HIV Inhibiting pyrimidine derivatives

The present invention is concerned with pyrimidine derivatives having HIV replication inhibiting properties. The invention further relates to methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of said compounds in the manufacture of a...

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Hauptverfasser: Andries, Koenraad Jozef Lodewijk Marcel, De Corte, Bart, De Jonge, Marc René, 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
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creator Andries, Koenraad Jozef Lodewijk Marcel
De Corte, Bart
De Jonge, Marc René
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
description The present invention is concerned with pyrimidine derivatives having HIV replication inhibiting properties. The invention further relates to methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of said compounds in the manufacture of a medicament useful for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. 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, CRor N; n is 0 to 4; Q is hydrogen or -NRR; Rand Rare selected from hydrogen, hydroxy, Calkyl, Calkyloxy, Calkylcarbonyl, Calkyloxycarbonyl, aryl, amino, mono- or di(Calkyl)amino, mono- or di(Calkyl)aminocarbonyl wherein each Calkyl may optionally be substituted; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)aminoCalkylidene; Ris hydrogen, aryl, Calkylcarbonyl, optionally substituted Calkyl, Calkyloxycarbonyl,; and Ris hydroxy, halo, optionally substituted Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; Ris hydrogen or Calkyl; L is optionally substituted Calkyl, Calkenyl, Calkynyl, Ccycloalkyl; or L is -X-Ror -X-Alk-Rwherein Rand Rare optionally substituted phenyl; Xand Xare -NR-, -NH-NH-, -N N-, -O-, -S-, -S( O)- or -S( O)-; Alk is Calkanediyl; 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.
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The invention further relates to methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of said compounds in the manufacture of a medicament useful for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. 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, CRor N; n is 0 to 4; Q is hydrogen or -NRR; Rand Rare selected from hydrogen, hydroxy, Calkyl, Calkyloxy, Calkylcarbonyl, Calkyloxycarbonyl, aryl, amino, mono- or di(Calkyl)amino, mono- or di(Calkyl)aminocarbonyl wherein each Calkyl may optionally be substituted; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)aminoCalkylidene; Ris hydrogen, aryl, Calkylcarbonyl, optionally substituted Calkyl, Calkyloxycarbonyl,; and Ris hydroxy, halo, optionally substituted Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; Ris hydrogen or Calkyl; L is optionally substituted Calkyl, Calkenyl, Calkynyl, Ccycloalkyl; or L is -X-Ror -X-Alk-Rwherein Rand Rare optionally substituted phenyl; Xand Xare -NR-, -NH-NH-, -N N-, -O-, -S-, -S( O)- or -S( O)-; Alk is Calkanediyl; 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. 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The invention further relates to methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of said compounds in the manufacture of a medicament useful for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. 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, CRor N; n is 0 to 4; Q is hydrogen or -NRR; Rand Rare selected from hydrogen, hydroxy, Calkyl, Calkyloxy, Calkylcarbonyl, Calkyloxycarbonyl, aryl, amino, mono- or di(Calkyl)amino, mono- or di(Calkyl)aminocarbonyl wherein each Calkyl may optionally be substituted; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)aminoCalkylidene; Ris hydrogen, aryl, Calkylcarbonyl, optionally substituted Calkyl, Calkyloxycarbonyl,; and Ris hydroxy, halo, optionally substituted Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; Ris hydrogen or Calkyl; L is optionally substituted Calkyl, Calkenyl, Calkynyl, Ccycloalkyl; or L is -X-Ror -X-Alk-Rwherein Rand Rare optionally substituted phenyl; Xand Xare -NR-, -NH-NH-, -N N-, -O-, -S-, -S( O)- or -S( O)-; Alk is Calkanediyl; 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.</abstract><oa>free_for_read</oa></addata></record>
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title HIV Inhibiting pyrimidine derivatives
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