Patent ID: 6130239
Filing Date: 2000-10-10
Classification: A61P,C07D

Abstract:
A compound having the formula: ##STR204## and the pharmaceutically acceptable salts thereof, wherein: R.sup.1 is selected from the group consisting of--H,--COR.sup.4,--COOR.sup.4,--CONR.sup.6 R.sup.7,lower alkyl which optionally may be substituted from the group consisting of --OR.sup.5, --NR.sup.6 R.sup.7, cycloalkyl, heterocycle, --COR.sup.4, --COOR.sup.4, --CONR.sup.6 R.sup.7, --CN, --NO.sub.2, --SO.sub.2 R.sup.4, halogen, and --SO.sub.2 NR.sup.6 R.sup.7,cycloalkyl which optionally may be substituted from the group consisting of --OR.sup.5, --NR.sup.6 R.sup.7, lower alkyl, heterocycle, --COR.sup.4, --COOR.sup.4, --CONR.sup.6 R.sup.7, --CN, --NO.sub.2, --SO.sub.2 R.sup.4, halogen, and --SO.sub.2 NR.sup.6 R.sup.7,heterocycle which optionally may be substituted from the group consisting of --OR.sup.5, --NR.sup.6 R.sup.7, lower alkyl, cycloalkyl, --COR.sup.4, --COOR.sup.4, --CONR.sup.6 R.sup.7, --CN, --NO.sub.2, --SO.sub.2 R.sup.4, halogen, and --SO.sub.2 NR.sup.6 R.sup.7 ;R.sup.2 is selected from the group consisting of--H,--OR.sup.4,--COOR.sup.4,--CONR.sup.6 R.sup.7,--NR.sup.6 R.sup.7,halogen,--NO.sub.2,--CN,--SO.sub.2 R.sup.4,--SO.sub.2 NR.sup.6 R.sup.7,perfluoroalkyl, andlower alkyl which optionally may be substituted by the group consisting of --OR.sup.8 and NR.sup.6 R.sup.7 ;R.sup.3 is selected from the group consisting of--H,--OR.sup.4,--COR.sup.4,--COOR.sup.4,--CONR.sup.6 R.sup.7,halogen,--CN,--NR.sup.6 R.sup.7,perfluoroalkyl, andlower alkyl which optionally may be substituted by the group consisting of --OR.sup.8 and --NR.sup.6 R.sup.7 ;R.sup.4 is selected from the group consisting of--H,lower alkyl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.6 R.sup.7, cycloalkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9,cycloalkyl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.6 R.sup.7, lower alkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9, andheterocycle which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.6 R.sup.7, lower alkyl, cycloalkyl, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9 ;R.sup.5 is selected from the group consisting of--H,--COR.sup.8,--CONR.sup.8 R.sup.9, andlower alkyl which optionally may be substituted by the group consisting of --OR.sup.9, --NR.sup.9 R.sup.10, --N(COR.sup.9)R.sup.10, --COR.sup.9, --CONR.sup.9 R.sup.10, and --COOR.sup.9 ;R.sup.6 and R.sup.7 are each independently selected from the group consisting of--H,--COR.sup.8,--COOR.sup.8,--CONR.sup.8 R.sup.9,--SO.sub.2 R.sup.8,--SO.sub.2 NR.sup.8 R.sup.9,lower alkyl which optionally may be substituted by the group consisting of --OR.sup.5, --NR.sup.8 R.sup.9, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, --SO.sub.2 NR.sup.8 R.sup.9,cycloalkyl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9,heterocycle which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, cycloalkyl, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9,aryl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9, andheteroaryl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9,cycloalkyl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9,heterocycle which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, cycloalkyl, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9,aryl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, cycloalkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9, andheteroaryl which optionally may be substituted by the group consisting of --OR.sup.5, --COOR.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9, --NR.sup.8 R.sup.9, lower alkyl, cycloalkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, and --SO.sub.2 NR.sup.8 R.sup.9 ;or alternatively, --NR.sup.6 R.sup.7 can optionally form a ring having 3 to 7 atoms, said ring optionally including one or more additional hetero atoms and being optionally substituted by the group consisting of one or more of lower alkyl, --OR.sup.5, --COR.sup.8, --COOR.sup.8, CONR.sup.8 R.sup.9, and --NR.sup.5 R.sup.9 ;R.sup.8 is selected from the group consisting of--H,lower alkyl which optionally may be substituted by the group consisting of cycloalkyl, heterocycle, aryl, heteroaryl, --OR.sup.9, --NR.sup.9 R.sup.10, and --N(COR.sup.9)R.sup.10,aryl which optionally may be substituted by the group consisting of --OR.sup.9, --COOR.sup.9, --COR.sup.9, --CONR.sup.10 R.sup.9, --NR.sup.10 R.sup.9, lower alkyl, cycloalkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.9, and --SO.sub.2 NR.sup.10 R.sup.9,heteroaryl which optionally may be substituted by the group consisting of --OR.sup.9, --COOR.sup.9, --COR.sup.9, --CONR.sup.10 R.sup.9, --NR.sup.10 R.sup.9, lower alkyl, cycloalkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.9, and --SO.sub.2 NR.sup.10 R.sup.9 ;cycloalkyl which optionally may be substituted by the group consisting of --OR.sup.9, --COOR.sup.9, --COR.sup.9, --CONR.sup.10 R.sup.9, --NR.sup.10 R.sup.9, lower alkyl, heterocycle, --CN, --NO.sub.2, --SO.sub.2 R.sup.9, and --SO.sub.2 NR.sup.10 R.sup.9 ; andheterocycle which optionally may be substituted by the group consisting of --OR.sup.9, --COOR.sup.9, --COR.sup.9, --CONR.sup.10 R.sup.9, --NR.sup.10 R.sup.9, lower alkyl, cycloalkyl, --CN, --NO.sub.2, --SO.sub.2 R.sup.9, and --SO.sub.2 NR.sup.10 R.sup.9 ;R.sup.9 is selected from the group consisting of --H and lower alkyl;R.sup.10 is selected from the group consisting of --H and lower alkyl;X is selected from the group consisting of ##STR205## and a is an optional bond.