Patent ID: 6222040
Filing Date: 2001-04-24
Classification: C07D

Abstract:
A compound having the structure: ##STR39##wherein each R.sub.1 is independently H, F, Cl, Br, --CN, --OH, --NO.sub.2, --NR.sub.5 R.sub.6, --SO.sub.2 R.sub.5, --(CH.sub.2).sub.n OR.sub.5, --(CH.sub.2).sub.n CONR.sub.5 R.sub.6, --(CH.sub.2).sub.n NR.sub.5 COR.sub.5, perfluoroalkyl, polyfluoroalkyl, aminoalkyl, or straight chained or branched C.sub.1 -C.sub.7 alkyl;wherein R.sub.5 is independently H; or straight chained or branched C.sub.1 -C.sub.7 alkyl;wherein R.sub.6 is independently H; or straight chained or branched C.sub.1 -C.sub.7 alkyl;wherein B is O, NH or S;wherein X is S, SO or SO.sub.2 ;wherein each n independently is an integer from 0 to 6 inclusive;wherein R.sub.8 is ##STR40##wherein Y is C or N;wherein R.sub.7 is independently straight chained or branched C.sub.1 -C.sub.7 alkyl;wherein R.sub.9 is independently H; or straight chained or branched C.sub.1 -C.sub.4 alkyl;wherein R.sub.10 is independently H; or straight chained or branched C.sub.1 -C.sub.4 alkyl;wherein R.sub.11 is ##STR41##wherein R.sub.12 is H, straight chained or branched C.sub.1 -C.sub.7 alkyl, (CH.sub.2).sub.n OR.sub.17, or O(CH.sub.2).sub.u OR.sub.17 ;wherein R.sub.13 is independently H; --(CH.sub.2).sub.u OR.sub.5 ; --(CH.sub.2).sub.t CONR.sub.5 R.sub.6 ; --(CH.sub.2).sub.u NR.sub.5 COR.sub.5 ; --(CH.sub.2).sub.t COR.sub.7 ; --(CH.sub.2).sub.t CO.sub.2 R.sub.5 ; --(CH.sub.2).sub.u NR.sub.5 R.sub.6 ; --(CH.sub.2).sub.u CN; straight chained or branched C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.7 alkyl in which the C.sub.2 -C.sub.7 atoms may be optionally substituted with one or more F or Cl; C.sub.3 -C.sub.7 cycloalkyl-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; phenyl or C.sub.1 -C.sub.6 phenylalkyl; wherein the phenyl or C.sub.1 -C.sub.6 phenylalkyl may be substituted with one or more of F, Cl, --CN, --NO.sub.2, --NR.sub.5 R.sub.6, --SO.sub.2 R.sub.5, --(CH.sub.2).sub.n COR.sub.7, --(CH.sub.2).sub.n OR.sub.5, --(CH.sub.2).sub.n CONR.sub.5 R.sub.6, --(CH.sub.2).sub.n NR.sub.5 COR.sub.5, --(CH.sub.2).sub.n CO.sub.2 R.sub.5, --(CH.sub.2).sub.n SO.sub.2 NR.sub.5 R.sub.6, straight chained or branched C.sub.1 -C.sub.7 alkyl, perfluoroalkyl, polyfluoroalkyl, or aminoalkyl;or R.sub.12 and R.sub.13 together with the amide linkage to which they are attached are pyrrolidinonyl, piperidonyl, or oxazolidinonyl;wherein R.sub.14 is H; straight chained or branched C.sub.1 -C.sub.4 alkyl; F; or --(CH.sub.2).sub.r OR.sub.5 ;wherein R.sub.15 is H, straight chained or branchedC.sub.1 -C.sub.4 alkyl, or F;with the proviso that when R.sub.14 is --OH, R.sub.15 cannot be F;wherein R.sub.3 is independently H; --(CH.sub.2).sub.u OR.sub.5 ; --(CH.sub.2).sub.t CONR.sub.5 R.sub.6 ; --(CH.sub.2).sub.u NR.sub.5 COR.sub.5 ; --(CH.sub.2).sub.t COR.sub.7 ; --(CH.sub.2).sub.t CO.sub.2 R.sub.5 ; --(CH.sub.2).sub.u NR.sub.5 R.sub.6 ; --(CH.sub.2).sub.u CN; 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 cycloalkenyl; phenyl, C.sub.1 -C.sub.6 phenylalkyl or C.sub.1 -C.sub.6 heteroarylalkyl; wherein the phenyl, C.sub.1 -C.sub.6 phenylalkyl, or C.sub.1 -C.sub.6 heteroarylalkyl may be substituted with one or more of F, Cl, Br, --CN, --NO.sub.2, --NR.sub.5 R.sub.6, --SO.sub.2 R.sub.5, --(CH.sub.2).sub.n COR.sub.7, --(CH.sub.2).sub.n OR.sub.5, --(CH.sub.2).sub.n CONR.sub.5 R.sub.6, --(CH.sub.2).sub.n NR.sub.5 COR.sub.5, --(CH.sub.2).sub.n CO.sub.2 R.sub.5, --(CH.sub.2).sub.n SO.sub.2 NR.sub.5 R.sub.6, straight chained or branched C.sub.1 -C.sub.7 alkyl, perfluoroalkyl, polyfluoroalkyl, or aminoalkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl, or C.sub.3 -C.sub.7 cycloalkyl or cycloalkenyl;wherein R.sub.4 is independently H; --(CH.sub.2) OR.sub.5 ; --(CH.sub.2).sub.t CONR.sub.5 