Benzyloxypropylamine derivative

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 233/18 (2006.01) A61K 31/165 (2006.01) A61K 31/166 (2006.01) A61K 31/192 (2006.01) A61K 31/22 (2006.01) A61K 31/27 (2006.01) A61K 31/40 (2006.01) A61K 31/4402 (2006.01) A61K 31/4406 (2006.01) A61K 31/4409 (2006.01) A61K 31/445 (2006.01) A61K 31/4465 (2006.01) A61K 31/4468 (2006.01) A61K 31/4545 (2006.01) A61K 31/455 (2006.01) A61K 31/47 (2006.01) A61K 31/4965 (2006.01) A61P 1/08 (2006.01) A61P 1/12 (2006.01) A61P 9/10 (2006.01) A61P 17/00 (2006.01) A61P 21/02 (2006.01) A61P 25/04 (2006.01) A61P 25/08 (

Patent

CA 2603030

Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.

La présente invention concerne un nouveau dérivé de la benzyloxypropylamine doté d~un excellent effet antagoniste sur les récepteurs de la tachykinine. Ce composé présente un bon transfert dans le sang et une longue demi-vie sanguine lors du test cinétique sanguin effectué sur un cobaye auquel le composé est administré par voie orale, et est stable dans le plasma animal. Le composé présente également un transfert important dans le système nerveux central lorsqu~il est administré par voie orale à un cobaye à une certaine dose. Par conséquent, le dérivé de la benzyloxypropylamine est très utile en tant que nouvel agent anti-tachykinine.

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