Janssen Pharmaceutica Nv

Petr Vladimirivich Davidenko

Lieven Meerpoel

Joannes Theodorus Maria Linders

Guy Rosalia Van Lommen

Christophe Francis Robert Nestor Buyck

Peter Walter Maria Roevens

Erwin Coesemans

Guy Rosalia Eugeen Van Lommen

Mirielle Braeken

Katharina Antonia Germania J M De Waepenaert

Monique Jenny Marie Berwaer

Jean-Pierre André Marc Bongartz

Gustaaf Maria Boeckx

Christophe Francis Buyck

Joannes Theodorus Linders

Jean-Pierre Andre Bongartz

Katharina Antonia De Waepenaert

Peter Walter Roevens

Monique Jenny Berwaer

Katharina Antonia Germania JM De Waepenaert

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 &#x2014;O&#x2014;C(&#x2550;O)&#x2014;; &#x2014;C(&#x2550;O)&#x2014;C(&#x2550;O)&#x2014;; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;; &#x2014;Z&#x2014;C(&#x2550;O)&#x2014;; &#x2014;Z&#x2014;NR&#x2014;C(&#x2550;O)&#x2014;; &#x2014;C(&#x2550;O)&#x2014;Z&#x2014;; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;Z&#x2014;; &#x2014;C(&#x2550;S)&#x2014;; &#x2014;NR&#x2014;C(&#x2550;S)&#x2014;; &#x2014;Z&#x2014;C(&#x2550;S)&#x2014;; &#x2014;Z&#x2014;NR&#x2014;C(&#x2550;S)&#x2014;; &#x2014;C(&#x2550;S)&#x2014;Z&#x2014;; &#x2014;NR&#x2014;C(&#x2550;S)&#x2014;Z&#x2014;; Z represents a bivalent radical selected from Calkanediyl, Calkenediyl or Calkynediyl; wherein each of said Calkanediyl, Calkenediyl or Calkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in Calkanediyl may optionally be replaced by Calkanediyl; Y represents &#x2014;C(&#x2550;O)&#x2014;NR&#x2014; or &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;; Rrepresents adamantanyl, Ccycloalkyl; arylor Het; Rrepresents Ccycloalkyl, 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 Ccycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; Rrepresents hydrogen, halo, Calkyl, Calkyl 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.

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 &#x2014;C(&#x2550;O)&#x2014;; &#x2014;O&#x2014;C(&#x2550;O)&#x2014;; C(&#x2550;O)&#x2014;C(&#x2550;O)&#x2014;; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;; &#x2014;Z&#x2014;C(O)&#x2014;; &#x2014;Z&#x2014;NR&#x2014;C(&#x2550;O)&#x2014;; &#x2014;C(&#x2550;O)&#x2014;Z&#x2014;; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;Z&#x2014;; &#x2014;S(&#x2550;O)p-; &#x2014;C(&#x2550;S)&#x2014;; &#x2014;NR&#x2014;C(&#x2550;S)&#x2014;; &#x2014;Z&#x2014;C(&#x2550;S)&#x2014;; &#x2014;Z&#x2014;NR&#x2014;C(&#x2550;S)&#x2014;; &#x2014;C(&#x2550;S)&#x2014;Z1-; &#x2014;NR&#x2014;C(&#x2550;S)&#x2014;Z&#x2014;; Y represents NR&#x2014;C(=0)-Z&#x2014;; &#x2014;NR&#x2014;C(=0)-Z&#x2014;NR&#x2014;; &#x2014;NR&#x2014;C(=0)-Z&#x2014;NR&#x2014;C(=0)-; &#x2014;NR&#x2014;C(=0)-Z&#x2014;NR&#x2014;C(=0)-O&#x2014;; &#x2014;NR&#x2014;C(=0)-Z-0-; &#x2014;NR&#x2014;C(=0)-Z-0-C(=0)-; &#x2014;NR&#x2014;C(=0)-Z&#x2014;C(=0)-; &#x2014;NR&#x2014;C(=0)-Z&#x2014;C(=0)-; &#x2014;NR&#x2014;C(=0)-0-Z&#x2014;C(=0)-; &#x2014;NR&#x2014;C(=0)-0-Z&#x2014;C(=0)-0-; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;O&#x2014;Z&#x2014;O&#x2014;C(&#x2550;O)&#x2014;; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;Z&#x2014;C(&#x2550;O)&#x2014;NR&#x2014;; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;Z&#x2014;NR&#x2014;C(=0)-NR&#x2014;; &#x2014;C(&#x2550;O)&#x2014;Z&#x2014;; &#x2014;C(&#x2550;O)&#x2014;Z&#x2014;O&#x2014;; &#x2014;C(=0)-NR&#x2014;Z&#x2014;; &#x2014;C(=0)-NR&#x2014;Z-0-; &#x2014;C(=0)-NR&#x2014;Z&#x2014;C(=0)-0-; &#x2014;C(=0)-NR&#x2014;Z-0-C(=0)-; &#x2014;C(=0)-NR&#x2014;Z&#x2014;NR&#x2014;; &#x2014;C(=0)-NR&#x2014;Z&#x2014;NR&#x2014;C(=0)-; &#x2014;C(=0)-NR&#x2014;Z&#x2014;NR&#x2014;C(=0)-0-; Rrepresents Calkyl optionally substituted with cyano, Calkyloxy, Calkyl-oxyCalkyloxy, CCycloalkyl or aryl; Calkenyl; Calkynyl; Ccycloalkyl; adamantanyl; aryl; arylCalkyl; Het; or HetCalkyl; provided that when Y represents &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;Z&#x2014;; &#x2014;NR&#x2014;C(=0)-Z&#x2014;NR; &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;Z&#x2014;C(&#x2550;O)&#x2014;NR&#x2014;; &#x2014;C(&#x2550;O)&#x2014;Z&#x2014;; &#x2014;NR&#x2014;C(=0)-Z&#x2014;NR&#x2014;C(=0)-NR&#x2014;; &#x2014;C(&#x2550;O)&#x2014;NR&#x2014;Z&#x2014;; &#x2014;C(&#x2550;O)&#x2014;NR&#x2014;O&#x2014;Z&#x2014;; or &#x2014;C(=0)-NR&#x2014;Z&#x2014;NR&#x2014;; then Rmay also represent hydrogen; Rrepresents hydrogen, Calkyl, Calkenyl or R; provided that if X represents &#x2014;O&#x2014;C(&#x2550;O)&#x2014;; the Rrepresents R; and provided that (A) 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. 

The invention relates to a DGAT inhibitor of formula (I),  including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and 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.

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Moscow, Russia

Petr Vladimirivich Davidenko