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US 2003/0078428 A1Published application
4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
AssigneeWarner-Lambert Company
InventorsStephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
Life of this patent
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Abstract
Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
Claims32
The compounds are defined by Formula I
- 12
- wherein:
- 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, CO2H or NR10R 11;
- n is 0 to 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- 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-C8 alkyl,
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- alkyl, aryl, aralkyl, or C3-C10 cycloalkyl;
- R7 is hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C10 (cycloalkyl or cycloalkyl optionally containing a heterroatom selected from O, S, or NR9);
- and wherein 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-0 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.
11 more elements
Dependencies are inferred from the claim text.