Patent ID: 6252086
Filing Date: 2001-06-26
Classification: A61P,C07D

Abstract:
A compound having the formula: ##STR205##or 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 is unsubstituted or substituted by 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 is unsubstituted or substituted by 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 is unsubstituted or substituted by the group consisting of --OR.sup.5, --NR.sup.5 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.7halogen,--NO.sub.2,--CN,--SO.sub.2 R.sup.4,--SO.sub.2 N R.sup.6 R.sup.7,perfluoroalkyl, andlower alkyl which is unsubstituted or substituted by the group consisting of --OR.sup.8 and NR R.sup.7 ;R.sup.3 is selected from the group consisting of--H.--COR.sup.4--COOR.sup.4,--CONR.sup.6 R.sup.7,halogen,--CN,--N R.sup.6 R.sup.7perfluoroalkyl, andlower alkyl which is unsubstituted or 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 is unsubstituted or 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 N R.sup.8 R.sup.9,cycloalkyl which is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or substituted by the group consisting of --OR.sup.5, --NR.sup.8 R.sup.9, --COOR.sup.8, --COR.sup.8, --CONR.sup.3 R.sup.9, --CN, --NO.sub.2, --SO.sub.2 R.sup.8, --SO.sub.2 NR.sup.8 R.sup.9,cycloalkyl which is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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,heteroaryl which is unsubstituted or 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, and--NR.sup.6 R.sup.7 can form a ring having 3 to 7 atoms, said ring including no additional hetero atoms or including one or more additional hetero atoms and being unsubstituted or 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 Is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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 is unsubstituted or 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.1 lR.sup.9 ; andheterocycle which is unsubstituted or 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 .dbd.N--; anda is either no bond or a bond.