Benzodiazepine compound and pharmaceutical composition

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 243/12 (2006.01) A61K 31/551 (2006.01) A61P 9/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 491/04 (2006.01) C07D 495/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2715872

The present invention provides a novel benzodiazepine compound that blocks the I Kur current or the Kv1.5 channel or the IKACH current (the GIRK1/4 channel) potently and more selectively than other K+ channels. The benzodiazepine com-pound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or low-er alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; X A and X B are each inde-pendently bond, lower alkylene, etc.

La présente invention concerne un nouveau composé de benzodiazépine qui bloque le courant IKur ou le canal Kv1.5 ou le courant IKACH (le canal GIRK1/4) efficacement et plus sélectivement que d'autres canaux K+. Le composé benzodiazépine de l'invention est représenté par la formule générale (1) dans laquelle R1, R2, R3, et R4 représentent chacun indépendamment un atome d'hydrogène ou un groupe alkyle inférieur; R2 et R3 peuvent être liés pour former un groupe alkylène inférieur; A1 représente un groupe alkylène inférieur éventuellement substitué par un ou plusieurs groupes hydroxy; et R5 est un groupe représenté par dans lequel R6 et R7 représentent chacun indépendamment un atome d'hydrogène ou un groupe organique; XA et XB représentent chacun indépendamment une liaison, un groupe alkylène inférieur, etc.

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