Benzoquinolinesulfonamide derivatives useful as rho-kinase...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/12 (2006.01) A61K 31/551 (2006.01) A61P 9/04 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 11/06 (2006.01) A61P 13/02 (2006.01) A61P 15/10 (2006.01) A61P 25/08 (2006.01) A61P 27/06 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2610166

The present invention relates to a compound having a highly selective Rho-kinase inhibiting activity and being useful as a therapeutic agent for a disease such as hypertension, pulmonary hypertension, cerebral vasospasm, cardiac angina, cardiac failure, arteriosclerosis, glaucoma, dysuria, asthma, or erectile dysfunction, and a drug containing the compound. Provided is a homopiperazine derivative represented by General Formula (1), an acid addition salt thereof, or a solvate of the derivative or the salt: (see formula 1) (wherein R1 represents an amino acid residue; R2 represents a hydrogen atom or an alkyl group; R3 represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen atom, a nitrile group, or a hydroxyl group; and R4 represents a hydrogen atom, a halogen atom, or a hydroxyl group).

La présente invention concernce un composé qui a un effet inhibiteur hautement sélectif sur la Rho-kinase et qui est utile comme agent thérapeutique pour des maladies comprenant l~hypertension, l~hypertension pulmonaire, l~angiospasme cérébral, l~angine de poitrine, la défaillance cardiaque, l~artériosclérose, le glaucome, la dysurie, l~asthme et la défaillance érectile. L~invention décrit un dérivé de l~homopipérazine représenté par la formule générale (1), son sel d~addition d~acide ou un solvate du dérivé ou du sel: dans laquelle R1 représente un résidu d~acide aminé; R2 représente un atome d~hydrogène ou un groupe alkyle; R3 représente un atome d~hydrogène, un groupe alkyle, un groupe alcényle, un groupe alcynyle, un groupe alcoxy, un atome d~halogène, un groupe nitrile ou un groupe hydroxyle; et R4 représente un atome d~hydrogène, un atome d~halogène ou un groupe hydroxyle.

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