Substituted 4-oxo-napthyridine-3-carboxamides as gaba brain...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/44 (2006.01)

Patent

CA 2301599

The present invention encompasses structures of Formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, or heteroaryl, which 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. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

La présente invention concerne des structures de la formule (I) ou leurs sels non toxiques et acceptables du point de vue pharmaceutique; dans la formule (I): X est hydrogène, halogène, alkyle (non) substitué, alcoxy ou amine (non) substitué; et Y est alkyle (non) substitué, aryle ou hétéroaryle; ces composés sont des agonistes, antagonistes ou agonistes inverses de récepteurs de GABAa du cerveau ou des promédicaments d'agonistes, d'antagonistes ou d'agonistes inverses de récepteurs de GABAa du cerveau. Ces composés s'utilisent dans le diagnostic et le traitement de l'anxiété, du syndrome de Down, du sommeil, de troubles cognitifs et épileptiques et de l'overdose de médicaments au benzodiazépine et pour l'activation de la vigilance.

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