| 摘要 |
The present invention relates to compound of general formula (1) wherein R1 represents C6-C10 aryl comprising one or two fused rings, wherein from 2 to 5 carbon atoms may be replaced with a heteroatom selected from O, S and NR6, and eventually substituted with from 5 to 11 substituents selected from R6, halo, CN, NO2, CF3, OCF3, COOR6, OCOR6, SO2NR6R7, CONR6R7, NR6R7, NR6COR7, (CH2)p—NR6R7, (CH2)p—OR6 and (CH2)pSR6, as well as, if appropriate, their pharmaceutically acceptable salts and/or isomers, tautomers, solvates or isotopic variations thereof. The compounds are useful for the treatment of cancers.; |
| 主权项 |
1. A compound of general formula (1)wherein
Q1 to Q5 are identical or different and represent CR6, R1 represents C6-C10 aryl comprising one or two fused rings, wherein from 2 to 5 carbon atoms may be replaced with a heteroatom selected from O, S, N and NR6, and may be substituted with from 5 to 11 substituents selected from R6, halo, CN, NO2, CF3, OCF3, COOR6, OCOR6, SO2NR6R7, CONR6R7, NR6R7, NR6COR7, (CH2)p—NR6R7, (CH2)p—OR6 and (CH2)pSR6, R2 is SO2R1 or R6, R3 and R4 are identical or different and are selected from COR8 and R5 represents R6, aryl, OR6, SR6, halo, CN, NO2, CF3, OCF3, COOR6, SO2NR6R7, CONR6R7, NR6R7 or NHCOR6, R6 and R7 are identical or different and represent H or alkyl, R8 is selected from H, alkyl, cycloalkyl, aryl, and alkylaryl, wherein aryl may be substituted with from one to four R5 substituents which are identical or different, or R8 represents —(CH2)q—NR6R7, wherein p represents an integer from 0 to 6, and q represents an integer from 0 to 6, and wherein the thiazolyl group is linked to the 6-membered group in meta or para position with respect to the sulfonamide group, and wherein the thiazolyl group is linked to the 6-membered group in position α or β with respect to the S atom,and pharmaceutically acceptable salts and/or isomers, tautomers, solvates or isotopic variations thereof;with the exclusion of the following compounds:
N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-2-hydroxy-benzamide, 2-(acetyloxy)-N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-benzamide, 3-chloro-N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-benzamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-1-hydroxy-2-naphtalenecarboxamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-3-hydroxy-2-naphtalenecarboxamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-2-methoxy-benzamide, N-[3-(2-amino-4-thiazolyl)phenyl]-4-chloro-benzenesulfonamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-benzamide, 2-chloro-N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-benzamide, 4-chloro-N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-benzamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-3,4-dimethoxy benzamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-3-methoxy benzamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-4-methoxy benzamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-3-methyl-benzamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-4-methyl-benzamide, N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-4-nitro-benzamide, and N-[4-[3-[[(4-chlorophenyl)sulfonyl]amino]phenyl]-2-thiazolyl]-4-methyl-benzamide. |
