Patent ID: 6159990
Filing Date: 2000-12-12
Classification: A61K,C07D

Abstract:
A compound having the structure: wherein each X is independently O or S;wherein q is 1;wherein each R.sub.2 is independently H; --(CH.sub.2).sub.t XR.sub.3 ; --(CH.sub.2).sub.t C(X)NR.sub.3 ; --(CH.sub.2).sub.t CO.sub.2 R.sub.3 ; --CO.sub.2 R.sub.3 ; straight chained or branched C.sub.1 -C.sub.7 alkyl, aminoalkyl, carboxamidoalkyl; straight chained or branched C.sub.2 -C.sub.7 alkenyl, or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;wherein each t is an integer from 1 to 4 inclusive;wherein each R.sub.3 is independently H; straight chained or branched C.sub.1 -C.sub.7 alkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl, or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;wherein R.sub.4 is aryl, heteroaryl, C.sub.1 -C.sub.7 alkyl substituted with one or two aryl, or C.sub.1 -C.sub.7 alkyl substituted with one or two heteroaryl; wherein the aryl or heteroaryl may be substituted with one or more of F, Cl, Br, I, --CN, --NO.sub.2, --N(R.sub.3).sub.2, --COR.sub.3, --(CH.sub.2).sub.t XR.sub.3, --(CH.sub.2).sub.n C(X)NR.sub.3, --(CH.sub.2).sub.n CO.sub.2 R.sub.3, straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl, polyfluoroalkyl or carboxamidoalkyl, or straight chained or branched C.sub.2 -C.sub.7 aminoalkyl, alkenyl or alkynyl, or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;wherein each n independently is an integer from 0 to 7 inclusive;wherein R.sub.5 is H; aryl, C.sub.1 -C.sub.7 alkyl substituted with aryl, heteroaryl, or C.sub.1 -C.sub.7 alkyl substituted with heteroaryl; wherein the aryl or heteroaryl may be substituted with one or more of F, Cl, Br, I, --CN, --NO.sub.2, --N(R.sub.3).sub.2, --COR.sub.3, --(CH.sub.2).sub.t XR.sub.3, --(CH.sub.2).sub.n C(X)NR.sub.3, --(CH.sub.2).sub.n CO.sub.2 R.sub.3, straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl, polyfluoroalkyl or carboxamidoalkyl, or straight chained or branched C.sub.2 -C.sub.7 aminoalkyl, alkenyl or alkynyl, or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;where R.sub.5 and one R.sub.2 on adjacent carbon atoms together may form aryl, heteroaryl, indane or tetrahydronaphthyl, C.sub.3 -C.sub.7 cycloalkyl, or heterocycloalkyl wherein one or two heteroatoms may be O, N or S;wherein R.sub.1 is ##STR26## where each R.sub.6 is independently aryl or heteroaryl, wherein the aryl or heteroaryl may be substituted with one or more of F, Cl, Br, I, --(CH.sub.2).sub.n XR.sub.3, --COR.sub.3, --(CH.sub.2).sub.n C(X)N(R.sub.3).sub.2, --(CH.sub.2).sub.n CO.sub.2 R.sub.3, --CN, --NO.sub.2, --N(R.sub.3).sub.2, --SO.sub.2 R.sub.3, 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 C.sub.5 -C.sub.7 cycloalkenyl;where each R.sub.7 is independently H; F; Cl; Br; I; --COR.sub.3 ; --CO.sub.2 R.sub.3 ; --(CH.sub.2).sub.n XR.sub.3 ; (CH.sub.2).sub.n C(X)N(R.sub.3).sub.2 ; --(CH.sub.2).sub.n CO.sub.2 R.sub.3 ; --CN; --NO.sub.2 ; --N(R.sub.3).sub.2 ; straight chained or branched C.sub.1 -C.sub.7 alkyl, hydroxyalkyl, aminoalkyl, carboxamidoalkyl, 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 C.sub.5 -C.sub.7 cycloalkenyl, wherein the alkyl, aminoalkyl, carboxamidoalkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl may be substituted with one or more aryl or heteroaryl, wherein the aryl or heteroaryl may be substituted with one or more of F, Cl, Br, I, --(CH.sub.2).sub.n XR.sub.3, --COR.sub.3, --(CH.sub.2).sub.n C(X)N(R.sub.3).sub.2, --(CH.sub.2).sub.n CO.sub.2 R.sub.3, --CN, --NO.sub.2, --N(R.sub.3).sub.2, --SO.sub.2 R.sub.3, 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 C.sub.5 -C.sub.7 cycloalkenyl; aryl or heteroaryl, wherein the aryl or heteroaryl may be substituted with one or more of F, Cl, Br, I, --(CH.sub.2).sub.n XR.sub.3, --COR.sub.3, --(CH.sub.2).sub.n C(X)N(R.sub.3).sub.2, --(CH.sub.2).sub.n CO.sub.2 R.sub.3, --CN, --NO.sub.2, --N(R.sub.3).sub.2, --SO.sub.2 R.sub.3, straight chained or branched C.sub.1 -C.sub.7 alkyl, straight chained or branched C.sub.1 -C.sub.7 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 C.sub.5 -C.sub.7 cycloalkenyl;wherein each R.sub.10 is independently H; (CH.sub.2).sub.t XR.sub.3 ; (CH.sub.2).sub.t C(X)NR.sub.3 ; (CH.sub.2).sub.t CO.sub.2 R.sub.3 ; straight chained or branched C.sub.1 -C.sub.7 alkyl or carboxamidoalkyl; straight chained or branched C.sub.2 -C.sub.7 aminoalkyl, alkenyl, or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;wherein R.sub.11 is aryl, heteroaryl, C.sub.1 -C.sub.7 alkyl substituted with one or two aryl, or C.sub.1 -C.sub.7 alkyl substituted with one or two heteroaryl; wherein any aryl or heteroaryl independently may be substituted with one or more of F, Cl, Br, I, --CN, --NO.sub.2, --N(R.sub.3).sub.2, --COR.sub.3, --(CH.sub.2).sub.n XR.sub.3, --(CH.sub.2).sub.n C(X)NR.sub.3, --(CH.sub.2).sub.n CO.sub.2 R.sub.3, straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl, polyfluoroalkyl, or carboxamidoalkyl, straight chained or branched C.sub.2 -C.sub.7 aminoalkyl, alkenyl, or alkynyl, or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;wherein each m independently is an integer from 0 to 3 inclusive;wherein Z is ##STR27## or C.sub.2 -C.sub.7 alkenyl, wherein the C.sub.2 -C.sub.7 alkenyl may be unsubstituted or substituted with one or more R.sub.9 groups;where R.sub.8 is H; (CH.sub.2).sub.t XR.sub.3 ; (CH.sub.2).sub.t C(X)NR.sub.3 ; (CH.sub.2).sub.t CO.sub.2 R.sub.3 ; straight chained or branched C.sub.1 -C.sub.7 alkyl, carboxamidoalkyl; straight chained or branched C.sub.2 -C.sub.7 aminoalkyl, alkenyl, or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;where each R.sub.9 is independently H; F; Cl; Br; I; (CH.sub.2).sub.m XR.sub.3 ; (CH.sub.2).sub.m C(X)NR.sub.3 ; (CH.sub.2).sub.m CO.sub.2 R.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, or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.7 cycloalkenyl;wherein Y is S, O, or NR.sub.3 ;or a pharmaceutically acceptable salt thereof.