| 摘要 |
Phenylamino benzhydroxamic acid derivatives of formula (I) wherein: R1 is hydrogen, C1-8 alkyl, C1-8 alkoxy, halo, trifluoromethyl or CN R2 is hydrogen R3, R4 and R5 are hydrogen, hydroxy, halo, trifluoromethyl, C1-8 alkyl, C1-8 alkoxy, nitro, CN, or (O or NH)m-(CH2)n-R9 where R9 is hydrogen, hydroxy, CO2H or NH10R11 n is 0 to 4 m is 0 or 1 R10 and R11 are hydrogen or C1-8 alkyl or taken together with the nitrogen to which they are attached can complete a 3 to 10 member cyclic ring optionally containing one, two or three additional heteroatoms selected from O, S, NH or N-C1-C8 alkyl. R6 is hydrogen, C1-8 alkyl, C(O)-C1-C8 alkyl, aryl, aralkyl or C3-10 cycloalkyl R7 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 alkyl (cycloalkyl or cycloalkyl optionally containing a heteroatom selected from O, S or NR9). Any of the foregoing alkyl, alkenyl and alkynyl groups can be unsubstituted or substituted by cycloalkyl (or cycloalkyl optionally containing a heteroatom selected from O, S or NR9), aryl, aryloxy, heteroaryl, or heteroaryloxy, or R6 and R7 taken together with the N-O to which they are attached can complete a 5 to 10 membered cyclic ring, optionally containing one, two or three additional heteroatoms selected from O, S, or NR10R11. Such derivatives are potent inhibitors of MEK and are effective in treating cancer, proliferative diseases such as psoriasis and restenosis, heart failure, stroke, hepatomegaly, diabetes and Alzheimer's disease.
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