Patent ID: 6136829
Filing Date: 2000-10-24
Classification: A61P,C07D

Abstract:
A compound having the formula; ##STR41## and pharmaceutically acceptable salts, wherein: A is O, S, or NR, wherein:R is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkenyl, oxathiadiazole, aryl, and alkylaryl, all optionally substituted by one or more of alkyl, hydroxy, alkoxy, halogen, haloalkyl, cyano, amino, and nitro; orNR together form a heterocyclic;R.sup.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl, oxathiadiazole, aryl, and alkylaryl, all optionally substituted by one or more of alkyl, hydroxy, alkoxy, halogen, haloalkyl, cyano, amino, and nitro;R.sup.2 is selected from the group consisting of amino, thioalkoxy, alkoxy, lower alkyl, lower alkenyl, and lower alkynyl, cycloalkyl, cycloalkenyl, haloalkyl, aryl, oxathiadiazole, alkylaryl, alkoxyalkyl, and thioalkoxyalkyl all optionally substituted by one or more of alkyl, hydroxy, alkoxy, halogen, haloalkyl, cyano, amino, and nitro;R.sup.3 is is selected from the group consisting of H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkenyl, aryl, oxathiadiazole, and alkylaryl, all optionally substituted by one or more of halogen, haloalkyl, cyano, nitro, --CO.sub.2 R, and --COR; orR.sup.3 is selected from the group consisting of alkylhydroxy, alkylpolyhydroxy, alkyl(poly)oxyacyl, CH.sub.2 C(.dbd.O)OR.sup.6, CH.sub.2 C(.dbd.O)NHR.sup.6, CH.sub.2 OC(.dbd.O)R.sup.6, and CH.sub.2 OC(.dbd.O)JR.sup.6, the CH.sub.2 is optionally substituted by one or more of lower alkyl, cycloalkyl, oxathiadiazole, aryl, amidino, guanidino, CO.sub.2 H, amino, hydroxy, thiol, halogen, haloalkyl, cyano, and nitro;J is selected from the group consisting of O, S, CH.sub.2, CHR.sup.6, C(R.sup.6).sub.2, NH, and NR.sup.6 ;R.sup.4 is selected from the group consisting of H, S(O)R.sup.7, SO.sub.2 R.sup.7, CH.sub.2 OC(O)--R.sup.7, and C(O)--R.sup.7 where C(O)--R.sup.7 represents amino acids or R.sup.7 is defined as below, or R.sup.4 and R.sup.3 taken together comprise a oxathiadiazole, optionally substituted with alkyl or oxygen, or taken together comprise a metal complex containing a divalent cation, or a boron complex;R.sup.5 is R.sup.6 or C(O)--R.sup.6 ;R.sup.6 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, oxathiadiazole, and aryl, all optionally substituted by one or more alkyl, hydroxy, alkoxy, halogen, trifluoromethyl, nitro, cyano, and amino groups;R.sup.7 is selected from the group consisting of substituted dihydropyridyl, alkyl, thioalkoxy, alkoxy, amino, and cycloalkoxy, all optionally substituted with one or more of amino, alkyl, alkylaryl, oxathiadiazole, and alkylmercaptoalkyl, which may optionally be substituted with one or more of hydroxy, amino, guanidino, and iminoalkyl;L is selected from the group consisting of lower alkylenes, lower alkenylenes and lower alkynylenes which may optionally be substituted by one or more alkyl, alkoxy, hydroxy, halogen, trifluoromethyl, nitro, cyano, and amino groups; orL 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, Se, Se(O).sub.g, SiE.sub.2 where E is lower alkyl, aryl, S(O).sub.g where g is 0, 1 or 2, or NR; orL 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 or oxathiadiazole, or aromatic ring which may optionally be substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino;X is selected from the group consisting of O, S(.dbd.O), and SO.sub.2 ;Y is a bond;Z is selected from the group consisting of O, S(.dbd.O), and SO.sub.2with the proviso that one of X or Z is O, and X.noteq.Z.