Inhibitor of kainic acid neurotoxicity and pyridothiazine...

C - Chemistry – Metallurgy – 07 – D

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C07D 513/04 (2006.01) A61K 31/54 (2006.01) A61K 31/5415 (2006.01) A61K 31/55 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2237911

Neuron protective agents on the basis of the inhibition of neuronotoxicity of kainic acid and compounds useful as such agents. Pyridothiazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and neuronotoxicity inhibitors containing as the active ingredient these compounds or pharmaceutically acceptable salts thereof, wherein A represents a pyridine ring; formula (II) represents formula (III) or formula (IV); and R1, R2, R3, R4 and R5 are the same or different and each represents hydrogen, optionally substituted lower alkyl, cycloalkyl, alkenyl, aryl, carboxy or lower alkoxycarbonyl or does not exist, or R2 and R3 together form a nitrogenous heterocycle optionally having a nitrogen atom as another heteroatom, being fused with a benzene ring, or being substituted by lower alkyl.

Agents de protection neuronale basés sur l'inhibition de la neurotoxicité de l'acide kaïnique et composés utiles en tant qu'agents de protection de ce type. Dérivés de la pyridothiazine de formule générale (I), ou leurs sels pharmaceutiquement acceptables, et inhibiteurs de la neurotoxicité contenant comme agents actifs ces composés ou ces sels pharmaceutiquement acceptables, où A représente un noyau pyridinique; (II) représente (III) ou (IV); et R?1¿, R?2¿, R?3¿, R?4¿ et R?5¿ sont identiques ou différents et représentent hydrogène, alkyle inférieur éventuellement substitué, cycloalkyle, alcényle, aryle, carboxy ou alcoxycarbonyle, ou bien n'existent pas, ou bien R?2¿ et R?3¿ ensemble constituent un hétérocycle azoté possédant éventuellement comme autre hétéroatome un atome d'azote, condensé avec un noyau benzénique ou substitué par un alkyle inférieur.

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