Pierre Fabre Medicament

Christophe Pignier

Elisabeth Dupont-Passelaigue

Isabelle Le Roy

Samuel Mialhe

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 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. 

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Castres, France

Christophe Pignier