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 -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NR-C(=O)-; -Z-C(O)-; -Z-NR-C(...
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creator | COESEMANS, ERWIN LINDERS, JOANNES THEODORUS MARIA BOECKX, GUSTAAF MARIA VAN LOMMEN, GUY ROSALIA EUGEEN BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR MEERPOEL, LIEVEN BRAEKEN, MIRIELLE BERWAER, MONIQUE JENNY MARIE ROEVENS, PETER WALTER MARIA BONGARTZ, JEAN-PIERRE ANDRE MARC DAVIDENKO, PETR VLADIMIRIVICH DE WAEPENAERT, 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 -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NR-C(=O)-; -Z-C(O)-; -Z-NR-C(=O)-; -C(=O)-Z-; -NR-C(=O)-Z-; -S(=O)p-; -C(=S)-; -NR-C(=S)-; -Z-C(=S)-; -Z-NR-C(=S)-; -C(=S)-Z1-; -NR-C(=S)-Z-; Y represents NR-C(=0)- Z-; -NR-C(=0)-Z-NR-; -NR-C(=0)-Z-NR-C(=0)-; -NR-C(=0)-Z-NR-C(=0)- O-; -NR-C(=0)-Z-0-; -NR-C(=0)-Z-0-C(=0)-; -NR-C(=0)-Z-C(=0)-; -NR-C(=0)-Z-C(=0)-0-; -NR-C(=0)-0-Z-C(=0)-; -NR-C(=0)-0-Z-C(=0)-0-; -NR-C(=O)-O-Z-O-C(=O)-; -NR-C(=O)-Z-C(=O)-NR-; -NR-C(=O)-Z-NR- C(=0)-NR-; -C(=O)-Z-; -C(=O)-Z-O-; -C(=0)-NR-Z-; -C(=0)-NR-Z-0-; -C(=0)-NR-Z-C(=0)-0-; -C(=0)-NR-Z-0-C(=0)-; -C(=0)-NR-0-Z-; -C(=O)- NR-Z-NR-; -C(=0)-NR-Z-NR-C(=0)-; -C(=0)-NR-Z-NR-C(=0)-0-; R represents Calkyl optionally substituted with cyano, Calkyloxy, Calkyl-oxyCalkyloxy, CCy cloalkyl or aryl; Calkenyl; Calkynyl; Ccycloalkyl; adamantanyl; aryl; arylCalkyl; Het; or HetCalkyl; provided that when Y represents -NR-C(=O)-Z-; -NR-C(=0)-Z-NR; -NR-C(=O)-Z-C(=O)- NR-; -C(=O)-Z-; -NR-C(=0)-Z-NR-C(=0)-NR-; -C(=O)-NR-Z-; -C(=O)-NR- O-Z-; or -C(=0)-NR-Z-NR-; then R may also represent hydrogen; R represents hydrogen, Calkyl, Calkenyl or R; provided that if X represents -O-C(=O)-, then R represents R; and provided that is 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 of said compounds. |
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fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_AU2008258487BB2</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>AU2008258487BB2</sourcerecordid><originalsourceid>FETCH-epo_espacenet_AU2008258487BB23</originalsourceid><addsrcrecordid>eNrjZFAMyCxILcpMycxL1S8AMROrgEyFFKBYWWJJZllqMQ8Da1piTnEqL5TmZlBxcw1x9tBNLciPTy0uSExOzUstiXcMNTIwsDAytTCxMHdyMjImUhkApwonrw</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>COESEMANS, ERWIN ; LINDERS, JOANNES THEODORUS MARIA ; BOECKX, GUSTAAF MARIA ; VAN LOMMEN, GUY ROSALIA EUGEEN ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; MEERPOEL, LIEVEN ; BRAEKEN, MIRIELLE ; BERWAER, MONIQUE JENNY MARIE ; ROEVENS, PETER WALTER MARIA ; BONGARTZ, JEAN-PIERRE ANDRE MARC ; DAVIDENKO, PETR VLADIMIRIVICH ; DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M</creator><creatorcontrib>COESEMANS, ERWIN ; LINDERS, JOANNES THEODORUS MARIA ; BOECKX, GUSTAAF MARIA ; VAN LOMMEN, GUY ROSALIA EUGEEN ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; MEERPOEL, LIEVEN ; BRAEKEN, MIRIELLE ; BERWAER, MONIQUE JENNY MARIE ; ROEVENS, PETER WALTER MARIA ; BONGARTZ, JEAN-PIERRE ANDRE MARC ; DAVIDENKO, PETR VLADIMIRIVICH ; DE WAEPENAERT, 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 -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NR-C(=O)-; -Z-C(O)-; -Z-NR-C(=O)-; -C(=O)-Z-; -NR-C(=O)-Z-; -S(=O)p-; -C(=S)-; -NR-C(=S)-; -Z-C(=S)-; -Z-NR-C(=S)-; -C(=S)-Z1-; -NR-C(=S)-Z-; Y represents NR-C(=0)- Z-; -NR-C(=0)-Z-NR-; -NR-C(=0)-Z-NR-C(=0)-; -NR-C(=0)-Z-NR-C(=0)- O-; -NR-C(=0)-Z-0-; -NR-C(=0)-Z-0-C(=0)-; -NR-C(=0)-Z-C(=0)-; -NR-C(=0)-Z-C(=0)-0-; -NR-C(=0)-0-Z-C(=0)-; -NR-C(=0)-0-Z-C(=0)-0-; -NR-C(=O)-O-Z-O-C(=O)-; -NR-C(=O)-Z-C(=O)-NR-; -NR-C(=O)-Z-NR- C(=0)-NR-; -C(=O)-Z-; -C(=O)-Z-O-; -C(=0)-NR-Z-; -C(=0)-NR-Z-0-; -C(=0)-NR-Z-C(=0)-0-; -C(=0)-NR-Z-0-C(=0)-; -C(=0)-NR-0-Z-; -C(=O)- NR-Z-NR-; -C(=0)-NR-Z-NR-C(=0)-; -C(=0)-NR-Z-NR-C(=0)-0-; R represents Calkyl optionally substituted with cyano, Calkyloxy, Calkyl-oxyCalkyloxy, CCy cloalkyl or aryl; Calkenyl; Calkynyl; Ccycloalkyl; adamantanyl; aryl; arylCalkyl; Het; or HetCalkyl; provided that when Y represents -NR-C(=O)-Z-; -NR-C(=0)-Z-NR; -NR-C(=O)-Z-C(=O)- NR-; -C(=O)-Z-; -NR-C(=0)-Z-NR-C(=0)-NR-; -C(=O)-NR-Z-; -C(=O)-NR- O-Z-; or -C(=0)-NR-Z-NR-; then R may also represent hydrogen; R represents hydrogen, Calkyl, Calkenyl or R; provided that if X represents -O-C(=O)-, then R represents R; and provided that is 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 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>2012</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=20121115&DB=EPODOC&CC=AU&NR=2008258487B2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20121115&DB=EPODOC&CC=AU&NR=2008258487B2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>COESEMANS, ERWIN</creatorcontrib><creatorcontrib>LINDERS, JOANNES THEODORUS MARIA</creatorcontrib><creatorcontrib>BOECKX, GUSTAAF MARIA</creatorcontrib><creatorcontrib>VAN LOMMEN, GUY ROSALIA EUGEEN</creatorcontrib><creatorcontrib>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creatorcontrib><creatorcontrib>MEERPOEL, LIEVEN</creatorcontrib><creatorcontrib>BRAEKEN, MIRIELLE</creatorcontrib><creatorcontrib>BERWAER, MONIQUE JENNY MARIE</creatorcontrib><creatorcontrib>ROEVENS, PETER WALTER MARIA</creatorcontrib><creatorcontrib>BONGARTZ, JEAN-PIERRE ANDRE MARC</creatorcontrib><creatorcontrib>DAVIDENKO, PETR VLADIMIRIVICH</creatorcontrib><creatorcontrib>DE WAEPENAERT, 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 -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NR-C(=O)-; -Z-C(O)-; -Z-NR-C(=O)-; -C(=O)-Z-; -NR-C(=O)-Z-; -S(=O)p-; -C(=S)-; -NR-C(=S)-; -Z-C(=S)-; -Z-NR-C(=S)-; -C(=S)-Z1-; -NR-C(=S)-Z-; Y represents NR-C(=0)- Z-; -NR-C(=0)-Z-NR-; -NR-C(=0)-Z-NR-C(=0)-; -NR-C(=0)-Z-NR-C(=0)- O-; -NR-C(=0)-Z-0-; -NR-C(=0)-Z-0-C(=0)-; -NR-C(=0)-Z-C(=0)-; -NR-C(=0)-Z-C(=0)-0-; -NR-C(=0)-0-Z-C(=0)-; -NR-C(=0)-0-Z-C(=0)-0-; -NR-C(=O)-O-Z-O-C(=O)-; -NR-C(=O)-Z-C(=O)-NR-; -NR-C(=O)-Z-NR- C(=0)-NR-; -C(=O)-Z-; -C(=O)-Z-O-; -C(=0)-NR-Z-; -C(=0)-NR-Z-0-; -C(=0)-NR-Z-C(=0)-0-; -C(=0)-NR-Z-0-C(=0)-; -C(=0)-NR-0-Z-; -C(=O)- NR-Z-NR-; -C(=0)-NR-Z-NR-C(=0)-; -C(=0)-NR-Z-NR-C(=0)-0-; R represents Calkyl optionally substituted