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)-; -NRx-C(=O)-; -Z1-C(O)-; -Z1-NR...
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| creator | COESEMANS, ERWIN LINDERS, JOANNES THEODORUS MARIA BOECKX, GUSTAAF MARIA VAN LOMMEN, GUY ROSALIA EUGEEN MEERPOEL, LIEVEN BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR BRAEKEN, MIRIELLE ROEVENS, PETER WALTER MARIA BERWAER, MONIQUE JENNY MARIE BONGARTZ, JEAN-PIERRE ANDRE MARC DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M DAVIDENKO, PETR VLADIMIRIVICH |
| 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)-; -NRx-C(=O)-; -Z1-C(O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(=O)-Z1-; -S(=O)p-; -C(=S)-; -NRx-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(=S)-Z1-; Y represents NRx-C(=0)- Z2-; -NRx-C(=0)-Z2-NRy-; -NRx-C(=0)-Z2-NRy-C(=0)-; -NRx-C(=0)-Z2-NRy-C(=0)- O-; -NRx-C(=0)-Z2-0-; -NRx-C(=0)-Z2-0-C(=0)-; -NRx-C(=0)-Z2-C(=0)-; -NRx-C(=0)-Z2-C(=0)-0-; -NRx-C(=0)-0-Z2-C(=0)-; -NRx-C(=0)-0-Z2-C(=0)-0-; -NRx-C(=O)-O-Z2-O-C(=O)-; -NRx-C(=O)-Z2-C(=O)-NRy-; -NRx-C(=O)-Z2-NRy- C(=0)-NRy-; -C(=O)-Z2-; -C(=O)-Z2-O-; -C(=0)-NRx-Z2-; -C(=0)-NRx-Z2-0-; -C(=0)-NRx-Z2-C(=0)-0-; -C(=0)-NRx-Z2-0-C(=0)-; -C(=0)-NRx-0-Z2-; -C(=O)- NRx-Z2-NRy-; -C(=0)-NRx-Z2-NRy-C(=0)-; -C(=0)-NRx-Z2-NRy-C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cy cloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents -NRX-C(=O)-Z2-; -NRx-C(=0)-Z2-NRy; -NRX-C(=O)-Z2-C(=O)- NRy-; -C(=O)-Z2-; -NRx-C(=0)-Z2-NRy-C(=0)-NR y -; -C(=O)-NRX-Z2-; -C(=O)-NRX- O-Z2-; or -C(=0)-NRx-Z2-NRy-; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents -O-C(=O)-, then R2 represents R3; and provided that (A) 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.
La invención se refiere a un inhibidor de DGAT de fórmula (I): (ver fórmula (I)) que incluye cualquier forma estereoquímicamente isomérica del mismo, en donde A representa CH o N; la línea punteada representa un enlace opcional en el caso en que A represente un átomo de carbono; X representa -C(=O)-; -O-C(=O)-; -C(=O)-C(O)-; -NRX-C(O)-; -Z1-C(=O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(O)-Z1-; -S(=O)p-; -C(=S)-; -NRX-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(S)-Z-; Y representa NRX- C(0)-Z2-; -NRX-C(0)-Z2-NRY-; -NRx-C(=O)-Z2-NRY-C(=O) -NRx C(=O)-Z2 NR'-C(=O)-O-; -NR'-C(=O)-Z2-O-; -NRX-C(=O)-Z2-O-C(0)-; -NRxC(=O)-Z2-C(=O)-; -NRxC(=O)-Z2-C(O)-O-; -NRX-C(=O |
| format | Patent |
| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_MX2009013335A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>MX2009013335A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_MX2009013335A3</originalsourceid><addsrcrecordid>eNrjZFAM8AxwDfJ08fRz1QczHaOATAUXoFiYY4hnmGswDwNrWmJOcSovlOZmUHJzDXH20E0tyI9PLS5ITE7NSy2J940wMjCwNDA0NjY2dTQmShEAfhoi-w</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 ; MEERPOEL, LIEVEN ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; BRAEKEN, MIRIELLE ; ROEVENS, PETER WALTER MARIA ; BERWAER, MONIQUE JENNY MARIE ; BONGARTZ, JEAN-PIERRE ANDRE MARC ; DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M ; DAVIDENKO, PETR VLADIMIRIVICH</creator><creatorcontrib>COESEMANS, ERWIN ; LINDERS, JOANNES THEODORUS MARIA ; BOECKX, GUSTAAF MARIA ; VAN LOMMEN, GUY ROSALIA EUGEEN ; MEERPOEL, LIEVEN ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; BRAEKEN, MIRIELLE ; ROEVENS, PETER WALTER MARIA ; BERWAER, MONIQUE JENNY MARIE ; BONGARTZ, JEAN-PIERRE ANDRE MARC ; DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M ; DAVIDENKO, PETR VLADIMIRIVICH</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)-; -NRx-C(=O)-; -Z1-C(O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(=O)-Z1-; -S(=O)p-; -C(=S)-; -NRx-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(=S)-Z1-; Y represents NRx-C(=0)- Z2-; -NRx-C(=0)-Z2-NRy-; -NRx-C(=0)-Z2-NRy-C(=0)-; -NRx-C(=0)-Z2-NRy-C(=0)- O-; -NRx-C(=0)-Z2-0-; -NRx-C(=0)-Z2-0-C(=0)-; -NRx-C(=0)-Z2-C(=0)-; -NRx-C(=0)-Z2-C(=0)-0-; -NRx-C(=0)-0-Z2-C(=0)-; -NRx-C(=0)-0-Z2-C(=0)-0-; -NRx-C(=O)-O-Z2-O-C(=O)-; -NRx-C(=O)-Z2-C(=O)-NRy-; -NRx-C(=O)-Z2-NRy- C(=0)-NRy-; -C(=O)-Z2-; -C(=O)-Z2-O-; -C(=0)-NRx-Z2-; -C(=0)-NRx-Z2-0-; -C(=0)-NRx-Z2-C(=0)-0-; -C(=0)-NRx-Z2-0-C(=0)-; -C(=0)-NRx-0-Z2-; -C(=O)- NRx-Z2-NRy-; -C(=0)-NRx-Z2-NRy-C(=0)-; -C(=0)-NRx-Z2-NRy-C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cy cloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents -NRX-C(=O)-Z2-; -NRx-C(=0)-Z2-NRy; -NRX-C(=O)-Z2-C(=O)- NRy-; -C(=O)-Z2-; -NRx-C(=0)-Z2-NRy-C(=0)-NR y -; -C(=O)-NRX-Z2-; -C(=O)-NRX- O-Z2-; or -C(=0)-NRx-Z2-NRy-; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents -O-C(=O)-, then R2 represents R3; and provided that (A) 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.
La invención se refiere a un inhibidor de DGAT de fórmula (I): (ver fórmula (I)) que incluye cualquier forma estereoquímicamente isomérica del mismo, en donde A representa CH o N; la línea punteada representa un enlace opcional en el caso en que A represente un átomo de carbono; X representa -C(=O)-; -O-C(=O)-; -C(=O)-C(O)-; -NRX-C(O)-; -Z1-C(=O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(O)-Z1-; -S(=O)p-; -C(=S)-; -NRX-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(S)-Z-; Y representa NRX- C(0)-Z2-; -NRX-C(0)-Z2-NRY-; -NRx-C(=O)-Z2-NRY-C(=O) -NRx C(=O)-Z2 NR'-C(=O)-O-; -NR'-C(=O)-Z2-O-; -NRX-C(=O)-Z2-O-C(0)-; -NRxC(=O)-Z2-C(=O)-; -NRxC(=O)-Z2-C(O)-O-; -NRX-C(=O)-O-Z2- C(=O)-; -NRxC(=O)-O-Z2-C(O)-O-; -NRx-C(=O)-OZ2-O-C(O)-; - NRX-C(=O)-Z2-C(=O)-NRSI-; -NRx-C(=O)-Z2-NR-C(=O)-NRf-; -C(=O)- Z2-; -C(=O)-Z2-O-; -C(=O)-NRX-Z2-; -C(=O)-NRX-Z2-O-; -CQO)-NRx- Z2-C(=O)-O-; -C(O)-NRx-Z2-O-C(O) -C(0)-NRX-O-Z2-; -C(=O)- NRx-Z2-NR-; -C(=O)-NR'-Z2-NR'--C(=O)-; -C(=O)-NRx-Z2-NRY-C(0)-O-; R' representa alquilo de C1-12 opcionalmente sustituido con ciano, alquiloxi de C1., alquilo de C1-oxi