Patent ID: 6221867
Filing Date: 2001-04-24
Classification: A61P,C07D

Abstract:
A compound of formula ##STR17##or the pharmaceutically acceptable salts of the foregoing compounds, wherein:R.sup.1 and R.sup.2 are independently selected from the group consisting of--H,--NR.sup.5 R.sup.6,lower alkyl which optionally may be substituted by --OR.sup.4, --COR.sup.4, --COOR.sup.4, --OCOR.sup.4, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --SO.sub.2 R.sup.4, --SO.sub.2 NR.sup.5 R.sup.6, cycloalkyl, heterocycle, aryl and heteroaryl, wherein the cycloalkyl and heterocycle optionally may be substituted by R.sup.11, and the aryl and heteroaryl optionally may be substituted by R.sup.12 ;cycloalkyl which optionally may be substituted by --OR.sup.4, --COR.sup.4, --COOR.sup.4, --OCOR.sup.4, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --SO.sub.2 R.sup.4, --SO.sub.2 NR.sup.5 R.sup.6, lower alkyl, heterocycle, aryl and heteroaryl, wherein the lower alkyl and heterocycle optionally may be substituted by R.sup.11, and the aryl and heteroaryl optionally may be substituted by R.sup.12 ;heterocycle which optionally may be substituted by --OR.sup.4, --COR.sup.4, --COOR.sup.4, --OCOR.sup.4, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6,--SO.sub.2 R.sup.4, --SO.sub.2 NR.sup.5 R.sup.6, lower alkyl, cycloalkyl, aryl and heteroaryl, wherein the lower alkyl and cycloalkyl optionally may be substituted by R.sup.11, and the aryl and heteroaryl optionally may be substituted by R.sup.12 ;aryl which optionally may be substituted by --OR.sup.4, --NR.sup.5 R.sup.6, halogen, --NO.sub.2, perfluoroalkyl, --COR.sup.4, --COOR.sup.4, --OCOR.sup.4, --CONR.sup.5 R.sup.6, --CN, --SO.sub.2 R.sup.4, --SO.sub.2 NR.sup.5 R.sup.6, lower alkyl, cycloalkyl, heterocycle, aryl and heteroaryl, wherein the lower alkyl, cycloalkyl and hetercycle optionally may be substituted by R.sup.11, and the aryl and heteroaryl optionally may be substituted by R.sup.12 ; andheteroaryl which optionally may be substituted by --OR.sup.4, --NR.sup.5 R.sup.6, halogen, --NO.sub.2, perfluoroalkyl, --COR.sup.4, --COOR.sup.4, --OCOR.sup.4, --CONR.sup.5 R.sup.6, --CN, --SO.sub.2 R.sup.4, --SO.sub.2 NR.sup.5 R.sup.6, lower alkyl, cycloalkyl, heterocycle, and aryl, wherein the lower alkyl, cycloalkyl and heterocycle optionally may be substituted by R.sup.11, and the aryl optionally may be substituted by R.sup.12 ; oralternatively, R.sup.1 and R.sup.2 may form a ring having 5 to 7 atoms and optionally being substituted by the group consisting of --OR.sup.8, --COR.sup.7, --COOR.sup.7, --CONR.sup.7 R.sup.9, --NR.sup.8 R.sup.9, and lower alkyl which optionally may be substituted by R.sup.11.R.sup.3 is selected from the group consisting of--H--OR.sup.4--COR.sup.4--COOR.sup.4--OCOR.sup.4--CONR.sup.5 R.sup.6halogen--CNperfluoroalkyl--NR.sup.5 R.sup.6, andlower alkyl which optionally may be substituted by --OR.sup.4, --OCOR.sup.4, or --NR.sup.5 R.sup.6 ;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.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.5 R.sup.6, cycloalkyl, heterocycle, aryl, and heteroaryl, and wherein the cycloalkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12, cycloalkyl which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.5 R.sup.6, lower alkyl, heterocycle, aryl, and heteroaryl, and wherein the lower alkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaxyl each may be optionally substituted by the group R.sup.12,heterocycle which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.5 R.sup.6, cycloalkyl, lower alkyl, aryl, and heteroaryl, and wherein the cycloalkyl and lower alkyl each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12,aryl