Aryl substituted pyrimidines and the use thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 239/46 (2006.01) A61K 31/505 (2006.01) A61P 25/00 (2006.01) C07D 239/32 (2006.01) C07D 239/42 (2006.01)

Patent

CA 2479036

This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aryl-substituted pyrimidine compounds of Formula (I): or a pharmaceutically acceptable salt, or solvate thereof, wherein A, R1, R2, R3 and R4 are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

L'invention concerne une méthode de traitement de troubles répondant au blocage des canaux à ion sodium au moyen de nouveaux composés de pyrimidine substituées par aryle de formule (I) ou d'un sel acceptable sur le plan pharmaceutique ou d'un solvate de ceux-ci. Dans la formule (I), A, R¿1?, R¿2?, R¿3? et R¿4? sont définis dans la description. L'invention concerne également l'utilisation des composés de formule I dans le traitement de lésions neuronales engendrées par une ischémie globale et focale, dans le traitement ou la prévention d'états neurodégénératifs, tels que la sclérose latérale amyotrophique (ALS) et dans le traitement, la prévention ou l'amélioration de douleurs aiguës ou chroniques, comme agents anti-tinnitus, comme anti-convulsifiants et comme dépresseurs antimaniaques, comme anesthésiques locaux, comme agents antiarythmiques et dans le traitement ou la prévention de neuropathie diabétique.

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