R.sub.6 ; --(CH.sub.2).sub.u NR.sub.5 COR.sub.5 ; --(CH.sub.2).sub.t COR.sub.7 ; --(CH.sub.2).sub.t CO.sub.2 R.sub.5 ; --(CH.sub.2).sub.u NR.sub.5 R.sub.6 ; --(CH.sub.2).sub.u CN; 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 cycloalkenyl; phenyl or C.sub.1 -C.sub.6 phenylalkyl; wherein the phenyl or C.sub.1 -C.sub.6 phenylalkyl may be substituted with one or more of F, Cl, Br, --CN, --NO.sub.2, --NR.sub.5 R.sub.6, --SO.sub.2 R.sub.5, --(CH.sub.2).sub.n COR.sub.7, --(CH.sub.2).sub.n OR.sub.5, --(CH.sub.2).sub.n CONR.sub.5 R.sub.6, --(CH.sub.2).sub.n NR.sub.5 COR.sub.5, --(CH.sub.2).sub.n CO.sub.2 R.sub.5, --(CH.sub.2).sub.n SO.sub.2 NR.sub.5 R.sub.6, straight chained or branched C.sub.1 -C.sub.7 alkyl, perfluoroalkyl, polyfluoroalkyl, or aminoalkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl, or C.sub.3 -C.sub.7 cycloalkyl or cycloalkenyl;or R.sub.3 and R.sub.4 taken together with the nitrogen atom to which they are attached are 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, or 1H-azepanyl, wherein the 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, or 1H-azepanyl is substituted with one or more of F, --CN, --(CH.sub.2).sub.n NR.sub.5 R.sub.6, --SO.sub.2 R.sub.5, --(CH.sub.2).sub.n COR.sub.7, --(CH.sub.2).sub.n OR.sub.5, --(CH.sub.2).sub.n CONR.sub.5 R.sub.6, --(CH.sub.2).sub.n NR.sub.5 COR.sub.5, --(CH.sub.2).sub.n CO.sub.2 R.sub.5, straight chained or branched C.sub.1 -C.sub.7 alkyl, perfluoroalkyl, polyfluoroalkyl, or aminoalkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl, or C.sub.3 -C.sub.7 cycloalkyl or cycloalkenyl, or phenyl or heteroaryl; wherein if --(CH.sub.2).sub.n NR.sub.5 R.sub.6, --(CH.sub.2).sub.n OR.sub.5, or --(CH.sub.2).sub.n NR.sub.5 COR.sub.5 are in the 2-position, then n is not 0; wherein the phenyl or heteroaryl may be substituted with one or more of F, Cl, Br, --CN, --NO.sub.2, --NR.sub.5 R.sub.6, --SO.sub.2 R.sub.5, --(CH.sub.2).sub.n COR.sub.7, --(CH.sub.2).sub.n OR.sub.5, --(CH.sub.2).sub.n CONR.sub.5 R.sub.6, --(CH.sub.2).sub.n NR.sub.5 COR.sub.5, --(CH.sub.2).sub.n CO.sub.2 R.sub.5, --(CH.sub.2).sub.n SO.sub.2 NR.sub.5 R.sub.6, straight chained or branched C.sub.1 -C.sub.7 alkyl, perfluoroalkyl, polyfluoroalkyl, or aminoalkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl, or C.sub.3 -C.sub.7 cycloalkyl or cycloalkenyl;or R.sub.3 and R.sub.4 taken together with the nitrogen atom to which they are attached are morpholinyl, thiomorpholinyl, [1,4]oxazepanyl, [1,4]thiazepanyl, piperazinyl, or [1,4]diazepanyl, wherein the morpholinyl, thiomorpholinyl, [1,4]oxazepanyl, [1,4]thiazepanyl, piperazinyl, or [1,4]diazepanyl is optionally substituted with straight chained or branched C.sub.1 -C.sub.5 alkyl or (CH.sub.2).sub.t OR.sub.5 ; and wherein the nitrogen atom of the piperazinyl or [1,4]diazepanyl ring may be optionally substituted with --(CH.sub.2).sub.u OR.sub.5 ; --COR.sub.5 ; --CO.sub.2 R.sub.5 ; straight chained or branched C.sub.1 -C.sub.5 alkyl; or phenyl; wherein the phenyl may be substituted with one or more of F, Cl, Br, --CN, --NO.sub.2, --NR.sub.5 R.sub.6 --(CH.sub.2).sub.n OR.sub.5, straight chained or branched C.sub.1 -C.sub.3 alkyl, perfluoroalkyl, polyfluoroalkyl, or aminoalkyl;wherein R.sub.17 is straight chained or branched C.sub.1 -C.sub.4 alkyl, perfluoroalkyl, or polyfluoroalkyl;wherein m is 0 or 1;wherein each p independently is an integer from 0 to 2 inclusive;wherein each r independently is an integer from 0 to 3 inclusive;wherein each s independently is an integer from 1 to 6 inclusive;wherein t is an integer from 1 to 4 inclusive;wherein each u independently is an integer from 2 to 4 inclusive;wherein v is 1 or 2;with the proviso that when v is 2, m is 0;wherein z is an integer from 2 to 7;or a pharmaceutically acceptable salt thereof.