5h,10h-imidazo[1,2-a]indeno[1,2-e]pyrazin-4-one derivatives,...

Details 5h,10h-imidazo[1,2-a]indeno[1,2-e]pyrazin-4-one derivatives,... 5h,10h-imidazo[1,2-a]indeno[1,2-e]pyrazin-4-one derivatives,...

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/675 (2006.01) C07D 233/90 (2006.01) C07D 403/10 (2006.01) C07F 9/6506 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2215469

Compounds of formula (I), wherein R is a hydrogen atom or a carboxy, alkoxycarbonyl, -CO-NR4R5, -PO3H2 or -CH2OH radical, and R1 is an -alk-NH2, -alk-NH-CO-R3, -alk-COOR4, -alk-CO-NR5R6 or -CO-NH-R7 radical. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the alpha -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.

Composés de formule (I), dans laquelle: R représente un atome d'hydrogène ou un radical carboxy, alcoxycarbonyle, -CO-NR4R5, -PO3H2 ou -CH2OH, et R1 représente un radical -alk-NH2, -alk-NH-CO-R3, -alk- COOR4, -alk-CO-NR5R6 ou -CO-NH-R7. Les composés de formule (I) présentent des propriétés pharmacologiques intéressantes. Ces composés sont des antagonistes du récepteur de l'acide .alpha.-amino--3-hydroxy-5-méthyl-4-isoxazolepropionique (AMPA), connu aussi sous le nom de récepteur du quisqualate. Par ailleurs, les composés de formule (I) sont des antagonistes non compétitifs du récepteur N-méthyl-D- aspartate (NMDA) et, plus particulièrement, ce sont des ligands pour les sites modulateurs de la glycine du récepteur NMDA.

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