HIV INHIBITING 1.2.4-TRIAZIN-6-ONE DERIVATES
The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to...
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creator | DE JONGE, MARC RENE VINKERS, HENDRIK MAARTEN JANSSEN, PAUL ADRIAAN JAN HEERES, JAN DAEYAERT, FREDERIK F. D KILONDA, AMURI KOYMANS, LUCIEN MARIA H LEWI, PAULUS JOANNES HOORNAERT, GEORGES J. C |
description | The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; -S( O)pR6; -NH-S( O)pR6; -C( O)R6; -NHC( O)H; -C( O)NHNH2; NHC( O)R6; C( NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; -C( O)-NHR13; -C( O)-NR13R14; -C( O)-R15; -CH N-NH-C( O)-R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 or X2 represents -NR1-; -NH-NH-; -N N-; -O-; -C( O)-; -C1-4alkanediyl-; -CHOH-; -S-; -S( O)p-; -X4-C1-4alkanediyl-; -C1-4alkanediyl-X4-; or -C1-4alkanediyl-X4-C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them. |
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C</creator><creatorcontrib>DE JONGE, MARC RENE ; VINKERS, HENDRIK MAARTEN ; JANSSEN, PAUL ADRIAAN JAN ; HEERES, JAN ; DAEYAERT, FREDERIK F. D ; KILONDA, AMURI ; KOYMANS, LUCIEN MARIA H ; LEWI, PAULUS JOANNES ; HOORNAERT, GEORGES J. C</creatorcontrib><description>The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; -S( O)pR6; -NH-S( O)pR6; -C( O)R6; -NHC( O)H; -C( O)NHNH2; NHC( O)R6; C( NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; -C( O)-NHR13; -C( O)-NR13R14; -C( O)-R15; -CH N-NH-C( O)-R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 or X2 represents -NR1-; -NH-NH-; -N N-; -O-; -C( O)-; -C1-4alkanediyl-; -CHOH-; -S-; -S( O)p-; -X4-C1-4alkanediyl-; -C1-4alkanediyl-X4-; or -C1-4alkanediyl-X4-C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.</description><language>eng ; fre ; ger</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2013</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20131023&DB=EPODOC&CC=EP&NR=1797050B1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76293</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20131023&DB=EPODOC&CC=EP&NR=1797050B1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>DE JONGE, MARC RENE</creatorcontrib><creatorcontrib>VINKERS, HENDRIK MAARTEN</creatorcontrib><creatorcontrib>JANSSEN, PAUL ADRIAAN JAN</creatorcontrib><creatorcontrib>HEERES, JAN</creatorcontrib><creatorcontrib>DAEYAERT, FREDERIK F. D</creatorcontrib><creatorcontrib>KILONDA, AMURI</creatorcontrib><creatorcontrib>KOYMANS, LUCIEN MARIA H</creatorcontrib><creatorcontrib>LEWI, PAULUS JOANNES</creatorcontrib><creatorcontrib>HOORNAERT, GEORGES J. C</creatorcontrib><title>HIV INHIBITING 1.2.4-TRIAZIN-6-ONE DERIVATES</title><description>The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; -S( O)pR6; -NH-S( O)pR6; -C( O)R6; -NHC( O)H; -C( O)NHNH2; NHC( O)R6; C( NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; -C( O)-NHR13; -C( O)-NR13R14; -C( O)-R15; -CH N-NH-C( O)-R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 or X2 represents -NR1-; -NH-NH-; -N N-; -O-; -C( O)-; -C1-4alkanediyl-; -CHOH-; -S-; -S( O)p-; -X4-C1-4alkanediyl-; -C1-4alkanediyl-X4-; or -C1-4alkanediyl-X4-C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2013</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZNDx8AxT8PTz8HTyDPH0c1cw1DPSM9ENCfJ0jPL00zXT9fdzVXBxDfIMcwxxDeZhYE1LzClO5YXS3AwKbq4hzh66qQX58anFBYnJqXmpJfGuAYbmluYGpgZOhsZEKAEAEVMkPQ</recordid><startdate>20131023</startdate><enddate>20131023</enddate><creator>DE JONGE, MARC RENE</creator><creator>VINKERS, HENDRIK MAARTEN</creator><creator>JANSSEN, PAUL ADRIAAN JAN</creator><creator>HEERES, JAN</creator><creator>DAEYAERT, FREDERIK F. D</creator><creator>KILONDA, AMURI</creator><creator>KOYMANS, LUCIEN MARIA H</creator><creator>LEWI, PAULUS JOANNES</creator><creator>HOORNAERT, GEORGES J. C</creator><scope>EVB</scope></search><sort><creationdate>20131023</creationdate><title>HIV INHIBITING 1.2.4-TRIAZIN-6-ONE DERIVATES</title><author>DE JONGE, MARC RENE ; VINKERS, HENDRIK MAARTEN ; JANSSEN, PAUL ADRIAAN JAN ; HEERES, JAN ; DAEYAERT, FREDERIK F. D ; KILONDA, AMURI ; KOYMANS, LUCIEN MARIA H ; LEWI, PAULUS JOANNES ; HOORNAERT, GEORGES J. C</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_EP1797050B13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre ; ger</language><creationdate>2013</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>DE JONGE, MARC RENE</creatorcontrib><creatorcontrib>VINKERS, HENDRIK MAARTEN</creatorcontrib><creatorcontrib>JANSSEN, PAUL ADRIAAN JAN</creatorcontrib><creatorcontrib>HEERES, JAN</creatorcontrib><creatorcontrib>DAEYAERT, FREDERIK F. D</creatorcontrib><creatorcontrib>KILONDA, AMURI</creatorcontrib><creatorcontrib>KOYMANS, LUCIEN MARIA H</creatorcontrib><creatorcontrib>LEWI, PAULUS JOANNES</creatorcontrib><creatorcontrib>HOORNAERT, GEORGES J. C</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>DE JONGE, MARC RENE</au><au>VINKERS, HENDRIK MAARTEN</au><au>JANSSEN, PAUL ADRIAAN JAN</au><au>HEERES, JAN</au><au>DAEYAERT, FREDERIK F. D</au><au>KILONDA, AMURI</au><au>KOYMANS, LUCIEN MARIA H</au><au>LEWI, PAULUS JOANNES</au><au>HOORNAERT, GEORGES J. C</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>HIV INHIBITING 1.2.4-TRIAZIN-6-ONE DERIVATES</title><date>2013-10-23</date><risdate>2013</risdate><abstract>The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; -S( O)pR6; -NH-S( O)pR6; -C( O)R6; -NHC( O)H; -C( O)NHNH2; NHC( O)R6; C( NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; -C( O)-NHR13; -C( O)-NR13R14; -C( O)-R15; -CH N-NH-C( O)-R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; -C( N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 or X2 represents -NR1-; -NH-NH-; -N N-; -O-; -C( O)-; -C1-4alkanediyl-; -CHOH-; -S-; -S( O)p-; -X4-C1-4alkanediyl-; -C1-4alkanediyl-X4-; or -C1-4alkanediyl-X4-C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.</abstract><oa>free_for_read</oa></addata></record> |
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subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
title | HIV INHIBITING 1.2.4-TRIAZIN-6-ONE DERIVATES |
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