Patent ID: 6197779
Filing Date: 2001-03-06
Classification: A61P,C07D

Abstract:
A method of treating Human Immunodeficiency Virus infection comprising administering to a subject in need thereof an effective amount of a compound of formula ##STR34##a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, whereinA is CH, CR.sup.4 or N;n is 0, 1, 2, 3 or 4;Q is hydrogen or --NR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently selected from hydrogen, hydroxy, C.sub.1-12 alkyl, C.sub.1-12 alkyloxy, C.sub.1-12 alkylcarbonyl, C.sub.1-12 alkyloxycarbonyl, aryl, amino, mono- or di(C.sub.1-12 alkyl)amino, mono- or di(C.sub.1-12 alkyl)aminocarbonyl wherein each of the aforementioned C.sub.1-12 alkyl groups may optionally and each individually be substituted with one or two substituents each independently selected from hydroxy, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkyloxycarbonyl, cyano, amino, imino, aminocarbonyl, aminocarbonylamino, mono- or di(C.sub.1-6 alkyl)amino, aryl and Het; orR.sup.1 and R.sup.2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C.sub.1-12 alkyl)aminoC.sub.1-4 alkylidene;R.sup.3 is hydrogen, aryl, C.sub.1-6 l alkylcarbonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkyl substituted with C.sub.1-6 alkyloxycarbonyl; andeach R.sup.4 independently is hydroxy, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, cyano, amino-carbonyl, nitro, amino, trihalomethyl, trihalomethyloxy or C.sub.1-6 alkyl substituted with cyano or aminocarbonyl;R.sup.5 is hydrogen or C.sub.1-4 alkyl;L is C.sub.1-10 alkyl, C.sub.3-10 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, or C.sub.1-10 alkyl substituted with one or two substituents independently selected from C.sub.3-7 cycloalkyl, indanyl, indolyl and phenyl, wherein said phenyl, indanyl and indolyl may be substituted with one, two, three, four or where possible five substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, cyano, aminocarbonyl, C.sub.1-6 alkyloxycarbonyl, formyl, nitro, amino, trihalomethyl, trihalomethyloxy and C.sub.1-6 alkylcarbonyl; orL is --X.sup.1 --R.sub.6 or X.sup.2 -Alk-R.sup.7 whereinR.sup.6 and R.sup.7 each independently are phenyl or phenyl substituted with one, two, three, four or five substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl, formyl, cyano, aminocarbonyl, nitro, amino, trihalomethyloxy and trihalomethyl; andX.sup.1 and X.sup.2 are each independently --NR.sup.3 --, --NH--NH--, --N.dbd.N--, --O--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2 --;Alk is C.sub.1-4 alkanediyl;aryl is phenyl or phenyl substituted with one, two, three, four or five substituents each independently selected from halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, cyano, nitro and trifluoromethyl;Het is an aliphatic or aromatic heterocyclic radical; said aliphatic heterocyclic radical is selected from pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, tetrahydrofuranyl and tetrahydrothienyl wherein each of said aliphatic heterocyclic radical may optionally be substituted with an oxo group; and said aromatic heterocyclic radical is selected from pyrrolyl, furanyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl and pyridazinyl wherein each of said aromatic heterocyclic radical may optionally be substituted with hydroxy.