alquiloxi de C1, cicloalquilo de C o arilo; alquenilo de C2 alquinilo de C2 cicloalquilo de C adamantanilo; arilo1 aril1alquilo de C1 Het'; o Het alquilo de C1 con la salvedad de que cuando Y representa -NRX-C(=O)-Z2-; -NRX-C(=O)-Z2-N R -N RxC(=O)- Z2-C(=O)-NR'-; -C(=O)-Z2-; -NRx-C(=O)-Z2-NR-C(O)-NRf-; -C(0)- NRX-Z2-; -C(0)-NRX-O-Z2-; o -C(O)-NRx-Z2-NRf-; entonces R' puede también representar hidrógeno; R2 representa hidrógeno, alquilo de C1...,2, alquenilo de C o R3 con la salvedad de que si X representa -O-C(0)-, entonces R2 representa R3 y con la salvedad de que (A) se excluye; un N- óxido de los mismos, una sal farmacéuticamente aceptable de los mismos o un solvato de los mismos; además, la invención se refiere a métodos para preparar dichos compuestos, composiciones farmacéuticas que comprenden dichos compuestos así como al uso como un medicamento de dichos compuestos.</description><language>eng ; spa</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=20100120&DB=EPODOC&CC=MX&NR=2009013335A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,778,883,25547,76298</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20100120&DB=EPODOC&CC=MX&NR=2009013335A$$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>MEERPOEL, LIEVEN</creatorcontrib><creatorcontrib>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creatorcontrib><creatorcontrib>BRAEKEN, MIRIELLE</creatorcontrib><creatorcontrib>ROEVENS, PETER WALTER MARIA</creatorcontrib><creatorcontrib>BERWAER, MONIQUE JENNY MARIE</creatorcontrib><creatorcontrib>BONGARTZ, JEAN-PIERRE ANDRE MARC</creatorcontrib><creatorcontrib>DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M</creatorcontrib><creatorcontrib>DAVIDENKO, PETR VLADIMIRIVICH</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)-; -NRx-C(=O)-; -Z1-C(O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(=O)-Z1-; -S(=O)p-; -C(=S)-; -NRx-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(=S)-Z1-; Y represents NRx-C(=0)- Z2-; -NRx-C(=0)-Z2-NRy-; -NRx-C(=0)-Z2-NRy-C(=0)-; -NRx-C(=0)-Z2-NRy-C(=0)- O-; -NRx-C(=0)-Z2-0-; -NRx-C(=0)-Z2-0-C(=0)-; -NRx-C(=0)-Z2-C(=0)-; -NRx-C(=0)-Z2-C(=0)-0-; -NRx-C(=0)-0-Z2-C(=0)-; -NRx-C(=0)-0-Z2-C(=0)-0-; -NRx-C(=O)-O-Z2-O-C(=O)-; -NRx-C(=O)-Z2-C(=O)-NRy-; -NRx-C(=O)-Z2-NRy- C(=0)-NRy-; -C(=O)-Z2-; -C(=O)-Z2-O-; -C(=0)-NRx-Z2-; -C(=0)-NRx-Z2-0-; -C(=0)-NRx-Z2-C(=0)-0-; -C(=0)-NRx-Z2-0-C(=0)-; -C(=0)-NRx-0-Z2-; -C(=O)- NRx-Z2-NRy-; -C(=0)-NRx-Z2-NRy-C(=0)-; -C(=0)-NRx-Z2-NRy-C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cy cloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents -NRX-C(=O)-Z2-; -NRx-C(=0)-Z2-NRy; -NRX-C(=O)-Z2-C(=O)- NRy-; -C(=O)-Z2-; -NRx-C(=0)-Z2-NRy-C(=0)-NR y -; -C(=O)-NRX-Z2-; -C(=O)-NRX- O-Z2-; or -C(=0)-NRx-Z2-NRy-; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents -O-C(=O)-, then R2 represents R3; and provided that (A) 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.
