3-6 cycloalkyl, phenyl, phenoxy, C3-5 heteroaryl or heterocyclic radical, or C3-5 heteroaryloxy or heterocyclic radical-oxy. The MEK inhibitor may also be the compound 2- (2-amino-3-methoxyphenyl)-4-oxo-4H-[l](2-amino-3-methoxyphenyl)-4-oxo-4H-[l] benzopyran.
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