Patent ID: 6268369
Filing Date: 2001-07-31
Classification: A61P,C07D

Abstract:
A compound having the structure: ##STR57##wherein A is ##STR58##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 --H; --NO.sub.2 ; --CN; 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; --N(R.sub.3).sub.2 ; --OR.sub.3 ; --(CH.sub.2).sub.p OR.sub.3 ; --COR.sub.3 ; --CO.sub.2 R.sub.3 ; or --CON (R.sub.3).sub.2 ;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 ##STR59##wherein R.sub.4 in the immediately preceding structure is --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 cycloakyl, monofluorocycloalkyl, polyfluorocycloalkyl or cycloalkenyl, ##STR60##wherein Z is C.sub.2 -C.sub.7 alkenylene or alkynylene; CH.sub.2 ; O; CONR.sub.3 ; S; SO; SO.sub.2 ; or NR.sub.3 ;wherein each D is independently CH.sub.2 ; O; S; NR.sub.3 ; CO; or CS;wherein W is C.dbd.O; C.dbd.NOR.sub.3 ; or substituted or unsubstituted phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl or benzimidazolyl, wherein the phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl or benzimidazolyl is substituted with --H, --F, --Cl, --Br, --I, --NO.sub.2, --CN, straight chained or branched C.sub.1 -C.sub.7 alkyl, straight chained or branched C.sub.1 -C.sub.7 monofluoroalkyl, straight chained or branched C.sub.1 -C.sub.7 polyfluoroalkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl, straight chained or branched C.sub.2 -C.sub.7 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 monofluorocycloalkyl, C.sub.3 -C.sub.7 polyfluorocycloalkyl, C.sub.3 -C.sub.7 cycloalkenyl, --N(R.sub.3).sub.2, --OR.sub.3, --COR.sub.3, --CO.sub.2 R.sub.3, or --CON(R.sub.3).sub.2 ;wherein each V is independently O; S; CR.sub.5 R.sub.7 ; C(R.sub.7).sub.2 ; or NR.sub.7 ;wherein each m is independently an integer from 0 to 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 --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; phenyl, thiophenyl, pyridyl, pyrrolyl, furanyl, imidazolyl or indolyl; or --COOR.sub.3, --COR.sub.3, --CONHR.sub.3, --CN, or --OR.sub.3 ;wherein each 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;wherein each R.sub.7 is independently --H; substituted or unsubstituted benzyl, benzoyl, phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl, benzimidazolyl or 2-keto-1-benzimidazolinyl, wherein the benzyl, benzoyl, phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl, benzimidazolyl or 2-keto-1-benzimidazolinyl is substituted with --H, --F, --Cl, --Br, --I, --NO.sub.2, --CN, straight chained or branched C.sub.1 -C.sub.7 alkyl, straight chained or branched C.sub.1 -C.sub.7 monofluoroalkyl, straight chained or branched C.sub.1 -C.sub.7 polyfluoroalkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl, straight chained or branched C.sub.2 -C.sub.7 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 monofluorocycloalkyl, C.sub.3 -C.sub.7 polyfluorocycloalkyl, C.sub.3 -C.sub.7 cycloalkenyl, --N(R.sub.3).sub.2, --OR.sub.3, --COR.sub.3, --CO.sub.2 R.sub.3, or --CON(R.sub.3).sub.2 ; substituted or unsubstituted straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl or polyfluoroalkyl; substituted or unsubstituted straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl or cycloalkenyl, wherein the alkyl, monofluoroalkyl, polyfluoroalkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is substituted with --H, phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl, or benzimidazolyl; andwherein R.sub.8 is --H; substituted or unsubstituted benzyl, benzoyl, phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl, benzimidazolyl or 2-keto-1-benzimidazolinyl, wherein the benzyl, benzoyl, phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl, benzimidazolyl or 2-keto-1-benzimidazolinyl is substituted with --H, --F, --Cl, --Br, --I, --NO.sub.2, --CN, straight chained or branched C.sub.1 -C.sub.7 alkyl, straight chained or branched C.sub.1 -C.sub.7 monofluoroalkyl, straight chained or branched C.sub.1 -C.sub.7 polyfluoroalkyl, straight chained or branched C.sub.2 -C.sub.7 alkenyl, straight chained or branched C.sub.2 -C.sub.7 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 monofluorocycloalkyl, C.sub.3 -C.sub.7 polyfluorocycloalkyl, C.sub.3 -C.sub.7 cycloalkenyl, --N(R.sub.3).sub.2, --OR.sub.3, --COR.sub.3, --CO.sub.2 R.sub.3, or --CON(R.sub.3).sub.2 ; substituted or unsubstituted straight chained or branched C.sub.1 -C.sub.7 alkyl, monofluoroalkyl or polyfluoroalkyl; substituted or unsubstituted straight chained or branched C.sub.2 -C.sub.7 alkenyl or alkynyl; or C.sub.3 -C.sub.7 cycloalkyl or cycloalkenyl, wherein the alkyl, monofluoroalkyl, polyfluoroalkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl is substituted with --H, phenyl, pyridyl, thiophenyl, furanyl, pyrazinyl, pyrrolyl, naphthyl, indolyl, imidazolyl, benzofurazanyl, benzofuranyl, benzimidazolyl, --N(R.sub.3).sub.2, --NO.sub.2, --CN, --CO.sub.2 R.sub.3, --OR.sub.3 ; ##STR61##or a pharmaceutically acceptable salt thereof.