Invention Grant
- Patent Title: Piperidine/piperazine derivatives
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Application No.: US14561252Application Date: 2014-12-05
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Publication No.: US09227935B2Publication Date: 2016-01-05
- Inventor: Jean-Pierre Andre Marc Bongartz , Joannes Theodorus Maria Linders , Lieven Meerpoel , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Mirielle Braeken , Christophe Francis Robert Nestor Buyck , Monique Jenny Marie Berwaer , Katharina Antonia Germania J. M. De Waepenaert , Peter Walter Maria Roevens , Petr Vladimirivich Davidenko
- Applicant: Janssen Pharmaceutica N.V.
- Applicant Address: BE Beerse
- Assignee: Janssen Pharmaceutical N.V.
- Current Assignee: Janssen Pharmaceutical N.V.
- Current Assignee Address: BE Beerse
- Priority: EP07109866 20070608
- Main IPC: A61K31/451
- IPC: A61K31/451 ; C07D401/12 ; C07D211/60 ; A61K31/495 ; C07D207/323 ; C07D211/26 ; C07D231/12 ; C07D233/54 ; C07D233/64 ; C07D235/18 ; C07D249/08 ; C07D257/04 ; C07D263/34 ; C07D277/56 ; C07D279/02 ; C07D279/12 ; C07D295/20 ; C07D307/54 ; C07D319/18 ; C07D417/12 ; C07D417/14 ; C07D207/277 ; C07D295/205 ; C07D295/21 ; C07D295/215

Abstract:
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.
Public/Granted literature
- US20150087629A1 PIPERIDINE/PIPERAZINE DERIVATIVES Public/Granted day:2015-03-26
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