摘要 |
This invention concerns the use of the compounds of formula (1), the N-oxide s, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein - a1- a2-a3-a4 forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and whe re possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1- 6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono--or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, - S(=O)p R4, -NH-S(-O)p R4, -C(-O)R4, -NHC(-O)H, -C(=O)NHNH2, -NHC(-O)R4, -C(=NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is -X-R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR1-, -NH-NH-, -N-N-, -O-, -C(=O)-, -CHOH-, -S-, -S(-O )- or -S(=O)2-; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering fr om HIV (Human Immunodeficiency Virus) infection.
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申请人 |
JANSSEN PHARMACEUTICA, N.V. |
发明人 |
KOYMANS, LUCIEN MARIA HENRICUS;KUKLA, MICHAEL JOSEPH;HEERES, JAN;JANSSEN, PAUL ADRIAAN JAN;VAN AKEN, KOEN JEANNE ALFONS;KAVASH, ROBERT W.;LUDOVICI, DONALD WILLIAM;DE CORTE, BART;DE JONGE, MARC RENE |