Novel 2-phenylpiperazine derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 241/04 (2006.01) A61K 31/496 (2006.01) C07D 241/08 (2006.01) C07D 401/06 (2006.01) C07D 403/04 (2006.01) C07D 403/06 (2006.01)

Patent

CA 2419665

The present invention is to offer a useful novel compound as a tachykinin antagonist. This invention is a novel 2-phenylpiperazine derivative having an excellent tachykinin antagonistic action. A piperazine derivative of the present invention has an excellent tachykinin receptor antagonistic activity and exhibits a strong inhibitory action against tachykinin-induced increase of vascular permeability in vivo tests. Moreover, it shows a preferred transfer into blood and a long half-life in blood in pharmacokinetic tests of oral administration to rats or guinea pigs, and is very stable in blood plasma of various animals. Consequently, a piperazine derivative of the present invention is very useful as a novel tachykinin antagonist.

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