Use of bioactive metabolites of gepirone for the treatment...

A - Human Necessities – 61 – K

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A61K 31/506 (2006.01) A61P 25/24 (2006.01)

Patent

CA 2395458

Bioactive gepirone metabolites, such as 3-OH gepirone (4,4,-dimethyl-3-hydroxy- 1-[4-[4-(2-pyrimidinyl)-1-piper- azinyl]butyl]-2,6-piperidinedione), and their pharmaceutically acceptable salts and hydrates, can be used to alleviate psychological disorders or the symptoms thereof. The use of these compounds provides advantages over other therapeutic azapirones as they possess superior bioavailability, faster onset of action, and more stable plasma levels when administered to a mammal.

L'invention concerne des métabolites bioactifs de gépirone, tels que la 3-OH gépirone (4,4,-diméthyl-3-hydroxy-1-[4-[4-(2-pyrimidinyl)-1-pipérazinyl]butyl]-2,6-pipéridinedione), ainsi que leurs sels et hydrates acceptables sur le plan pharmaceutique, qui peuvent être utilisés afin de remédier des troubles psychologiques ou des symptômes associés. L'utilisation de ces composés assure des avantages par rapport aux autres azapirones thérapeutiques car ils possèdent une biodisponibilité supérieure, un début d'action plus rapide, et des taux plasmatiques plus stables lorsqu'ils sont administrés à un mammifère.

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