| abstract |
A heterocyclic aromatic amide of Formula I: ** Formula ** wherein: ** Formula ** a) represents a 6-membered heterocyclic aromatic ring in which X1 is N, X2 and X3 are CH and X4 is CH, COMe, CMe, CCl, COEt or CSMe, b) Z is O, S or NORz in which RZ is H or C1-C3 alkyl; and c) A represents (i) C3-C14 cycloalkyl, containing 0-3 heteroatoms and 0-2 unsaturations, substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 haloalkyl, cyano, nitro, aroyl, aryloxy, heteroaryloxy, C1-C6 alkylthio, arylthio, heteroarylthio, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C8 acyloxy, aryl, heteroaryl, C1-C6 acyl, C1-C6 carboalkoxy or unsubstituted amido or substituted with one or two alkyl groups C1-C6, or (ii) a C6-C14 bi- or tricyclic ring system containing 0-3 heteroatoms and 0-2 unsaturations, substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 haloalkyl, cyano, nitro , aroyl, aryloxy, heteroaryloxy, C1-C6 alkylthio, arylthio, heteroaryl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C8 acyloxy, aryl, heteroaryl, C1-C6 acyl, C1-C6 carboalkoxy or unsubstituted amido or substituted with one or two C1-C6 alkyl groups, wherein alkyl, alkenyl and alkynyl groups are unsubstituted or are substituted with one or more groups selected from h halogen, hydroxy, cyano, nitro, aroyl, aryloxy, aryl, arylthio, heteroaryl, heteroaryloxy, heteroarylthio, C1-C8 acyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1- haloalkylthio C6, carboaryloxy, carboheteroaryloxy, C1-C6 carboalkoxy or unsubstituted amido or substituted with one or two C1-C6 alkyl groups, wherein aryl groups are phenyl or naphthyl groups and heteroaryl groups are 5 or 6 membered aromatic rings containing one or more heteroatoms and wherein heteroaromatic rings may be condensed to other aromatic systems, wherein aryl and heteroaryl groups are unsubstituted or are substituted with one or more groups selected from nitro, C1-C6 alkyl, C1-C6 haloalkyl, C3 cycloalkyl -C6, C2-C6 alkenyl, C2-C6 alkynyl, aryl, heteroaryl, halogen, hydroxy, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 alkylsulfonyl, C1-C6 alkylsulfinyl, OC (O) C1-C6 alkyl, OC (O) aryl, OC (O) C3-C6 cycloalkyl, NHC (O) C1-C6 alkyl, NHC (O) C3-C6 cycloalkyl, NHC (O) aryl, NHC (O) heteroaryl, C3-C6 cycloalkylthio, C3-C6 cycloalkylsulfonyl, C3-C6 cycloalkylsulfinyl, aryloxy, heteroaryloxy, heteroarylthio, heteroarylsulfinonyl, heteroarylsulfinonyl , arylthio, arylsulfinyl, arylsulfonyl, C (O) Ry, C (NORx) Ry where Ry and Rx are independently H, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 cycloalkyl, aryl or heteroaryl in which any substituent containing alkyl or cycloalkyl may be substituted with one or more halogens; with the proviso that the following compounds are excluded: -3-hydroxy-4-methoxy-N- (1'-benzylpiperidin-4'-yl) picolinamide: - (2'-trans) -3-hydroxy-4-methoxy -N- (2'-methylcyclohexyl) picolinamide; - (2'-cis) -3-hydroxy-4-methoxy-N- (2'-methylcyclohexyl) picolinamide; -3-hydroxy-4-methoxy-N- (4'-methylcyclohexyl) picolinamide; -3-hydroxy-4-methoxy-N- (4'-hydroxycyclohexyl) picolinamide; and -3-hydroxy-4-methoxy-N- (2'-hydroxycyclohexyl) picolinamide. |