Pyridinecarboxamide derivatives

Details Pyridinecarboxamide derivatives Pyridinecarboxamide derivatives

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) C07D 213/80 (2006.01) C07D 213/82 (2006.01)

Patent

CA 2243445

N-(12-Nitroxydodecyl)-6-(4-ethyl or isoproyl-1-piperazinyl)pyridine-3- carboxamide or physiologically acceptable salts thereof. These compounds are excellent in the effects of inhibiting cerebral edema, particularly ischemic cerebral edema, and inhibiting delayed neuron death (or inhibiting calcium inflow into neuros). They are useful as a cerebral edema inhibitor or a cerebrovascular disorder remedy, because cerebral edema is a pathological condition accompanying cerebrovascular disorder, particularly one observed in an acute stage. Because also they scarcely exhibit any behavior suppressing activity believed to be a side effect in the therapy of cerebrovascular disorder in an acute stage, they are especially excellent as a remedy therefor. In addition, they have the effects of protecting the brain (i.e., an antianoxic effect), increasing cerebral blood flow, and inhibiting lipid peroxidation, which further enhance the usefulness as a cerebrovascular disorder remedy.

L'invention concerne un N-(12-nitroxydodécyl)-6-(4-éthyl ou isopropyl-1-pipérazinyl)pyridine-3-carboxamide ou ses sels physiologiquement acceptables. Ces composés sont extrêmement efficaces pour inhiber un oedème cérébral, en particulier un oedème cérébral ischémique, et inhiber la mort neuronale différée (ou inhiber l'afflux de calcium dans les neurones). Ils s'utilisent comme inhibiteur de l'oedème cérébral ou comme remède aux troubles cérébrovasculaires, car l'oedème cérébral constitue un état pathologique accompagnant les troubles cérébrovasculaires, en particulier du type de ceux qui sont observés en phase aiguë. Etant donné que ces composés ne présentent pratiquement aucune activité affectant le comportement, supposée être un effet secondaire dans la thérapie des troubles cérébrovasculaires en phase aiguë, ils constituent un excellent remède à ces troubles. En outre, ils ont un effet protecteur sur le cerveau (par ex. un effet antianoxique), augmentent le flux sanguin dans le cerveau, et inhibent la péroxydation lipidique, ce qui renforce leur utilité comme remède aux troubles cérébrovasculaires.

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