PIPERIDINE/PIPERAZINE DERIVATIVES

The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C( O)-; -C( O)-C( O)-; -NRX-C( O)-; -Z-C( O)-; -Z-NRX-C( O)-;...

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Hauptverfasser: VAN LOMMEN GUY ROSALIA EUGEEN, BRAEKEN MIRIELLE, ROEVENS PETER WALTER MARIA, BONGARTZ JEAN-PIERRE ANDRE MARC, COESEMANS ERWIN, DAVIDENKO PETR VLADIMIRIVICH, BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR, LINDERS JOANNES THEODORUS MARIA, MIEERPOEL LIEVEN, BERWAER MONIQUE JENNY MARIE, DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M
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creator VAN LOMMEN GUY ROSALIA EUGEEN
BRAEKEN MIRIELLE
ROEVENS PETER WALTER MARIA
BONGARTZ JEAN-PIERRE ANDRE MARC
COESEMANS ERWIN
DAVIDENKO PETR VLADIMIRIVICH
BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR
LINDERS JOANNES THEODORUS MARIA
MIEERPOEL LIEVEN
BERWAER MONIQUE JENNY MARIE
DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M
description The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C( O)-; -C( O)-C( O)-; -NRX-C( O)-; -Z-C( O)-; -Z-NRX-C( O)-; -C( O)-Z-; -NRX-C( O)-Z-; -C( S)-; -NRX-C( S)-; -Z-C( S)-; -Z-NRX-C( S)-; -C( S)-Z-; -NRX-C( S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C( O)-NRX- or -NRX-C( O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
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fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_US2010210618A1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>US2010210618A1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_US2010210618A13</originalsourceid><addsrcrecordid>eNrjZFAM8AxwDfJ08fRz1QczHaOATAUXoFiYY4hnmGswDwNrWmJOcSovlOZmUHZzDXH20E0tyI9PLS5ITE7NSy2JDw02MjA0MDI0MDO0cDQ0Jk4VAMEtI1s</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>PIPERIDINE/PIPERAZINE DERIVATIVES</title><source>esp@cenet</source><creator>VAN LOMMEN GUY ROSALIA EUGEEN ; BRAEKEN MIRIELLE ; ROEVENS PETER WALTER MARIA ; BONGARTZ JEAN-PIERRE ANDRE MARC ; COESEMANS ERWIN ; DAVIDENKO PETR VLADIMIRIVICH ; BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR ; LINDERS JOANNES THEODORUS MARIA ; MIEERPOEL LIEVEN ; BERWAER MONIQUE JENNY MARIE ; DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M</creator><creatorcontrib>VAN LOMMEN GUY ROSALIA EUGEEN ; BRAEKEN MIRIELLE ; ROEVENS PETER WALTER MARIA ; BONGARTZ JEAN-PIERRE ANDRE MARC ; COESEMANS ERWIN ; DAVIDENKO PETR VLADIMIRIVICH ; BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR ; LINDERS JOANNES THEODORUS MARIA ; MIEERPOEL LIEVEN ; BERWAER MONIQUE JENNY MARIE ; DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M</creatorcontrib><description>The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C( O)-; -C( O)-C( O)-; -NRX-C( O)-; -Z-C( O)-; -Z-NRX-C( O)-; -C( O)-Z-; -NRX-C( O)-Z-; -C( S)-; -NRX-C( S)-; -Z-C( S)-; -Z-NRX-C( S)-; -C( S)-Z-; -NRX-C( S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C( O)-NRX- or -NRX-C( O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.</description><language>eng</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>2010</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&amp;date=20100819&amp;DB=EPODOC&amp;CC=US&amp;NR=2010210618A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20100819&amp;DB=EPODOC&amp;CC=US&amp;NR=2010210618A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>VAN LOMMEN GUY ROSALIA EUGEEN</creatorcontrib><creatorcontrib>BRAEKEN MIRIELLE</creatorcontrib><creatorcontrib>ROEVENS PETER WALTER MARIA</creatorcontrib><creatorcontrib>BONGARTZ JEAN-PIERRE ANDRE MARC</creatorcontrib><creatorcontrib>COESEMANS ERWIN</creatorcontrib><creatorcontrib>DAVIDENKO PETR VLADIMIRIVICH</creatorcontrib><creatorcontrib>BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR</creatorcontrib><creatorcontrib>LINDERS JOANNES THEODORUS MARIA</creatorcontrib><creatorcontrib>MIEERPOEL LIEVEN</creatorcontrib><creatorcontrib>BERWAER MONIQUE JENNY MARIE</creatorcontrib><creatorcontrib>DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M</creatorcontrib><title>PIPERIDINE/PIPERAZINE DERIVATIVES</title><description>The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C( O)-; -C( O)-C( O)-; -NRX-C( O)-; -Z-C( O)-; -Z-NRX-C( O)-; -C( O)-Z-; -NRX-C( O)-Z-; -C( S)-; -NRX-C( S)-; -Z-C( S)-; -Z-NRX-C( S)-; -C( S)-Z-; -NRX-C( S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C( O)-NRX- or -NRX-C( O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. 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BRAEKEN MIRIELLE ; ROEVENS PETER WALTER MARIA ; BONGARTZ JEAN-PIERRE ANDRE MARC ; COESEMANS ERWIN ; DAVIDENKO PETR VLADIMIRIVICH ; BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR ; LINDERS JOANNES THEODORUS MARIA ; MIEERPOEL LIEVEN ; BERWAER MONIQUE JENNY MARIE ; DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US2010210618A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2010</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>VAN LOMMEN GUY ROSALIA EUGEEN</creatorcontrib><creatorcontrib>BRAEKEN MIRIELLE</creatorcontrib><creatorcontrib>ROEVENS PETER WALTER MARIA</creatorcontrib><creatorcontrib>BONGARTZ JEAN-PIERRE ANDRE MARC</creatorcontrib><creatorcontrib>COESEMANS ERWIN</creatorcontrib><creatorcontrib>DAVIDENKO PETR VLADIMIRIVICH</creatorcontrib><creatorcontrib>BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR</creatorcontrib><creatorcontrib>LINDERS JOANNES THEODORUS MARIA</creatorcontrib><creatorcontrib>MIEERPOEL LIEVEN</creatorcontrib><creatorcontrib>BERWAER MONIQUE JENNY MARIE</creatorcontrib><creatorcontrib>DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>VAN LOMMEN GUY ROSALIA EUGEEN</au><au>BRAEKEN MIRIELLE</au><au>ROEVENS PETER WALTER MARIA</au><au>BONGARTZ JEAN-PIERRE ANDRE MARC</au><au>COESEMANS ERWIN</au><au>DAVIDENKO PETR VLADIMIRIVICH</au><au>BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR</au><au>LINDERS JOANNES THEODORUS MARIA</au><au>MIEERPOEL LIEVEN</au><au>BERWAER MONIQUE JENNY MARIE</au><au>DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PIPERIDINE/PIPERAZINE DERIVATIVES</title><date>2010-08-19</date><risdate>2010</risdate><abstract>The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C( O)-; -C( O)-C( O)-; -NRX-C( O)-; -Z-C( O)-; -Z-NRX-C( O)-; -C( O)-Z-; -NRX-C( O)-Z-; -C( S)-; -NRX-C( S)-; -Z-C( S)-; -Z-NRX-C( S)-; -C( S)-Z-; -NRX-C( S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C( O)-NRX- or -NRX-C( O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.</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 PIPERIDINE/PIPERAZINE DERIVATIVES
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