Aryl substituted tetrahydroindazoles and their use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/56 (2006.01) A61K 31/416 (2006.01) A61K 31/4439 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2419966

Disclosed are compounds of formula (I) and the pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, n, and Ar are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

L'invention concerne des composés de la formule (I) et leurs sels pharmaceutiquement acceptables, dans laquelle les variables R¿1?, R¿2?, R¿3?, n, et Ar sont tels que définis dans le mémorandum descriptif. Ces composés sont des agonistes hautement sélectifs, des antagonistes ou des agonistes inverses pour les récepteurs cérébraux de GABA¿A?, ou des promédicaments d'agonistes, d'antagonistes ou d'agonistes inverses pour les récepteurs cérébraux de GABA¿A?. Ces composés sont donc utiles pour le diagnostic et le traitement de l'anxiété, de la dépression, du syndrome de Down, du trouble du sommeil et du trouble épileptique, de la surdose de médicaments à base de benzodiazépine, et pour une stimulation améliorée de la mémoire.

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