首页> 外国专利> 5H,10H-IMIDAZO1,2-AINDENO1,2-EPYRAZIN-4-ONE DERIVATIVES, INTERMEDIATES,PREPARATION AND USE THEREOF, AND DRUGS CONTAINING SAID DERIVATIVES

5H,10H-IMIDAZO1,2-AINDENO1,2-EPYRAZIN-4-ONE DERIVATIVES, INTERMEDIATES,PREPARATION AND USE THEREOF, AND DRUGS CONTAINING SAID DERIVATIVES

机译:5H,10H-咪唑并[1,2-A]茚并[1,2-E]吡嗪-4-酮衍生物,中间体,制备和使用以及含有所述衍生物的药物

摘要

A compound of formula (II): in which 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 (II) can be used to prepare compounds of formula (I): in which R and R1 have the same meanings as above. 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. The compounds of formula (I) are also non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.
机译:式(II)的化合物:其中R为氢原子或羧基,烷氧基羰基,-CO-NR4R5,-PO3H2或-CH2OH基团,且R1为-alk-NH2,-alk-NH-CO-R3 ,-alk-COOR4,-alk-CO-NR5R6或-CO-NH-R7基团。式(II)的化合物可用于制备式(I)的化合物:其中R和R 1具有与上述相同的含义。式(I)的化合物具有有价值的药理学性质,并且是α-氨基-3-羟基-5-甲基-5-甲基-4-异恶唑丙酸(AMPA)受体(也称为喹喹酸酯)的拮抗剂。式(I)的化合物也是N-甲基-D-天冬氨酸(NMDA)受体的非竞争性拮抗剂,并且更具体地是NMDA受体甘氨酸调节位点的配体。

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