La invención se refiere a un inhibidor de DGAT de fórmula (I): (ver fórmula (I)) que incluye cualquier forma estereoquímicamente isomérica del mismo, en donde A representa CH o N; la línea punteada representa un enlace opcional en el caso en que A represente un átomo de carbono; X representa -C(=O)-; -O-C(=O)-; -C(=O)-C(O)-; -NRX-C(O)-; -Z1-C(=O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(O)-Z1-; -S(=O)p-; -C(=S)-; -NRX-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(S)-Z-; Y representa NRX- C(0)-Z2-; -NRX-C(0)-Z2-NRY-; -NRx-C(=O)-Z2-NRY-C(=O) -NRx C(=O)-Z2 NR'-C(=O)-O-; -NR'-C(=O)-Z2-O-; -NRX-C(=O)-Z2-O-C(0)-; -NRxC(=O)-Z2-C(=O)-; -NRxC(=O)-Z2-C(O)-O-; -NRX-C(=O)-O-Z2- C(=O)-; -NRxC(=O)-O-Z2-C(O)-O-; -NRx-C(=O)-OZ2-O-C(O)-; - NRX-C(=O)-Z2-C(=O)-NRSI-; -NRx-C(=O)-Z2-NR-C(=O)-NRf-; -C(=O)- Z2-; -C(=O)-Z2-O-; -C(=O)-NRX-Z2-; -C(=O)-NRX-Z2-O-; -CQO)-NRx- Z2-C(=O)-O-; -C(O)-NRx-Z2-O-C(O) -C(0)-NRX-O-Z2-; -C(=O)- NRx-Z2-NR-; -C(=O)-NR'-Z2-NR'--C(=O)-; -C(=O)-NRx-Z2-NRY-C(0)-O-; R' representa alquilo de C1-12 opcionalmente sustituido con ciano, alquiloxi de C1., alquilo de C1-oxi alquiloxi de C1, cicloalquilo de C o arilo; alquenilo de C2 alquinilo de C2 cicloalquilo de C adamantanilo; arilo1 aril1alquilo de C1 Het'; o Het alquilo de C1 con la salvedad de que cuando Y representa -NRX-C(=O)-Z2-; -NRX-C(=O)-Z2-N R -N RxC(=O)- Z2-C(=O)-NR'-; -C(=O)-Z2-; -NRx-C(=O)-Z2-NR-C(O)-NRf-; -C(0)- NRX-Z2-; -C(0)-NRX-O-Z2-; o -C(O)-NRx-Z2-NRf-; entonces R' puede también representar hidrógeno; R2 representa hidrógeno, alquilo de C1...,2, alquenilo de C o R3 con la salvedad de que si X representa -O-C(0)-, entonces R2 representa R3 y con la salvedad de que (A) se excluye; un N- óxido de los mismos, una sal farmacéuticamente aceptable de los mismos o un solvato de los mismos; además, la invención se refiere a métodos para preparar dichos compuestos, composiciones farmacéuticas que comprenden dichos compuestos así como al uso como un medicamento de dichos compuestos.</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>eNrjZFAM8AxwDfJ08fRz1QczHaOATAUXoFiYY4hnmGswDwNrWmJOcSovlOZmUHJzDXH20E0tyI9PLS5ITE7NSy2J940wMjCwNDA0NjY2dTQmShEAfhoi-w</recordid><startdate>20100120</startdate><enddate>20100120</enddate><creator>COESEMANS, ERWIN</creator><creator>LINDERS, JOANNES THEODORUS MARIA</creator><creator>BOECKX, GUSTAAF MARIA</creator><creator>VAN LOMMEN, GUY ROSALIA EUGEEN</creator><creator>MEERPOEL, LIEVEN</creator><creator>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creator><creator>BRAEKEN, MIRIELLE</creator><creator>ROEVENS, PETER WALTER MARIA</creator><creator>BERWAER, MONIQUE JENNY MARIE</creator><creator>BONGARTZ, JEAN-PIERRE ANDRE MARC</creator><creator>DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M</creator><creator>DAVIDENKO, PETR VLADIMIRIVICH</creator><scope>EVB</scope></search><sort><creationdate>20100120</creationdate><title>PIPERIDINE/PIPERAZINE DERIVATIVES</title><author>COESEMANS, ERWIN ; LINDERS, JOANNES THEODORUS MARIA ; BOECKX, GUSTAAF MARIA ; VAN LOMMEN, GUY