2,4-pyrimidinedione derivatives of formula (I) having high antiviral
activity against wild-type and mutant HIV-1 and low toxicity are useful
for treating AIDS (I) wherein: R.sup.1 is a C.sub.6-10 aryl or C.sub.3-10
heteroaryl group optionally having one or more substituents selected from
the group consisting of halogen, C.sub.1-6 alkyl, C.sub.1-6 alkyl
substituted with one or more halogen atoms, C.sub.3-4 cycloalkyl, cyano,
nitro, hydroxy, thiohydroxy, azido, C.sub.1-6 alkoxy, oximino, C.sub.1-3
alkyloximino, O--(C.sub.1-6 alkyl)-substituted oximino, C--.sub.1-6
alkylcarbonyl, C.sub.3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethlyl,
C.sub.1-6 alkoxymethyl, C.sub.1-6 acyloxynethyl, carbamoyloxymethyl,
anminomethyl, N--(C.sub.1-3 alkyl)aminomethyl, N,N-di(C.sub.1-3
alkyl)aminomethyl, carboxy, C.sub.1-6 alkoxycarbonyl, aziridine, amino,
hydroxyethylamino, cyclopropylamino, C.sub.1-6 alkylamino, di(C.sub.1-6
alkyl)amino, trifluoroacetamido, C.sub.1-6 acylamido, carbamoyl,
hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C.sub.1-6 alkylcarbamoyl,
di(C.sub.1-6 alkyl)carbamoyl, aminocarbamoyl, dimethylaminocarbamoyl,
hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl and tetrazolyl; a
tetrahydropyridyl or piperidyl group optionally substituted with a
C.sub.1-6 alkyl or C.sub.1-6 alkoxycarbonyl group; a tetrahydropyranyl
group; or a tetrahydrofuryl group; R.sup.2 is hydrogen, halogen, nitro,
cyano, C.sub.1-3 alkoxycarbonyl, C.sub.1-3 alkylamino, di(C.sub.1-3
alkyl)amino, C.sub.1-3 alkylcarbamol, di(C.sub.1-3 alkyl)carbamoyl,
C.sub.1-3 alkyl, C.sub.3-6 cycloalkyl or benzyl; R.sup.3 and R.sup.4 are
each independently hydrogen, halogen, hydroxy, cyano, nitro, amino
acetamido, trifluoroacetamido, azido, C.sub.1-3 alkyl, C-.sub.1-3 alkyl
substituted with one or more halogen atoms, C.sub.1-3 alkoxycarbonyl,
carbamoyl C.sub.1-3 alkylcarbamoyl, di(C.sub.1-3 alkyl) carbamoyl or
C-.sub.1-3 alkoxy; A is O or S; and Z is O, S, C.dbd.O, NH or CH.sub.2.
##STR1##
производные 2,4-pyrimidinedione формулы (I) имея высокую противовирусную деятельность против одичал-tipa и мутанта HIV-1 и низкой токсичности полезны для обрабатывать AIDS (I) при котором: R.sup.1 будет группой арила C.sub.6-10 или heteroaryl C.sub.3-10 опционно имея one or more заместители выбранные от галоида группы consist of, C.sub.1-6 алкила, C.sub.1-6 алкил замененный с one or more атомами галоида, C.sub.3-4 cycloalkyl, cyano, нитро, окси, thiohydroxy, azido, C.sub.1-6 алкоксидное, oximino, C.sub.1-3 alkyloximino, о -- (C.sub.1-6 алкыл)-zamenennoe oximino, ч -- .sub.1-6 alkylcarbonyl, C.sub.3-6 cycloalkylcarbonyl, оксиметильное, azidomethlyl, C.sub.1-6 alkoxymethyl, C.sub.1-6 acyloxynethyl, carbamoyloxymethyl, anminomethyl, н -- (C.sub.1-3 alkyl)aminomethyl, н, N-di(C.sub.1-3 alkyl)aminomethyl, carboxy, C.sub.1-6 alkoxycarbonyl, aziridine, амино, hydroxyethylamino, cyclopropylamino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, trifluoroacetamido, C.sub.1-6 acylamido, carbamoyl, alkyl)carbamoyl di(C.sub.1-6, aminocarbamoyl, dimethylaminocarbamoyl, hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl и tetrazolyl; группа tetrahydropyridyl или piperidyl опционно заменила с группой алкила C.sub.1-6 или alkoxycarbonyl C.sub.1-6; группа tetrahydropyranyl; или группа tetrahydrofuryl; R.sup.2 водоподом, галоидом, нитро, cyano, alkoxycarbonyl C.sub.1-3, alkylamino C.sub.1-3, alkyl)amino di(C.sub.1-3, alkylcarbamol C.sub.1-3, alkyl)carbamoyl di(C.sub.1-3, алкил C.sub.1-3, cycloalkyl C.sub.3-6 или бензиловое; R.sup.3 и R.sup.4 каждое независимо acetamido водопода, галоида, окси, cyano, нитро, амино, trifluoroacetamido, azido, алкил C.sub.1-3, алкил C-.sub.1-3 замененные с carbamoyl one or more атомов, alkoxycarbonyl C.sub.1-3, carbamoyl C.sub.1-3 alkylcarbamoyl, алкила di(C.sub.1-3) или C-.sub.1-3 галоида алкоксидного; А будет о или с; и з будет о, с, C.dbd.O, nh или CH.sub.2. ## ## STR1