which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --NO.sub.2, halogen, perfluoroalkyl, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.5 R.sup.6, lower alkyl, cycloallyl, heterocycle, aryl, and heteroaryl, and wherein the lower alkyl, cycloalkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12, andheteroaryl which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --NO.sub.2, halogen, perfluoroalkyl, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.5 R.sup.6, cycloalkyl, lower alkyl, heterocycle, aryl, and heteroaryl, and wherein the lower alkyl, cycloalkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12 ;R.sup.5 and R.sup.6 are each independently selected from the group consisting of--H,--COR.sup.7,--COOR.sup.7,--CONR.sup.7 R.sup.9, andlower alkyl which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8, --NR.sup.7 R.sup.8, --SO.sub.2 NR.sup.7, --SO.sub.2 NR.sup.7 R.sup.8, cycloalkyl, heterocycle, aryl, and heteroaryl, and wherein the cycloalkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12,cycloalkyl which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8, --NR.sup.7 R.sup.8, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.7 R.sup.8, lower alkyl, heterocycle, aryl, and heteroaryl, and wherein the lower alkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12,heterocycle which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8, --NR.sup.7 R.sup.8, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.7 R.sup.8, cycloalkyl, lower alkyl, aryl, and heteroaryl, and wherein the cycloalkyl and lower alkyl each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12,aryl which optionally may be substituted by the group consisting of OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8, --NR.sup.7 R.sup.8, --NO.sub.2, halogen, perfluoroalkyl, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.7 R.sup.8, lower alkyl, cycloalkyl, heterocycle, aryl, and heteroaryl, and wherein the lower alkyl, cycloalkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12, andheteroaryl which optionally may be substituted by the group consisting of --OR.sup.8, --COOR.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8, --NR.sup.7 R.sup.8, --NO.sub.2, halogen, perfluoroalkyl, --SO.sub.2 R.sup.7, --SO.sub.2 NR.sup.7 R.sup.8, lower alky, cycloalkyl, heterocycle, aryl, and heteroaryl, and wherein the lower alkyl, cycloalkyl and heterocycle each may be optionally substituted by the group R.sup.11 and the aryl and heteroaryl each may be optionally substituted by the group R.sup.12 ; oralternatively, --NR.sup.5 R.sup.6 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 lower alkyl, --OR.sup.8, --COR.sup.7, --COOR.sup.7, --CONR.sup.7 R.sup.9, and --NR.sup.8 R.sup.9 ;R.sup.7 is selected from the group consisting of--H, andlower alkyl which optionally may be substituted by the group consisting of cycloalkyl, heterocycle, aryl, heteroaryl, --OR.sup.9, and --NR.sup.8 R.sup.9 ;R.sup.8 is selected from the group consisting of--H,--COR.sup.9,--CONR.sup.10 R.sup.9, andlower alkyl which optionally may be substituted by R.sup.11 ;R.sup.9 and R.sup.10 are each independently selected from the group consisting of --H and lower alkyl;R.sup.11 is selected from the group consisting of --OR.sup.9, --COR.sup.9, --COOR.sup.9, --OCOR.sup.9, CONR.sup.9 R.sup.10, --NR.sup.9 R.sup.10, --N(COR.sup.9)R.sup.10, --SO.sub.2 R.sup.9, --SO.sub.2 NR.sup.9 R.sup.10 ;R.sup.12 is selected from the group consisting of --OR.sup.9, --COR.sup.9, --COOR.sup.9, --OCOR.sup.9, --CONR.sup.9 R.sup.10, --NR.sup.9 R.sup.10, --N(COR.sup.9)R.sup.10, --SO.sub.2 R.sup.9, --SO.sub.2 NR.sup.9 R.sup.10, halogen, --CN, --NO.sub.2, perfluoroalkyl; andX is selected from the group consisting of --N-- and --C--.