| abstract |
Invention Patent: <B> "HIV REPRODUCTION INHIBITOR PYRIMIDINES" <D>. This invention deals with the use of compounds of the formula (I), N-oxides, pharmaceutically acceptable addition salts, quaternary amines and their stereochemically isomeric form, where a ^ 1 ^ = a ^ 2 ^ = a ^ 3 ^ = a ^ 4 ^ - forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the aggregated vinyl group; n is 0 to 4; and where possible 5; R ^ 1 ^ is hydrogen, aryl, formyl, C ~ 1-6 ~ alkylcarbonyl, C ~ 1-6 ~ alkyl, C ~ 1-6 ~ alkyloxycarbonyl, C ~ 1-6 ~ substituted alkyl or C ~ 1-6 ~ C 1-4 alkyloxy substituted alkylcarbonyl; each R3 independently is hydroxy, halo, optionally substituted C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl or C ~ 2-6 ~ -alkynyl, C ~ 3-7 ~ cycloalkyl, C ~ 1-6 ~ alkyloxy , C ~ 1-6 ~ alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di (C ~ 1-6 ~ alkyl) amino, polyhalomethyl, polyhalo-methyloxy, polyhalomethylthio, -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 heterocyclic ring; p is 1 or 2; L is optionally substituted by C ~ 1-10 ~ alkyl, C ~ 2-10 ~ alkenyl or C ~ 3-7 ~ cycloalkyl; or L is -XR ^ 3 ^ where R ^ 3 ^ is phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl, optionally substituted X is -NR ^ 1 ^ -, -NH-NH-, -N = N, -O-, C (= O) -CHOH-, -S-, -S (= O) - or -S (= O) ~ 2 ~ -; Q is hydrogen, C ~ 1-6 ~ alkyl, halo, polyhalo-C ~ 1-6 ~ alkyl or an optionally substituted group; Y represents hydroxy, C ~ 3-7 ~ cycloalkyl, C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl or C ~ 2-6 ~ alkyl, optionally substituted, C ~ 1-6 ~ alkyloxy, C ~ 1-6 ~ alkyloxycarbonyl, carbonyl, cyano, nitro, amino, mono- or di (C ~ 1-6 ~ alkyl) amino, polyhalo-methyl, polyhalomethyloxy, polyhalomethio, -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 aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of patients suffering from HIV infection (Human Immunodeficiency Virus). |