Janssen Pharmaceutica Nv

Peter Walter Maria Roevens

Lieven Meerpoel

Leo Jacobus Jozef Backx

Joannes Theodorus Maria Linders

Louis Jozef Elisabeth Van Der Veken

Marcel Viellevoye

Christophe Francis Robert Nestor Buyck

Erwin Coesemans

Guy Rosalia Eugeen Van Lommen

Jean-Pierre André Marc Bongartz

Mirielle Braeken

Monique Jenny Marie Berwaer

Katharina Antonia Germania J M De Waepenaert

Petr Vladimirivich Davidenko

Libuse Jaroskova

Brian Joel Hrupka

Jean-Pierre Andre Marc Bongartz

Gustaaf Maria Boeckx

Cornelus Gerardus Maria Janssen

Jozef Bertha August Thijssen

Katharina Antonia Germania JM De Waepenaert

The present invention relates to combinations of a DGAT inhibitor and a peroxisome proliferator-activator receptor (PPAR) agonist or a prodrug thereof. The invention further relates to methods for preparing such combinations, pharmaceutical compositions comprising said combinations as well as the use as a medicament of said combinations. The present invention also relates to novel DGAT inhibitors. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicament of said compounds.

Drug combinations comprising a DGAT inhibitor and a PPAR-agonist

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 present invention relates to combinations of a DGAT inhibitor and a peroxisome proliferator-activator receptor (PPAR) agonist or a prodrug thereof.

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.

Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.

Polyarylcarboxamides useful as lipid lowering agents

N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.

N-aryl piperidine substituted biphenylcarboxamides

The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.  The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

MTP inhibiting aryl piperidines or piperazines substituted with 5-membered heterocycles

The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.  The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hyper-triglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

MTP inhibiting aryl piperydines or piperazines substituted with 5-membered heterocycles

Polyarylcarboxamide compounds of formula I) are useful as lipid lowering agents.

Polyarylcarboxamide compounds of formula (I):are useful as lipid lowering agents.

Growing community of inventors

Malle, Belgium

Peter Walter Maria Roevens