Patent ID: 6251944
Filing Date: 2001-06-26
Classification: A61K,A61P,C07C,C07D

Abstract:
A compound of the formula ##STR361##or a phamaceutically acceptable salt thereof, wherein ##STR362##wherein Y.sup.1 is selected from the group consisting of N--R.sup.2, O, and S;R.sup.2 is selected from the group consisting of alkyl; aryl; alkoxy; cyano; nitro; amino; aminocarbonyl; alkenyl; alkynyl; alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxyl, haloalkyl, cyano, nitro, carboxyl, amino, alkoxy, aryl or aryl optionally substituted with one or more halogen, haloalkyl, lower alkyl, alkoxy, cyano, alkylsulfonyl, alkylthio, nitro, carboxyl, amino, hydroxyl, sulfonic acid, sulfonamide, aryl, fused aryl, aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, hydroxy, lower alkyl, alkoxy, cyano, nitro, alkylthio, alkylsulfonyl, sulfonic acid, sulfonamide, carboxyl derivatives, amino, aryl,R.sup.7 and R.sup.8 are independently selected from the group consisting of H; alkyl; alkenyl; alkynyl; aralkyl; cycloalkyl; bicycloalkyl; aryl; acyl; benzoyl; alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxy, haloalkyl, cyano, nitro, carboxyl derivatives, amino, alkoxy, thio, alkylthio, sulfonyl, aryl, aralkyl, aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethyl, sulfonyl, alkylsulfonyl, haloalkylsulfonyl, sulfonic acid, sulfonamide, aryl, aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, aryl, --SO.sub.2 R.sup.10 wherein R.sup.10 is selected from the group consisting of alkyl, and aryl and all optionally substituted with one or more substituent selected from the group consisting of halogen, haloalkyl, alkyl, alkoxy, cyano, nitro, amino, acylamino, trifluoroalkyl, amido, alkylaminosulfonyl, alkylsulfonyl, alkylsulfonylamino, alkylamino, dialkylamino, trifluoromethylthio, trifluoroalkoxy, trifluoromethylsulfonyl, aryl, aryloxy, thio, and alkylthio, and ##STR363##wherein R.sup.10 is defined above; R.sup.5 is selected from the group consisting of H, alkyl, alkenyl, alkynyl, benzyl, and phenethyl;Z.sup.1, Z.sup.2, Z.sup.4 and Z.sup.5 are independently selected from the group consisting of H; alkyl; hydroxy; alkoxy; aryloxy; aralkoxy; halogen; haloalkyl; haloalkoxy; nitro; amino; aminoalkyl; alkylamino; dialkylamino; cyano; alkylthio; alkylsulfonyl; carboxyl derivatives; carboxyalkyl; alkoxycarbonylalkyl; acetamide; aryl; cycloalkyl; thio; and A, wherein A is defined above;B is selected from the group consisting of--CH.sub.2 CONH--, --CONR.sup.52 --(CH.sub.2).sub.P --, --C(O)O--, --SO.sub.2 NH--, --CH.sub.2 O--, and --OCH.sub.2 --;wherein p is an integer selected from the group consisting of 0, 1 and 2;wherein R.sup.50 is selected from the group consisting of H, alkyl, aryl, carboxyl derivative and --CONHCH.sub.2 CO.sub.2 R.sup.53 wherein R.sup.53 is H or lower alkyl;R.sup.52 is selected from the group consisting of H or alkyl;R.sup.51 is selected from the group consisting of H, alkyl, carboxyl derivatives, --NHSO.sub.2 R.sup.54, and NHCONHR.sup.54 ;wherein R.sup.54 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, aralkyl, aralkenyl and aryl substituted by one or more alkyl or halo;t is 0;R is X--R.sup.3 wherein X is selected from the group consisting of O, S and NR.sup.4, wherein R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen; alkyl; alkenyl; alkynyl; haloalkyl; aryl; arylalkyl; and in the case of the free acid, all pharmaceutically acceptable salts thereof.