Aza and aza (n-oxy) analogs of glycine/nmda receptor...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) A61K 31/695 (2006.01) C07D 241/52 (2006.01) C07D 401/00 (2006.01) C07D 403/00 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 411/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 473/00 (2006.01) C07D 475/00 (2006.01) C07D 487/04 (2006.01) C07D 519/00 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2211608

Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia, and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment or prevention a substituted or unsubstituted pyridine and pyridine (N-oxide) analogs of 4-hydroxydihydroquinolones, tetrahydroquinoline-trione-oximes and quinoxalones of Formula (I), tautomers and pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor or tautomers, pharmaceutically acceptable salts or N-oxides thereof; wherein A, D, E, G, R, R1, X, Y, Z are as defined in the description.

Procédés de traitement ou de prévention de la déperdition neuronale associée à l'accident vasculaire cérébral, à l'ischémie, au traumatisme du système nerveux central, à l'hypoglycémie et à la chirurgie, et de traitement de maladies neurodégénératives, dont la maladie d'Alzheimer, la sclérose latérale amyotrophique, la chorée de Huntington et le syndrome de Down, de traitement ou de prévention des effets secondaires de l'hyperactivité des acides aminés excitateurs, ainsi que de traitement de l'anxiété, de la douleur chronique et des convulsions, d'induction de l'anesthésie et de traitement ou de prévention de la tolérance aux opiacées, qui consistent à administrer à un animal nécessitant un traitement ou une prévention de ce type des analogues de pyridine et de (N-oxyde) de pyridine substitués ou non substitués de 4-hydroxydihydroquinolones, de tétrahydroquinoline-trione-oximes et de quinoxalones de formule (I), des tautomères et des sels pharmaceutiquement acceptables desdites substances qui présentent une forte liaison avec le récepteur glycine, ou des tautomères, des sels ou N-oxydes pharmaceutiquement acceptables de ceux-ci, formule dans laquelle A, D, E, G, R, R¿1?, X, Y, Z sont définis dans la description.

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