Frederik Frans Desire Daeyaert,Hendrik Maarten Vinkers,Jan Heeres,Jerome Emile Georges Guillemont,Koen Jeanne Alfons Van Aken,Lucien Maria Henricus Koymans,Marc Renede Jonge,PAULUS JOANNES LEWI,Patric
申请号：
BRPI0211909
公开号：
BRPI0211909B1
申请日:
2002.08.09
申请国别(地区):
BR
年份:
2018
代理人:
摘要：
"hiv-inhibiting pyrimidine derivatives". The present invention relates to hiv replication inhibitors of formula (I), n-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof wherein the ring containing -a ^ 1 ^ = a ^ 2 ^ -a ^ 3 ^ = a ^ 4 ^ - and -b ^ 1 ^ = b ^ 2 ^ -b ^ 3 ^ = b ^ 4 ^ - represents phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl； n is from 0 to 5, m is from 1 to 4； R2 is hydrogen； arila； formyl； C 1-6 alkylcarbonyl； C 1-6 alkyl； C 1-6 alkyloxycarbonyl； substituted C 1-6 alkyl； C 1-6 alkylcarbonyl； R 2 is hydroxy, halo, optionally substituted C 1-6 alkyl, C 3-7 cycloalkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, C 1-6 alkyloxy 1-6-, C1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di (C1-6 alkyl) amino, polyhalomethyl, polyalomethyloxy, polyalomethyl, -s (= o) ~ p ~ r ^ 6 ^, -nh-s (= o) ~ p ~ r ^ 6 ^, -c (= o) r ^ 6 ^, -nhc (= o) h, -c (= o) nhnh ~ 2 -, -nhc (= o) r ^ 6 ^, -c (= nh) r ^ 6 ^ or a 5 membered heterocycle； x ~ 1 ~ is -nr ^ 5 ^ -, -nh-nh-, -n = n-, -o-, -c (= o) -, C 1-4 alkanediyl, -choh-, -s -, -s (= o) ~ p - -, -x-2-alkanediyl C 1-4 - or alkanediyl C 1-4 - x -2 - -； R ^ 3 ^ is nhr ^ 13 ^； nr ^ 13 ^ r ^ 14 ^； -c (= o) -nhr ^ 13 ^； -c (= o) -nr ^ 13 ^ r ^ 14 ^； -c (= o) -r ^ 15 ^； -c = n-nh-c (= o) -r ^ 16 ^； substituted C 1-6 alkyl； optionally substituted C1-6 alkyloxy C1-6 alkyl； substituted C 2-6 alkenyl； substituted C 2-6 alkynyl； hydroxy substituted C1-6 alkyl and a second substituent； -C (= n-o-R 8) alkyl-C 1-4； R 7 or R 3 -R 7； R 4 is halo, hydroxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, cyano, nitro, C 1-6 polyalkylalkyl, polyalkyloxyoxy C 1-6, aminocarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonyl, formyl, amino, mono- or di (C 1-4 alkyl) amino； their use as a medicament, processes for their preparation and pharmaceutical compositions comprising them."derivados de pirimidina que inibem o hiv". a presente inv
