Patent ID: 6344473
Filing Date: 2002-02-05
Classification: C07D

Abstract:
A compound having the formula; and pharmaceutially 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, heterocycle, aryl, alkylaryl, and alkylheterocycle, all optionally substituted by one or more of alkyl, hydroxy, alkoxy, halogen, haloalkyl, cyano, amino, and nitro; or NR together form a heterocyclic; R1 is selected from the group consisting of hydrogen, lower alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl, heterocycle, aryl, alkylaryl, and alkylheterocycle, all optionally substituted by one or more of alkyl, hydroxy, alkoxy, halogen, haloalkyl, cyano, amino, and nitro; R2 is selected from the group consisting of amino, thioalkoxy, alkoxy, lower alkyl, lower alkenyl, and lower alkynyl, cycloalkyl, cycloalkenyl, haloalkyl, aryl, heterocycle, alkylaryl, alkylheterocycle, alkoxyalkyl, and thioalkoxyalkyl all optionally substituted by one or more of alkyl, hydroxy, alkoxy, halogen, haloalkyl, cyano, amino, and nitro; R3 is selected from the group consisting of H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocycle, alkylaryl, and alkylheterocycle, all optionally substituted by one or more of halogen, haloalkyl, cyano, nitro, â€”CO2R, and â€”COR; or R3 is selected from the group consisting of alkylhydroxy, alkylpolyhydroxy, alkyl(poly)oxyacyl, CH2C(&boxH;O)OR6, CH2C(&boxH;O)NHR6, CH2OC(&boxH;O)R6, and CH2OC(&boxH;O)JR6, the CH2 is optionally substituted by one or more of lower alkyl, cycloalkyl, heterocycle, aryl, amidino, guanidino, CO2H, amino, hydroxy, thiol, halogen, haloalkyl, cyano, and nitro; J is selected from the group consisting of O, S, CH2, CHR6, C(R6)2, NH, and NR6; R4 is selected from the group consisting of H, S(O)R7, SO2R7, CH2OC(O)â€”R7, and C(O)â€”R7 where C(O)â€”R7 represents amino acids or R7 is defined as below, or R4 and R3 taken together comprise a 5- or 6-membered heterocyclic ring containing two or more heteroatoms, optionally substituted with alkyl or oxygen, or taken together comprise a metal complex containing a divalent cation, or a boron complex; R5 is R6 or C(O)â€”R6; R6 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycle, and aryl, all optionally substituted by one or more alkyl, hydroxy, alkoxy, halogen, trifluoromethyl, nitro, cyano, and amino groups; R7 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, heterocycle, alkylheterocycle, 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; or L is selected from the group consisting of the formula â€”(CH2)kQ(CH2)tâ€” where k is 1, 2 or 3, t is 1, 2 or 3 and Q is O, Se, Se(O)g, SiE2 where E is lower alkyl, aryl, S(O)g where g is 0,1 or 2, or NR; or L is selected from the group consisting of the formula â€”(CH2)mT(CH2)nâ€” where m is 0, 1 or 2, n is 0, 1 or 2, T is a 3 to 6 membered carbocyclic or heterocyclic ring, 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 C(&boxH;O), C(&boxH;S), C&boxH;C(R6)2, and C(R6)2; Y is a bond Z is selected from the group consisting of C(&boxH;O), C(&boxH;S), C&boxH;C(R6)2, and C(R6)2.