with cyano, Calkyloxy, Calkyl-oxyCalkyloxy, CCy cloalkyl or aryl; Calkenyl; Calkynyl; Ccycloalkyl; adamantanyl; aryl; arylCalkyl; Het; or HetCalkyl; provided that when Y represents -NR-C(=O)-Z-; -NR-C(=0)-Z-NR; -NR-C(=O)-Z-C(=O)- NR-; -C(=O)-Z-; -NR-C(=0)-Z-NR-C(=0)-NR-; -C(=O)-NR-Z-; -C(=O)-NR- O-Z-; or -C(=0)-NR-Z-NR-; then R may also represent hydrogen; R represents hydrogen, Calkyl, Calkenyl or R; provided that if X represents -O-C(=O)-, then R represents R; and provided that is 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 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>2012</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZFAMyCxILcpMycxL1S8AMROrgEyFFKBYWWJJZllqMQ8Da1piTnEqL5TmZlBxcw1x9tBNLciPTy0uSExOzUstiXcMNTIwsDAytTCxMHdyMjImUhkApwonrw</recordid><startdate>20121115</startdate><enddate>20121115</enddate><creator>COESEMANS, ERWIN</creator><creator>LINDERS, JOANNES THEODORUS MARIA</creator><creator>BOECKX, GUSTAAF MARIA</creator><creator>VAN LOMMEN, GUY ROSALIA EUGEEN</creator><creator>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creator><creator>MEERPOEL, LIEVEN</creator><creator>BRAEKEN, MIRIELLE</creator><creator>BERWAER, MONIQUE JENNY MARIE</creator><creator>ROEVENS, PETER WALTER MARIA</creator><creator>BONGARTZ, JEAN-PIERRE ANDRE MARC</creator><creator>DAVIDENKO, PETR VLADIMIRIVICH</creator><creator>DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M</creator><scope>EVB</scope></search><sort><creationdate>20121115</creationdate><title>Piperidine/piperazine derivatives</title><author>COESEMANS, ERWIN ; 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the dotted line represents an optional bond in case A represents a carbon atom; X represents -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NR-C(=O)-; -Z-C(O)-; -Z-NR-C(=O)-; -C(=O)-Z-; -NR-C(=O)-Z-; -S(=O)p-; -C(=S)-; -NR-C(=S)-; -Z-C(=S)-; -Z-NR-C(=S)-; -C(=S)-Z1-; -NR-C(=S)-Z-; Y represents NR-C(=0)- Z-; -NR-C(=0)-Z-NR-; -NR-C(=0)-Z-NR-C(=0)-; -NR-C(=0)-Z-NR-C(=0)- O-; -NR-C(=0)-Z-0-; -NR-C(=0)-Z-0-C(=0)-; -NR-C(=0)-Z-C(=0)-; -NR-C(=0)-Z-C(=0)-0-; -NR-C(=0)-0-Z-C(=0)-; -NR-C(=0)-0-Z-C(=0)-0-; -NR-C(=O)-O-Z-O-C(=O)-; -NR-C(=O)-Z-C(=O)-NR-; -NR-C(=O)-Z-NR- C(=0)-NR-; -C(=O)-Z-; -C(=O)-Z-O-; -C(=0)-NR-Z-; -C(=0)-NR-Z-0-; -C(=0)-NR-Z-C(=0)-0-; -C(=0)-NR-Z-0-C(=0)-; -C(=0)-NR-0-Z-; -C(=O)- NR-Z-NR-; -C(=0)-NR-Z-NR-C(=0)-; -C(=0)-NR-Z-NR-C(=0)-0-; R represents Calkyl optionally substituted with cyano, Calkyloxy, Calkyl-oxyCalkyloxy, CCy cloalkyl or aryl; Calkenyl; Calkynyl; Ccycloalkyl; adamantanyl; aryl; arylCalkyl; Het; or HetCalkyl; provided that when Y represents -NR-C(=O)-Z-; -NR-C(=0)-Z-NR; -NR-C(=O)-Z-C(=O)- NR-; -C(=O)-Z-; -NR-C(=0)-Z-NR-C(=0)-NR-; -C(=O)-NR-Z-; -C(=O)-NR- O-Z-; or -C(=0)-NR-Z-NR-; then R may also represent hydrogen; R represents hydrogen, Calkyl, Calkenyl or R; provided that if X represents -O-C(=O)-, then R represents R; and provided that is 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 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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