Patent ID: 6207708
Filing Date: 2001-03-27
Classification: A61P,C07C,C07D,C07F

Abstract:
A compound having the formula; ##STR151##and pharmaceutically acceptable salts, wherein:A is O;R.sup.1 is not present or is selected from the group consisting of hydrogen, hydroxyalkyl, alkoxyalkyl, alkyl and haloalkyl;R.sup.2 is selected from the group consisting of straight and branched alkyl, alkenyl, and alkynyl, cycloalkyl, cycloalkenyl, haloalkyl; all optionally substituted by one or more of hydrogen, alkyl, alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, or amino groups;R.sup.3 is selected from the group consisting of aryl, alkylaryl, all optionally substituted by one or more of halogen, nitrile, carboxy, carboxyalkyl, carboxyalkylaryl; orR.sup.3 is also selected from the group consisting of H, alkyl, alkenyl, CH.sub.2 OC(.dbd.O)YR.sup.6, alkylhydroxy, alkylpolyhydroxy, amino, hydroxy, alkyl(poly)oxyacyl, alkylcarboxy, optionally substituted by one or more of alkyl, hydroxy, amino, carboxy, carboxyalkyl, alkylcarbonyl;R.sup.4 is selected from H, OH, SH, OR.sup.6, SR.sup.6, OC(.dbd.O)R.sup.6, CH.sub.2 OC(.dbd.O)YR.sup.6, OC(.dbd.O)YR.sup.6 ;Y is independently selected from O, S, CH.sub.2, CHR.sup.6, C(R.sup.6).sub.2, NH, NR.sup.6 ;R.sup.5 is selected from H, OH, SH; OR.sup.6, SR.sup.6, OC(.dbd.O)R.sup.6, CH.sub.2 OC(.dbd.O)YR.sup.6, OC(.dbd.O)YR.sup.6,R.sup.6 is selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, and aryl all optionally substituted by one or more alkyl, alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, or amino groups;R.sup.7 is selected from H, CH.sub.2 OC(O)--R.sup.9, C(O)--R.sup.9 where C(O)--R.sup.9 can represent natural and synthetic amino acids or R.sup.9 can be defined as below;R.sup.8 is selected from H, acyl;provided that R.sup.4, R.sup.5, R.sup.7 and R.sup.8 are not simultaneously hydrogen;R.sup.9 is selected from substituted alkyl, alkoxy, amino, cycloalkoxy, optionally substituted with one or more of amino, alkyl, alkylaryl, alkylmercaptoalkyl, which may optionally be substituted with one or more of hydroxy, amino, guanidino, iminoalkyl;X is selected from the group consisting of alkylene, alkenylene and alkynylene and which may optionally be substituted by one or more alkyl, alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, or amino groups; orX is selected from the group consisting of the formula --(CH.sub.2).sub.k Q(CH.sub.2).sub.t -- where k is 1, 2 or 3, t is 1, 2 or 3 and Q is O or NR where R is H or alkyl which may be optionally substituted with alkyl, alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, amino; orX is selected from the group consisting of the formula --(CH.sub.2).sub.m T(CH.sub.2).sub.n -- where m is 0, 1 or 2, n is 0, 1 or 2, T is a 3 to 6 membered carbocyclic ring or aromatic ring which may optionally be substituted by one or more substituents selected from the group consisting of alkyl, alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino.