| 摘要 |
A benzene derivative of the formula (I): <IMG> (I) wherein R1 is hydrogen, C1-6-alkyl, C1-6-haloalkyl, -NH2, -NHR21; R2 is hydroxyl, -OR22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, -NHR23, -N(R24)2, -NH2; R4 is hydrogen, C1-6-alkyl, or -C(=O)R25; R7 is -CO-, -SO2-; R8 is -CO-, single bond; R12 is -R11-R5; R11 is -N(R5)-, -NH-, -O-, -N(R26)-, -N(C(=O)R27)-, -N(C(=O)NH2)-, -N(C(=O)NHR23)-; R13 is hydrogen, C1-6-alkyl, C1-6-haloalkyl, -NHC(=O) (CH2)mC6H5, -NHC(=O)R29, -NHC(=O)CH(C6H5)2, -NH2, -NHR30, -(CH2)nC6H5; Z is C, CH, N; A is CH, N; R5 is hydrogen, -CH2C6H4COOH, -CH2C6H4COOR31, -CH2C6H4OH, -CH2C6H4OR32, -CH2C6H4NH2, -CH2C6H4N(R33)2, -CH2C6H4-azole, -CH2C6H4NHR34, -CH2C6H4C6H4R14; R14 is azole, -COOH; R21 to R34 are independently C1-6-alkyl or C1-6-haloalkyl; m is 0 to 6; n is 0 to 6; t is 0 or 1, with the proviso that when Z is N, R5 is hydrogen, -CH2C6H4COOH, -CH2C6H4COOR31, -CH2C6H4OH, -CH2C6H4OR32, -CH2C6H4NH2, -CH2C6H4N(R33)2, -CH2C6H4-azole, or -CH2C6H4NHR34, or a salt thereof, and a pharmaceutical composition comprising said benzene derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.
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