Radiolabeled neurokinin-1 receptor antagonists

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01) A61K 31/454 (2006.01) A61K 51/00 (2006.01)

Patent

CA 2499825

The present invention is directed to radiolabeled neurokinin-1 receptor antagonists of the formula: (See above formula) wherein: A is -CD2- or -CH2CH2-; or a pharmaceutically acceptable salt thereof, which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals; examples are [18F][2- fluorodideuteromethoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-benzyl]-([2S,3S]-2- phenyl-piperidin- 3-yl)-amine, and pharmaceutically acceptable salts thereof; and [18F][3- fluoroethoxy-5-(5- trifluoromethyl-tetrazol-1-yl)-benzyl]-([2S,3S]-2-phenyl-piperidin-3-yl)- amine, and pharmaceutically acceptable salts thereof.

La présente invention concerne des antagonistes radiomarqués du récepteur de la neurokinine-1, utilisés pour le marquage et l'imagerie diagnostique des récepteurs de la neurokinine-1 chez les mammifères.

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