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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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&date=20100819&DB=EPODOC&CC=US&NR=2010210618A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20100819&DB=EPODOC&CC=US&NR=2010210618A1$$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. 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><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>2010</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZFAM8AxwDfJ08fRz1QczHaOATAUXoFiYY4hnmGswDwNrWmJOcSovlOZmUHZzDXH20E0tyI9PLS5ITE7NSy2JDw02MjA0MDI0MDO0cDQ0Jk4VAMEtI1s</recordid><startdate>20100819</startdate><enddate>20100819</enddate><creator>VAN LOMMEN GUY ROSALIA EUGEEN</creator><creator>BRAEKEN MIRIELLE</creator><creator>ROEVENS PETER WALTER MARIA</creator><creator>BONGARTZ JEAN-PIERRE ANDRE MARC</creator><creator>COESEMANS ERWIN</creator><creator>DAVIDENKO PETR VLADIMIRIVICH</creator><creator>BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR</creator><creator>LINDERS JOANNES THEODORUS MARIA</creator><creator>MIEERPOEL LIEVEN</creator><creator>BERWAER MONIQUE JENNY MARIE</creator><creator>DE WAEPENARET KATHARINA ANTONIA GERMANIA J.M</creator><scope>EVB</scope></search><sort><creationdate>20100819</creationdate><title>PIPERIDINE/PIPERAZINE DERIVATIVES</title><author>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</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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