Piperidine/piperazine derivatives

US8981094B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Jean-Pierre Andre Marc Bongartz · Turnhout, BE
• Joannes Theodorus Maria Linders · Eindhoven, NL
• Lieven Meerpoel · Beerse, BE
• Guy Rosalia Eugeen Van Lommen · Berlaar, BE
• Erwin Coesemans · Nijlen, BE
• Mirielle Braeken · Vlimmeren, BE
• Christophe Francis Robert Nestor Buyck · Temse, BE
• Monique Berwaer · Montigny-le-Tilleul, BE
• Katharina Antonia Germania J. M. De Waepenaert · Vosselaar, BE
• Peter Walter Maria Roevens · Malle, BE
• Gustaaf Maria Boeckx · Oud-Turnhout, BE
• Petr Vladimirivich Davidenko · Moscow, RU

Key dates

• Filing date: Jun 6, 2008
• Grant date: Mar 17, 2015
• Expiry date: Jul 24, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D333/24
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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)—Z—; 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)-; —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—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, C3-6Cycloalkyl 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—;…