Non-nucleoside reverse transcriptase inhibitors

   
   

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 --(CHR.sub.8).sub.n- --D--(CHR.sub.8).sub.m --; D is --NR.sub.9 --, --O--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2 --; R.sub.8 is independently H, C.sub.1 -C.sub.3 alkyl, halo substitutedC.sub.1 -C.sub.3 alkyl; R.sub.9 is H, C.sub.1 -C.sub.3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.

Composés de la formule I : ## du ## STR1 là où ; R.sub.1 est O, S ; R.sub.2 est un heterocycle contenant de l'azote sur option substitué, où l'azote est situé à la position 2 relativement au (obligation de thio)urea ; R.sub.3 est H, C.sub.1 - C.sub.3 l'alkyl, R.sub.4 - R.sub.7 est indépendamment choisi parmi H, C.sub.1 - C.sub.6 l'alkyl, C.sub.2 - C.sub.6 l'alkényle, C.sub.2 - C.sub.6 l'alkynyl, haloC.sub.1 - C.sub.6 l'alkyl, C.sub.1 - C.sub.6 l'alkanoyl, haloC.sub.1 - C.sub.6 l'alkanoyl, C.sub.1 - C.sub.6 alcoxy, haloC.sub.1 - C.sub.6 alcoxy, 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, aminé, carboxy, carbamoyl, cyano, halo, hydroxy, cétonique ; X est -- (CHR.sub.8).sub.n- -- D -- le --; D de (CHR.sub.8).sub.m est -- --O de NR.sub.9 --. --. --S --. -- S(.dbd.O) -- ou -- S(.dbd.O).sub.2 le --; R.sub.8 est indépendamment H, C.sub.1 - C.sub.3 l'alkyl, le halo substitutedC.sub.1 - alkyl C.sub.3 ; R.sub.9 est H, C.sub.1 - l'alkyl C.sub.3 ; n et m sont indépendamment 0, 1 ou 2 ; et les prodrogues et pharmaceutiquement les sels acceptables en, ont l'utilité car des inhibiteurs du transcriptase HIV-1 renversé, en particulier mutants d'évasion de drogue.

 
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