Compounds of the formula I:
##STR1##
where;
R.sub.1 is O, S;
R.sub.2 is an optionally substituted nitrogen-containing heterocycle,
wherein the nitrogen is located at the 2 position relative to the
(thio)urea bond;
R.sub.3 is H, C.sub.1 -C.sub.3 alkyl,
R.sub.4 -R.sub.7 are independently selected from H, C.sub.1 -C.sub.6 alkyl,
C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, haloC.sub.1 -C.sub.6
alkyl, C.sub.1 -C.sub.6 alkanoyl, haloC.sub.1 -C.sub.6 alkanoyl, C.sub.1
-C.sub.6 alkoxy, haloC.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6
alkyloxy-C.sub.1 -C.sub.6 alkyl, haloC.sub.1 -C.sub.6 alkyloxy-C.sub.1
-C.sub.6 alkyl hydroxy-C.sub.1 -C.sub.6 alkyl, amino-C.sub.1 -C.sub.6
alkyl, carboxy-C.sub.1 -C.sub.6 alkyl, cyano-C.sub.1 -C.sub.6 alkyl,
amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto;
X is --(CR.sub.8 R.sub.9).sub.n --
R.sub.8 and R.sub.9 are independently H, C.sub.1 -C.sub.3 alkyl, OH or
R.sub.8 and R.sub.9 together are .dbd.O
n is 1, 2 or 3
and prodrugs and pharmaceutically acceptable salts thereof, have utility as
inhibitors of HIV-1 reverse transcriptase, particularly drug escape
mutants.
Смеси формулы iego: ## ## STR1 где; R.sub.1 будет о, с; R.sub.2 будет опционно замененным nitrogen-containing heterocycle, при котором азот расположен на положении 2 по отношению к (скрепление thio)urea; R.sub.3 будет ю, C.sub.1 - C.sub.3 алкилом, R.sub.4 - R.sub.7 независимо выбрано от ю, C.sub.1 - C.sub.6 алкила, C.sub.2 - C.sub.6 алкенил, C.sub.2 - C.sub.6 alkynyl, haloC.sub.1 - C.sub.6 алкил, C.sub.1 - C.sub.6 alkanoyl, haloC.sub.1 - C.sub.6 alkanoyl, C.sub.1 - C.sub.6 алкоксидное, haloC.sub.1 - C.sub.6 алкоксидное, C.sub.1 - C.sub.6 alkyloxy-C.sub.1 - C.sub.6 алкил, haloC.sub.1 - C.sub.6 alkyloxy-C.sub.1 - C.sub.6 алкил hydroxy-C.sub.1 - C.sub.6 алкил, amino-C.sub.1 - C.sub.6 алкил, carboxy-C.sub.1 - C.sub.6 алкил, cyano-C.sub.1 - C.sub.6 алкил, амино, carboxy, carbamoyl, cyano, венчик, окси, keto; X будет -- (CR.sub.8 R.sub.9).sub.n -- R.sub.8 и R.sub.9 будут независимо ю, C.sub.1 - алкил C.sub.3, oh или R.sub.8 и R.sub.9 совместно будут dbd.O н 1, 2 или 3 и prodrugs и фармацевтически приемлемо соли thereof, имеют общее назначение по мере того как иы АБС битор обратного transcriptase HIV-1, определенно мутанты избежания снадобья.
