This invention concerns the use of compounds of formula:
##STR1##
the N-oxides, the pharmaceutically acceptable addition salts, quaternary
amines and the stereochemically isomeric forms thereof, wherein -a.sup.1
=-a.sup.2 -a.sup.3 =a.sup.4 - forms a phenyl, pyridinyl, pyrimidinyl,
pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and
where possible 5; R.sup.1 is hydrogen, aryl, formyl, C.sub.1-6
alkylcarbonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy-carbonyl, substituted
C.sub.1-6 alkyl, or substituted C.sub.1-6 alkyloxyC.sub.1-6 alkylcarbonyl;
each R.sup.2 independently is hydroxy, halo, optionally substituted
C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, C.sub.3-7
cycloalkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkyloxycarbonyl, carboxyl,
cyano, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, polyhalomethyl,
polyhalomethyloxy, polyhalo-methylthio, --S(.dbd.O).sub.p R.sup.6,
--NH--S(.dbd.O).sub.p R.sup.6, --C(.dbd.O)R.sup.6, --NHC(.dbd.O)H,
--C(.dbd.O)NHNH.sub.2, --NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or a
5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted
C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl or C.sub.3-7
cycloalkyl; or L is --X--R.sup.3 wherein R.sup.3 is optionally substituted
phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is --NR.sup.1
--, --NH--NH--, --N.dbd.N--, --O--, --C(.dbd.O)--, --CHOH--, --S--,
--S(.dbd.O)-- or --S(.dbd.O).sub.2 --; Q is hydrogen, C.sub.1-6 alkyl,
halo, polyhalo-C.sub.1-6 alkyl or an optionally substituted amino group; Y
represents hydroxy, halo, C.sub.3-7 cycloalkyl, optionally substituted
C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, C.sub.1-6
alkyloxy, C.sub.1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-
or di(C.sub.1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy,
polyhalomethylthio, --S(.dbd.O).sub.p R.sup.6, --NH--S(.dbd.O).sub.p
R.sup.6, --C(.dbd.O)R.sup.6, --NHC(.dbd.O)H, --C(.dbd.O)NHNH.sub.2,
--NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or aryl; aryl is optionally
substituted phenyl; Het is an optionally substituted heterocyclic radical;
for the manufacture of a medicine for the treatment of subjects suffering
from HIV (Human Immunodeficiency Virus) infection.
Esta invenção concerne o uso dos compostos da fórmula: ## do ## STR1 os N-óxidos, os sais pharmaceutically aceitáveis da adição, amines quaternary e os formulários stereochemically isomeric disso, wherein - a.sup.1 = - a.sup.2 -- a.sup.3 = a.sup.4 - formulários um phenyl, pyridinyl, pyrimidinyl, pyridazinyl ou pyrazinyl com o grupo unido do vinil; n é 0 a 4; e onde 5 possíveis; R.sup.1 é hidrogênio, arilo, formyl, alkylcarbonyl C.sub.1-6, alkyl C.sub.1-6, alkyloxy-alkyloxy-carbonyl C.sub.1-6, o alkyl C.sub.1-6 substituído, ou alkylcarbonyl substituído de C.sub.1-6 alkyloxyC.sub.1-6; cada R.sup.2 é independentemente hydroxy, halo, o alkyl C.sub.1-6, o alkenyl C.sub.2-6 ou o alkynyl C.sub.2-6, o cycloalkyl C.sub.3-7, o alkyloxy C.sub.1-6, o alkyloxycarbonyl C.sub.1-6, carboxyl, cyano, nitro, amino, mono- opcionalmente substituídos ou di(C.sub.1-6 o alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-polyhalo-methylthio, -- S(.dbd.O).sub.p R.sup.6, -- NH -- S(.dbd.O).sub.p R.sup.6, -- C(.dbd.O)R.sup.6, -- NHC(.dbd.O)H, -- C(.dbd.O)NHNH.sub.2, -- NHC(.dbd.O)R.sup.6, -- C(.dbd.NH)R.sup.6 ou um anel 5-membered heterocyclic; p é 1 ou 2; L é opcionalmente o alkyl C.sub.1-10, o alkenyl C.sub.2-10, o alkynyl C.sub.2-10 ou o cycloalkyl C.sub.3-7 substituído; ou L é -- X -- R.sup.3 wherein R.sup.3 é opcionalmente phenyl, pyridinyl, pyrimidinyl, pyrazinyl ou pyridazinyl substituído; X são -- NR.sup.1 --. -- nh -- nh --. -- --O --. de N.dbd.N --. -- C(.dbd.O) --. -- --S do choh --. --. -- S(.dbd.O) -- ou -- S(.dbd.O).sub.2 o --; Q é hidrogênio, alkyl C.sub.1-6, halo, alkyl polyhalo-C.sub.1-6 ou um amino grupo opcionalmente substituído; Y representa hydroxy, o halo, o cycloalkyl C.sub.3-7, o alkyl C.sub.1-6, o alkenyl C.sub.2-6 ou o alkynyl C.sub.2-6, o alkyloxy C.sub.1-6, o alkyloxycarbonyl C.sub.1-6, carboxyl, cyano, nitro, amino, mono- opcionalmente substituídos ou di(C.sub.1-6 o alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -- S(.dbd.O).sub.p R.sup.6, -- NH -- S(.dbd.O).sub.p R.sup.6, -- C(.dbd.O)R.sup.6, -- NHC(.dbd.O)H, -- C(.dbd.O)NHNH.sub.2, -- NHC(.dbd.O)R.sup.6, -- C(.dbd.NH)R.sup.6 ou arilo; o arilo é opcionalmente phenyl substituído; Het é um radical heterocyclic opcionalmente substituído; para a manufatura de uma medicina para o tratamento dos assuntos que sofrem da infecção do HIV (vírus humano do immunodeficiency).
