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, CR<SUP>4 </SUP>or N; n is 0 to 4; Q is hydrogen or -NR<SUP>1</SUP>R<SUP>2</SUP>; R<SUP>1 </SUP>and R<SUP>2 </SUP>are selected from hydrogen, hydroxy, C<SUB>1-12</SUB>alkyl, C<SUB>1-12</SUB>alkyloxy, C<SUB>1-12</SUB>alkylcarbonyl, C<SUB>1-12</SUB>alkyloxycarbonyl, aryl, amino, mono- or di(C<SUB>1-12</SUB>alkyl)-amino, mono- or di(C<SUB>1-12</SUB>alkyl)aminocarbonyl wherein each C<SUB>1-12</SUB>alkyl may optionally be substituted; or R<SUP>1 </SUP>and R<SUP>2 </SUP>taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C<SUB>1-12</SUB>alkyl)aminoC<SUB>1-4</SUB>alkylidene; R<SUP>3 </SUP>is hydrogen, aryl. C<SUB>1-6</SUB>alkylcarbonyl, optionally substituted C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkyloxy-carbonyl; and R<SUP>4 </SUP>is hydroxy, halo, optionally substituted C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R<SUP>5 </SUP>is hydrogen or C<SUB>1-4</SUB>alkyl; L is optionally substituted C<SUB>1-10</SUB>alkyl, C<SUB>3-10</SUB>alkenyl, C<SUB>3-10</SUB>alkynyl, C<SUB>3-7</SUB>cycloalkyl; or L is -X<SUP>1</SUP>-R<SUP>6 </SUP>or -X<SUP>2</SUP>-Alk-R<SUP>7 </SUP>wherein R<SUP>6 </SUP>and R<SUP>7 </SUP>are optionally substituted phenyl; X<SUP>1 </SUP>and X<SUP>2 </SUP>are -NR<SUP>3</SUP>-, -NH-NH-, -N-N-, -O-, -S-, -S(-O)- or -S(-O)<SUB>2</SUB>-; Alk is C<SUB>1-4</SUB>alkanediyl; 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 US2005197354(A1) 申请公布日期 2005.09.08
申请号 US20050111358 申请日期 2005.04.21
申请人 ANDRIES KOENRAAD JOZEF L.M.;DE CORTE BART;DE JONGE MARC R.;HEERES JAN;HO CHIH Y.;JANSSEN MARCEL A.C.;JANSSEN PAUL A.J.;KOYMANS LUCIEN M.H.;KUKLA MICHAEL J.;LUDOVICI DONALD W.;VAN AKEN KOEN J.A. 发明人 ANDRIES KOENRAAD JOZEF L.M.;DE CORTE BART;DE JONGE MARC R.;HEERES JAN;HO CHIH Y.;JANSSEN MARCEL A.C.;JANSSEN PAUL A.J.;KOYMANS LUCIEN M.H.;KUKLA MICHAEL J.;LUDOVICI DONALD W.;VAN AKEN KOEN J.A.
分类号 C07D239/42;C07D239/46;C07D239/48;C07D239/50;C07D401/12;(IPC1-7):A61K31/506;C07D43/02 主分类号 C07D239/42
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