Patent ID: 6096917
Filing Date: 2000-08-01
Classification: C07C,C07D

Abstract:
A compound of the formula ##STR63## wherein: R is hydrogen;R.sup.0 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy(C.sub.1 -C.sub.6 alkyl), sulfhydryl, sulfamyl, --SO.sub.2 --Cl, --S--C(O)--N(CH.sub.3).sub.2, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, C.sub.1 -C.sub.4 alkylsulfonylamino, di(C.sub.1 -C.sub.4 alkylsulfonyl)amino, --X.sup.0 --O--C(O)--C.sub.1 -C.sub.4 alkyl, --O--(X.sup.1).sub.i, --C(O)--X.sup.3, --N--C(O)--R.sup.2 or --O--R.sup.3 ;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, hydroxy(C.sub.1 -C.sub.6 alkyl), sulfhydryl, sulfamyl, --SO.sub.2 --Cl, --S--C(O)--N(CH.sub.3).sub.2, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, C.sub.1 -C.sub.4 alkylsulfonylamino, di(C.sub.1 -C.sub.4 alkylsulfonyl)amino, --(C.sub.1 -C.sub.6 alkyl) --O--C(O)--C.sub.1 -C.sub.4 alkyl, --O--(X.sup.1).sub.i, --C(O)--X.sup.3, --N--C(O)--R.sup.2 or --O--R.sup.3 ;X.sup.0 is a bond or divalent(C.sub.1 -C.sub.6 alkyl);X.sup.1 is an amino acid ester of glycine, alanine or valine;i is 1, 2 or 3;X.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo(C.sub.1 -C.sub.6 alkyl), hydroxy(C.sub.1 -C.sub.6 alkyl) or phenyl;R.sup.2 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo(C.sub.1 -C.sub.4 alkyl), hydroxy(C.sub.1 -C.sub.4 alkyl), phenyl, p-methoxy-phenyl, p-fluoro-phenyl, naphthyl, or cyclohexyl;R.sup.3 is C.sub.2 -C.sub.6 alkenyl, --CH.sub.2 --R.sup.3a, --C(O)--R.sup.3b, --C(S)--R.sup.3c, --C(CH.sub.3).sub.2 C(O)NH.sub.2, phenyl or a group of the formula ##STR64## R.sup.3a is phenyl, p-fluorophenyl, cyclohexyl, cyclopentyl, cyclopropyl or naphthyl;R.sup.3b is benzyloxy, C.sub.1 -C.sub.6 alkoxy, halo(C.sub.1 -C.sub.4 alkoxy), amino, C.sub.1 -C.sub.4 alkylamino or di(C.sub.1 -C.sub.4 alkyl)amino;R.sup.3c is amino, C.sub.1 -C.sub.4 alkylamino or di(C.sub.1 -C.sub.4 alkyl)amino;R.sup.3d is oxygen, hydroximino, hydrazino or .dbd.CHZ;Z is hydrogen, C.sub.1 -C.sub.4 alkyl, halogen, di(C.sub.1 -C.sub.4 alkyl)amino, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl(C.sub.1 -C.sub.4 alkyl), N-(C.sub.1 -C.sub.4 alkyl)carbamoyl or N,N-di(C.sub.1 -C.sub.4 alkyl)carbamoyl;R.sup.3e is hydrogen, or trifluoromethyl;X is a bond or --(CH.sub.2)--;R.sup.4 is .dbd.N--R.sup.5 ;R.sup.5 is hydroxy, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, C.sub.1 -C.sub.4 alkoxy, benzyloxy, or --O--CH.sub.2 --C(O)--R.sup.5a ;R.sup.5a is hydroxy or C.sub.1 -C.sub.4 alkoxy;R.sup.6 is hydrogen, halo, C.sub.1 -C.sub.4 alkyl or .dbd.O;R.sup.7 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.8 is hydroxy, or C.sub.1 -C.sub.6 alkoxy;or a pharmaceutically acceptable salt thereof.