Patent ID: 6245773
Filing Date: 2001-06-12
Classification: A61K,C07D

Abstract:
A compound having the structure: ##STR75##wherein A is ##STR76##wherein each of Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4 and Y.sub.5 is independently --H; straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl; C.sub.3 -C.sub.7 cycloalkyl, monofluorocycloalkyl, polyfluorocycloalkyl or cycloalkenyl; --F, --Cl, --Br, or --I; --NO.sub.2 ; --N.sub.3 ; --CN; --OR.sub.3, --OCOR.sub.3, --COR.sub.3, --CONHR.sub.3, --CON(R.sub.3).sub.2, or --COOR.sub.3 ; or any two of Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4 and Y.sub.5 present on adjacent carbon atoms can constitute a methylenedioxy group;wherein X is S; O; or NR.sub.3 ;wherein R.sub.1 is --CO.sub.2 R.sub.3 ;wherein R.sub.2 is --H; straight chained or branched C.sub.1 -C.sub.7 alkyl, hydroxyalkyl, alkoxyalkyl, aminoalkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl; C.sub.3 -C.sub.7 cycloalkyl, monofluorocycloalkyl, polyfluorocycloalkyl or cycloalkenyl; C.sub.3 -C.sub.10 cycloalkyl-C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 cycloalkyl-C.sub.1 -C.sub.10 -monofluoroalkyl or C.sub.3 -C.sub.10 cycloalkyl-C.sub.1 -C.sub.10 -polyfluoroalkyl; --CN; --CH.sub.2 XR.sub.3, --CH.sub.2 X(CH.sub.2).sub.p NHR.sub.3, --(CH.sub.2).sub.n NHR.sub.3, --CH.sub.2 X(CH.sub.2).sub.p N(R.sub.3).sub.2, --CH.sub.2 X(CH.sub.2).sub.p N.sub.3, or --CH.sub.2 X(CH.sub.2).sub.p NHCXR.sub.7 ; or --OR.sub.3 ;wherein each p is independently an integer from 1 to 7;wherein each n is independently an integer from 0 to 5;wherein each R.sub.3 is independently --H; straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl, monofluorocycloalkyl,polyfluorocycloalkyl or cycloalkenyl;wherein R.sub.4 is ##STR77##wherein Z is CO; CO.sub.2 ; CONR.sub.3 ; S; SO; SO.sub.2 ; or NR.sub.3 ;wherein o is an integer from 1 to 3;wherein each R is independently --H; --F; straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl; --N(R.sub.3).sub.2 ; --NO.sub.2 ; --CN; --CO.sub.2 R.sub.3 ; or --OR.sub.3 ;wherein R.sub.5 is aryl or heteroaryl, substituted with one or more F; Cl; Br; I; COR.sub.3 ; CO.sub.2 R.sub.3 ; --CON(R.sub.3).sub.2 ; CN; --NO.sub.2 ; --N(R.sub.3).sub.2 ; --OR.sub.3 ; --SR.sub.3 ; (CH.sub.2).sub.o OR.sub.3 ; (CH.sub.2).sub.o SR.sub.3 ; straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl, polyfluoroalkyl, aminoalkyl, or carboxamidoalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl, C.sub.2 -C.sub.7 alkynyl; or C.sub.3 -C.sub.7 cycloalkyl, monofluorocycloalkyl, polyfluorocycloalkyl or cycloalkenyl; with the proviso that R.sub.5 is not aryl substituted with straight chained or branched C.sub.1 -C.sub.7 alkyl;wherein R.sub.6 is independently --H; straight chained or branched C.sub.1 -C.sub.7 alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl; C.sub.3 -C.sub.7 cycloalkyl, monofluorocycloalkyl, polyfluorocycloalkyl or cycloalkenyl; or --OR.sub.3 ; andwherein R.sub.7 is aryl or heteroaryl, substituted with one or more F; Cl; Br; I; COR.sub.3 ; CO.sub.2 R.sub.3 ; --CON(R.sub.3).sub.2 ; CN; --NO.sub.2 ; --N(R.sub.3).sub.2 ; --OR.sub.3 ; --SR.sub.3 ; (CH.sub.2).sub.o OR.sub.3 ; (CH.sub.2).sub.o SR.sub.3 ; straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl, polyfluoroalkyl, aminoalkyl, or carboxamidoalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl, C.sub.2 -C.sub.7 alkynyl; or C.sub.3 -C.sub.7 cycloalkyl, monofluorocycloalkyl, polyfluorocycloalkyl or cycloalkenyl;or a pharmaceutically acceptable salt thereof.