DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY

摘要

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 C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(═O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, 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 C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.

主权项

1. A method for blocking Kv potassium channels comprising the administration to a person in need thereof of an effective amount of a compound of general formula I:where
R1 represents one or more substituents of the phenyl core X chosen from among the group consisting of: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, and linear or branched C1-C4 alkoxy, n represents 0, 1 or 2, A represents oxygen or sulphur, D represents —C(═O)—, —CH2O— or —O—, B represents nitrogen when n is 1 or 2 and D represents —C(═O)—, or B represents CH when n is 0 and D represents —CH2O— or when n is 1 and D represents —O—, R2 represents a substituent of phenyl core Y selected from a hydrogen, a methyl, a fluorine atom, a chlorine atom and a methoxy, and HetAr represents a pyridyl or quinolyl group, possibly substituted with a group selected from a linear or branched C1-C4 alkyl, a linear or branched 1-C4 alkoxy, a halogen, and trifluoromethyl,or one of its pharmaceutically acceptable salts.