Piperidine/piperazine derivatives

• Main Authors: VAN LOMMEN GUY ROSALIA EUGEEN, BRAEKEN MIRIELLE, ROEVENS PETER WALTER MARIA, BONGARTZ JEAN-PIERRE ANDRE MARC, COESEMANS ERWIN, DAVIDENKO PETR VLADIMIRIVICH, DE WAEPENAERT KATHARINA ANTONIA GERMANIA J. M, BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR, MEERPOEL LIEVEN, LINDERS JOANNES THEODORUS MARIA, BERWAER MONIQUE JENNY MARIE
• Format: Patent
• Language: English
• Published: 05.01.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

The invention relates to a DGAT inhibitor of formula 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 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.