发明名称 HIV inhibiting pyrimidine derivatives
摘要 This invention concerns the use of the compounds of formula <CHEM> the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR<4> or N; n is 0 to 4; Q is hydrogen or -NR<1>R<2>; R<1> and R<2> are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R<1> and R<2> taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R<3> is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R<4> is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R<5> is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is -X<1>-R<6> or -X<2>-Alk-R<7> wherein R<6> and R<7> are optionally substituted phenyl; X<1> and X<2> are -NR<3>-, -NH-NH-, -N=N-, -O-, -S-, -S(=O)- or -S(=O)2-; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.
申请公布号 EP0945443(A1) 申请公布日期 1999.09.29
申请号 EP19990200918 申请日期 1999.03.24
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL;DE CORTE, BART;DE JONGE, MARC RENE;HEERES, JAN;HO, CHIH YUNG;JANSSEN, MARCEL AUGUST CONSTANT;JANSSEN, PAUL ADRIAAN JAN;KOYMANS, LUCIEN MARIA HENRICUS;KUKLA, MICHAEL JOSEPH;LUDOVICI, DONALD WILLIAM;VAN AKEN, KOEN JEANNE ALFONS
分类号 A61K31/505;A61K31/506;A61P31/12;A61P31/18;A61P37/00;C07D239/42;C07D239/46;C07D239/47;C07D239/48;C07D239/50;C07D401/12;C07D409/12 主分类号 A61K31/505
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