发明名称 HIV inhibiting pyrimidine derivatives
摘要 This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 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 R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is optionally 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 US8026248(B2) 申请公布日期 2011.09.27
申请号 US20050111358 申请日期 2005.04.21
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 A01N43/54;A61K31/505;C07D239/02;C07D239/42;C07D239/46;C07D239/48;C07D239/50;C07D401/00;C07D401/12;C07D403/00;C07D405/00;C07D409/00;C07D411/00;C07D413/00;C07D417/00;C07D419/00 主分类号 A01N43/54
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