abstract |
These compounds are useful as inhibitors of p38 kinase and in the preparation of drugs for the treatment of related diseases. Claim 1: A bicyclic compound characterized by the general formula (1), wherein A represents CR1R2 or NR3; R1 and R2 independently represent C1-4 alkyl; R3 represents - (CH2) P-Cy1, or C1-6 alkyl optionally substituted by one or more R7; m represents 1 or 2; R4 represents -B-R8; R5 represents hydrogen, C1-4 alkyl, halogen or C1-4 alkoxy; R6 may be attached to any available carbon atom of the phenyl ring and represents halogen or methyl; n represents 0 or 1; B represents -CONR9-, -NR9CO- or -NR9CONR9-; R7 represents hydroxy, C1-4 alkoxy, halogen, -NR10R10 or phenyl optionally substituted by one or more groups selected from C1-4 alkyl, halogen, C1-4 alkoxy, C1-4 haloalkyl and C1-4 haloalkoxy, and additionally two R7 groups on the same carbon atom can be attached forming a group - (CH2) q-; R8 represents C1-6 alkyl or - (CH2) P-Cy2; p represents 0, 1 or 2; q represents 2, 3, 4, 5 or 6; Cy1 represents phenyl, heteroaryl, C3-7 cycloalkyl or heterocyclyl, which may all be optionally substituted by one or more R11; Cy2 represents phenyl, heteroaryl or C3-7 cycloalkyl, which may all be optionally substituted by one or more R12; R9 and R10 independently represent hydrogen or C1-4 alkyl; R11 represents halogen, R13, -OR13 ', -NO2, -CN, -COR13', - CO2R13 ', -CONR14R14', -NR14'14 ', -NR14'-COR13', -NR14'-CONR14'R14 ', -NR14'CO2R13, -NR14'SO2R13, -SR13 ', -SOR13, -SO2R13, -SO2NR14'R14', or Cy3; R12 represents C1-4 alkyl, halogen, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, or Cy3; R13 represents C1-4 alkyl, C1-4 haloalkyl or C1-4 hydroxyalkyl; R13 'represents hydrogen or R13; R14 represents C1-4 alkyl or C1-4 hydroxyalkyl; R14 'represents hydrogen or R14'; Cy3 represents phenyl, heteroaryl, C3-7 cycloalkyl or heterocyclyl, which may all be optionally substituted by one or more groups selected from C1-4 alkyl, halogen, C1-4 alkoxy, C1-4 haloalkyl and C1-4 haloalkoxy; R15 represents hydrogen, R16, -COR17, -CONHR17, -SO2R17 or -COOR17; R16 represents C1-6 alkyl optionally substituted by one or more groups selected from halogen, -OR13 ', -NO2, -CN, -COR13', -CO2R13 ', -CONR14'R14', -NR18R18, -NR14'COR13 ' , -NR14'CONR14'R14 ', -NR14'CO2R13, -NR14'SO2R13, -SR13', -SOR13, - SO2R13, -SO2NR14'R14 'and Cy4; R17 represents R16 or Cy4; R18 represents hydrogen, C1-4 alkyl, C1-4 hydroxyalkyl or C1-4 alkoxy-C1-4 alkyl; Cy4 represents phenyl, heteroaryl, C3-7 cycloalkyl or heterocyclyl, which may all be optionally substituted by one or more groups selected from C1-4 alkyl, halogen, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, hydroxy , C1-4 hydroxyalkyl and -NR19R19; and R19 represents hydrogen or C1-4 alkyl; or a salt thereof. |