4-aryl-3-hydroxyquinolin-2-one derivatives as ion channel...

C - Chemistry – Metallurgy – 07 – D

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C07D 215/227 (2006.01) A61K 31/47 (2006.01) C07D 215/18 (2006.01) C07D 215/20 (2006.01) C07D 215/38 (2006.01) C07D 215/40 (2006.01)

Patent

CA 2266605

There is provided novel substituted 4-aryl-3-hydroxyquinolin-2-one derivatives of formula (I) wherein R is hydrogen or methyl; R1, R2, R3 and R4 each are independently hydrogen, bromo, chloro or trifluoromethyl, and when R1, R3 and R4 are hydrogen, R2 is nitro; R5 is hydrogen or methyl; and R6 is bromo or chloro; or a nontoxic pharmaceutically acceptable salt thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.

Cette invention concerne de nouveaux dérivés de 4-aryl-3-hydroxyquinolin-2-one substitués, lesquels correspondent à la formule (I) où R représente hydrogène. R?1¿, R?2¿, R?3¿ et R?4¿ représentent chacun indépendamment hydrogène, bromo, chloro ou trifluorométhyle, étant entendu que lorsque R?1¿, R?3¿ et R?4¿ représentent hydrogène, R?2¿ représente nitro. R?5¿ représente hydrogène ou méthyle, tandis que R?6¿ représente bromo ou chloro. Cette invention concerne également les sels de ces dérivés acceptables et non toxiques sur le plan pharmaceutique, lesquels peuvent être utilisés en qualité d'ouvreurs de canaux potassium activés par du calcium et à conductance élevée. Ces dérivés sont utiles dans le traitement des troubles qui résultent de l'ouverture de canaux potassium.

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