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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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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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.</description><language>eng</language><creationdate>2002</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://image-ppubs.uspto.gov/dirsearch-public/print/downloadPdf/6440986$$EPDF$$P50$$Guspatents$$Hfree_for_read</linktopdf><link.rule.ids>230,308,780,802,885,64037</link.rule.ids><linktorsrc>$$Uhttps://image-ppubs.uspto.gov/dirsearch-public/print/downloadPdf/6440986$$EView_record_in_USPTO$$FView_record_in_$$GUSPTO$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Andries, Koenraad Jozef Lodewijk Marcel</creatorcontrib><creatorcontrib>De Corte, Bart</creatorcontrib><creatorcontrib>De Jonge, Marc René</creatorcontrib><creatorcontrib>Heeres, Jan</creatorcontrib><creatorcontrib>Ho, Chih Yung</creatorcontrib><creatorcontrib>Janssen, Marcel August Constant</creatorcontrib><creatorcontrib>Janssen, Paul Adriaan Jan</creatorcontrib><creatorcontrib>Koymans, Lucien Maria Henricus</creatorcontrib><creatorcontrib>Kukla, Michael Joseph</creatorcontrib><creatorcontrib>Ludovici, Donald William</creatorcontrib><creatorcontrib>Van Aken, Koen Jeanne Alfons</creatorcontrib><creatorcontrib>Janssen Pharmaceutica, N.V</creatorcontrib><title>HIV Inhibiting pyrimidine derivatives</title><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.</description><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2002</creationdate><recordtype>patent</recordtype><sourceid>EFH</sourceid><recordid>eNrjZFD18AxT8MzLyEzKLMnMS1coqCzKzM1MycxLVUhJLcosSyzJLEst5mFgTUvMKU7lhdLcDApuriHOHrqlxQWJJal5JcXx6UWJIMrAzMTEwNLCzJgIJQAbWSgw</recordid><startdate>20020827</startdate><enddate>20020827</enddate><creator>Andries, Koenraad Jozef Lodewijk Marcel</creator><creator>De Corte, Bart</creator><creator>De Jonge, Marc René</creator><creator>Heeres, Jan</creator><creator>Ho, Chih Yung</creator><creator>Janssen, Marcel August Constant</creator><creator>Janssen, Paul Adriaan Jan</creator><creator>Koymans, Lucien Maria Henricus</creator><creator>Kukla, Michael Joseph</creator><creator>Ludovici, Donald William</creator><creator>Van Aken, Koen Jeanne Alfons</creator><scope>EFH</scope></search><sort><creationdate>20020827</creationdate><title>HIV Inhibiting pyrimidine derivatives</title><author>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</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-uspatents_grants_064409863</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2002</creationdate><toplevel>online_resources</toplevel><creatorcontrib>Andries, Koenraad Jozef Lodewijk Marcel</creatorcontrib><creatorcontrib>De Corte, Bart</creatorcontrib><creatorcontrib>De Jonge, Marc René</creatorcontrib><creatorcontrib>Heeres, Jan</creatorcontrib><creatorcontrib>Ho, Chih Yung</creatorcontrib><creatorcontrib>Janssen, Marcel August Constant</creatorcontrib><creatorcontrib>Janssen, Paul Adriaan Jan</creatorcontrib><creatorcontrib>Koymans, Lucien Maria Henricus</creatorcontrib><creatorcontrib>Kukla, Michael Joseph</creatorcontrib><creatorcontrib>Ludovici, Donald William</creatorcontrib><creatorcontrib>Van Aken, Koen Jeanne Alfons</creatorcontrib><creatorcontrib>Janssen Pharmaceutica, N.V</creatorcontrib><collection>USPTO Issued Patents</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Andries, Koenraad Jozef Lodewijk Marcel</au><au>De Corte, Bart</au><au>De Jonge, Marc René</au><au>Heeres, Jan</au><au>Ho, Chih Yung</au><au>Janssen, Marcel August Constant</au><au>Janssen, Paul Adriaan Jan</au><au>Koymans, Lucien Maria Henricus</au><au>Kukla, Michael Joseph</au><au>Ludovici, Donald William</au><au>Van Aken, Koen Jeanne Alfons</au><aucorp>Janssen Pharmaceutica, N.V</aucorp><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>HIV Inhibiting pyrimidine derivatives</title><date>2002-08-27</date><risdate>2002</risdate><abstract>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.</abstract><oa>free_for_read</oa></addata></record> |
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title | HIV Inhibiting pyrimidine derivatives |
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