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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Hauptverfasser: 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
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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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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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