Piperidine/piperazine derivatives

US9499567B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Jean-Pierre Andre Marc Bongartz · Turnhout, BE
• Lieven Meerpoel · Beerse, BE
• Gustaaf Maria Boeckx · Oud-Turnhout, BE
• Guy Rosalia Eugeen Van Lommen · Berlaar, BE
• Christophe Francis Robert Nestor Buyck · Temse, BE
• Daniel Obrecht · Amriswil, CH
• Philipp Ermert · Allschwil, CH
• Anatol Luther · Binzen, DE

Key dates

• Filing date: Jul 20, 2015
• Grant date: Nov 22, 2016
• Expiry date: Jul 20, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention further relates to a DGAT inhibitor of formulaincluding 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 —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 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, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof.The invention further relates to meth…