Pierre Fabre Medicament

Elisabeth Dupont-Passelaigue

Wouter Koek

Didier Junquero

Isabelle Le Roy

Christophe Pignier

Samuel Mialhe

Karine Valeille

Isabelle Leroy

Jean-Francois Patoiseau

Yves Rival

Christian Faure

Jean-Pierre Rieu

André Delhon

Jean-Fran&ccedil;ois Patoiseau

Jean-Francedillaois Patoiseau

Jean-François Patoiseau

Francoise Couret

Francedillaoise Couret

The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C-Calkyl, or linear or branched C-Calkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents &#x2014;C(&#x2550;O)&#x2014;, or B represents CH when n=0 and D represents &#x2014;CHO&#x2014; or when n=1 and D represents &#x2014;O&#x2014;, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C-Calkyl, a linear or branched C-Calkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.

Derivatives of heteroarylsulfonamides, their preparation and their application in human therapy

The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where Rand Rare simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C-Calkyl, hydroxy, a straight or branched C-Calkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C-Calkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.

Diarylpyridazinone derivatives, preparation thereof, and use thereof for the treatment of humans

The present invention relates to compounds having general formula I characterized in that  

Nitrogen heterocycle derivatives, preparation thereof and application thereof in human therapeutics

The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: &#x2014;Rrepresents one or more groups such as: trifluoromethyl, halogen such as F, Cl, &#x2014;when n=m=1, W represents CH then Y represents oxygen, &#x2014;U represents: &#x2022;either &#x2014;(C&#x2550;O)CHNH&#x2014; and is branched at position 4 of pyridazinone, then R2 represents H, &#x2022;or &#x2014;(C&#x2550;O)NH&#x2014; and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, &#x2014;R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders. 

Derivatives of 2H pyridazin-3-ones, their preparation and their use as SCD-1 inhibitors

The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C-Calkyl, or linear or branched C-Calkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents &#x2014;C(&#x2550;O)&#x2014;, or B represents CH when n=0 and D represents &#x2014;CHO&#x2014; or when n=1 and D represents &#x2014;O&#x2014;, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C-Calkyl, a linear or branched C-Calkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts. 

The present invention relates to derivatives of general formula I wherein: &#x2014;W represents nitrogen, &#x2014;Rrepresents: &#x2022;a hydrogen or a linear or branched C-Calkyl radical or, &#x2022;a C-Calkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C-Calcoxy, C-Calkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C-CN-alkylcarbamoyl groups or, &#x2022;a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C-Calkyl, linear or branched C-Calkoxy groups, &#x2022;a C2-oxocycloalkyl radical&#x2014;Rrepresents a methyl or heptyl, -m, n are equal to 1, &#x2014;V represents CH, &#x2014;X&#x2014;Y represents &#x2014;N&#x2014; (C&#x2550;O)&#x2014;, &#x2014;CH&#x2014;O&#x2014;, &#x2014;Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C-Calkyl groups. 

Derivatives of triazines and uracils, their preparation and their application in human therapeutics

The invention relates to 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I in which the variables are defined herein, as well as additive salts with pharmaceutically acceptable bases and the various enantiomers of compounds having asymmetrical carbons, as well as their mixtures in all proportions, including racemic mixtures in particular.

1,2,4-triazine derivatives, preparation and use thereof in human therapy

The invention concerns novel 3-oxo-(2H)-1,2,4-triazine derivatives of general formula (I) in which R,represents: hydrogen, when A is an optionally substituted nitrogen atom; a linear or branched,-C,alkyl group; a C,-C,phenyl alkyl group, the phenyl ring being optionally substituted by one or several groups such as C,-C,alkyl, C,-C,alkoxy, halogen, trifluoromethyl. R,represents: hydrogen; a linear or branched C,-C,alkyl radical; a C,phenyl or phenylalkyl group, the phenyl ring being optionally substituted by one or several groups such as C,-C,alkyl, C,-C,alkoxy, halogen, trifluoromethyl. A represents an oxygen atom or a nitrogen atom optionally NR,substituted. R,represents hydrogen or a methyl group. B represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl, pyridyl or pyrimidyl, optionally substituted by one or several groups such as C,-C,alkyl, C,-C,alkoxy, hydroxy, trifluoromethyl or halogen and n can be whole numbers ranging between 3 and 5; (IIb) in which Ar is as defined in formula (IIa) and m can be a whole number ranging between 1 and 2; (IIc) in which R,represents hydrogen or a C,-C,alkyl group and n can be whole numbers ranging between 3 and 5.

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Colomiers, France

Elisabeth Dupont-Passelaigue