ROSALIA EUGEEN ; MEERPOEL, LIEVEN ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; BRAEKEN, MIRIELLE ; ROEVENS, PETER WALTER MARIA ; BERWAER, MONIQUE JENNY MARIE ; BONGARTZ, JEAN-PIERRE ANDRE MARC ; DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M ; DAVIDENKO, PETR VLADIMIRIVICH</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_MX2009013335A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; spa</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>COESEMANS, ERWIN</creatorcontrib><creatorcontrib>LINDERS, JOANNES THEODORUS MARIA</creatorcontrib><creatorcontrib>BOECKX, GUSTAAF MARIA</creatorcontrib><creatorcontrib>VAN LOMMEN, GUY ROSALIA EUGEEN</creatorcontrib><creatorcontrib>MEERPOEL, LIEVEN</creatorcontrib><creatorcontrib>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creatorcontrib><creatorcontrib>BRAEKEN, MIRIELLE</creatorcontrib><creatorcontrib>ROEVENS, PETER WALTER MARIA</creatorcontrib><creatorcontrib>BERWAER, MONIQUE JENNY MARIE</creatorcontrib><creatorcontrib>BONGARTZ, JEAN-PIERRE ANDRE MARC</creatorcontrib><creatorcontrib>DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M</creatorcontrib><creatorcontrib>DAVIDENKO, PETR VLADIMIRIVICH</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>COESEMANS, ERWIN</au><au>LINDERS, JOANNES THEODORUS MARIA</au><au>BOECKX, GUSTAAF MARIA</au><au>VAN LOMMEN, GUY ROSALIA EUGEEN</au><au>MEERPOEL, LIEVEN</au><au>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</au><au>BRAEKEN, MIRIELLE</au><au>ROEVENS, PETER WALTER MARIA</au><au>BERWAER, MONIQUE JENNY MARIE</au><au>BONGARTZ, JEAN-PIERRE ANDRE MARC</au><au>DE WAEPENAERT, KATHARINA ANTONIA GERMANIA J.M</au><au>DAVIDENKO, PETR VLADIMIRIVICH</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PIPERIDINE/PIPERAZINE DERIVATIVES</title><date>2010-01-20</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 -C(=O)-; -O-C(=O)-; -C(=O)-C(=O)-; -NRx-C(=O)-; -Z1-C(O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(=O)-Z1-; -S(=O)p-; -C(=S)-; -NRx-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(=S)-Z1-; Y represents NRx-C(=0)- Z2-; -NRx-C(=0)-Z2-NRy-; -NRx-C(=0)-Z2-NRy-C(=0)-; -NRx-C(=0)-Z2-NRy-C(=0)- O-; -NRx-C(=0)-Z2-0-; -NRx-C(=0)-Z2-0-C(=0)-; -NRx-C(=0)-Z2-C(=0)-; -NRx-C(=0)-Z2-C(=0)-0-; -NRx-C(=0)-0-Z2-C(=0)-; -NRx-C(=0)-0-Z2-C(=0)-0-; -NRx-C(=O)-O-Z2-O-C(=O)-; -NRx-C(=O)-Z2-C(=O)-NRy-; -NRx-C(=O)-Z2-NRy- C(=0)-NRy-; -C(=O)-Z2-; -C(=O)-Z2-O-; -C(=0)-NRx-Z2-; -C(=0)-NRx-Z2-0-; -C(=0)-NRx-Z2-C(=0)-0-; -C(=0)-NRx-Z2-0-C(=0)-; -C(=0)-NRx-0-Z2-; -C(=O)- NRx-Z2-NRy-; -C(=0)-NRx-Z2-NRy-C(=0)-; -C(=0)-NRx-Z2-NRy-C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cy cloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents -NRX-C(=O)-Z2-; -NRx-C(=0)-Z2-NRy; -NRX-C(=O)-Z2-C(=O)- NRy-; -C(=O)-Z2-; -NRx-C(=0)-Z2-NRy-C(=0)-NR y -; -C(=O)-NRX-Z2-; -C(=O)-NRX- O-Z2-; or -C(=0)-NRx-Z2-NRy-; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents -O-C(=O)-, then R2 represents R3; and provided that (A) 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.
