发明名称 HIV replication inhibiting pyrimidines
摘要 This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a<1>=a<2>-a<3>=a<4>- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R<1 >is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R<2 >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)pR<6>, -NH-S(=O)pR<6>, -C(=O)R<6>, -NHC(=O)H, -C(=O)NHNH2, -NHC(=O)R<6>, -C(=NH)R<6 >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-R<3 >wherein R<3 >is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR<1>-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- or -S(=O)2-; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S(=O)pR<6>, -NH-S(=O)pR<6></highlig
申请公布号 US2004039005(A1) 申请公布日期 2004.02.26
申请号 US20030634682 申请日期 2003.08.05
申请人 DE CORTE BART;DE JONGE MARC RENE;HEERES JAN;HO CHIH YUNG;JAN JANSSEN PAUL ADRIAAN;KAVASH ROBERT W.;KOYMANS LUCIEN MARIA HENRICUS;KUKLA MICHAEL JOSEPH;LUDOVICI DONALD WILLIAM;VAN AKEN KOEN JEANNE ALFONS 发明人 DE CORTE BART;DE JONGE MARC RENE;HEERES JAN;HO CHIH YUNG;JAN JANSSEN PAUL ADRIAAN;KAVASH ROBERT W.;KOYMANS LUCIEN MARIA HENRICUS;KUKLA MICHAEL JOSEPH;LUDOVICI DONALD WILLIAM;VAN AKEN KOEN JEANNE ALFONS;KOENRAAD JOZEF LODEWIJK MARCEL ANDRIES
分类号 C07D239/47;A61K;A61K31/505;A61K31/506;A61K31/513;A61K31/551;A61K31/5513;A61K31/675;A61K31/715;A61P31/18;C07D;C07D239/42;C07D239/46;C07D239/48;C07D239/50;C07D239/80;C07D401/12;C07D403/12;(IPC1-7):A61K31/715 主分类号 C07D239/47
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