La invención se refiere a un inhibidor de DGAT de fórmula (I): (ver fórmula (I)) que incluye cualquier forma estereoquímicamente isomérica del mismo, en donde A representa CH o N; la línea punteada representa un enlace opcional en el caso en que A represente un átomo de carbono; X representa -C(=O)-; -O-C(=O)-; -C(=O)-C(O)-; -NRX-C(O)-; -Z1-C(=O)-; -Z1-NRx-C(=O)-; -C(=O)-Z1-; -NRx-C(O)-Z1-; -S(=O)p-; -C(=S)-; -NRX-C(=S)-; -Z1-C(=S)-; -Z1-NRX-C(=S)-; -C(=S)-Z1-; -NRx-C(S)-Z-; Y representa NRX- C(0)-Z2-; -NRX-C(0)-Z2-NRY-; -NRx-C(=O)-Z2-NRY-C(=O) -NRx C(=O)-Z2 NR'-C(=O)-O-; -NR'-C(=O)-Z2-O-; -NRX-C(=O)-Z2-O-C(0)-; -NRxC(=O)-Z2-C(=O)-; -NRxC(=O)-Z2-C(O)-O-; -NRX-C(=O)-O-Z2- C(=O)-; -NRxC(=O)-O-Z2-C(O)-O-; -NRx-C(=O)-OZ2-O-C(O)-; - NRX-C(=O)-Z2-C(=O)-NRSI-; -NRx-C(=O)-Z2-NR-C(=O)-NRf-; -C(=O)- Z2-; -C(=O)-Z2-O-; -C(=O)-NRX-Z2-; -C(=O)-NRX-Z2-O-; -CQO)-NRx- Z2-C(=O)-O-; -C(O)-NRx-Z2-O-C(O) -C(0)-NRX-O-Z2-; -C(=O)- NRx-Z2-NR-; -C(=O)-NR'-Z2-NR'--C(=O)-; -C(=O)-NRx-Z2-NRY-C(0)-O-; R' representa alquilo de C1-12 opcionalmente sustituido con ciano, alquiloxi de C1., alquilo de C1-oxi alquiloxi de C1, cicloalquilo de C o arilo; alquenilo de C2 alquinilo de C2 cicloalquilo de C adamantanilo; arilo1 aril1alquilo de C1 Het'; o Het alquilo de C1 con la salvedad de que cuando Y representa -NRX-C(=O)-Z2-; -NRX-C(=O)-Z2-N R -N RxC(=O)- Z2-C(=O)-NR'-; -C(=O)-Z2-; -NRx-C(=O)-Z2-NR-C(O)-NRf-; -C(0)- NRX-Z2-; -C(0)-NRX-O-Z2-; o -C(O)-NRx-Z2-NRf-; entonces R' puede también representar hidrógeno; R2 representa hidrógeno, alquilo de C1...,2, alquenilo de C o R3 con la salvedad de que si X representa -O-C(0)-, entonces R2 representa R3 y con la salvedad de que (A) se excluye; un N- óxido de los mismos, una sal farmacéuticamente aceptable de los mismos o un solvato de los mismos; además, la invención se refiere a métodos para preparar dichos compuestos, composiciones farmacéuticas que comprenden dichos compuestos así como al uso como un medicamento de dichos compuestos.</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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