1,2,3,4-tetrahydroquinoxalinedione derivative

Details 1,2,3,4-tetrahydroquinoxalinedione derivative 1,2,3,4-tetrahydroquinoxalinedione derivative

C - Chemistry, Metallurgy

07

D

C07D 403/04 (2006.01) A61K 31/498 (2006.01) C07D 241/44 (2006.01) C07D 471/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2199468

A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier. (see formula I) wherein symbols in the above formula represent the following meanings, respectively: X: N, CH, R: an imidazolyl group or a di-lower alkylamino group, R1: (1) a halogen atom, a nitro group, a cyano group, a carboxyl group, an amino group, a mono- or di-lower alkylamino group, a lower alkanoyl group, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group or a carbamoyl group, (2) a lower alkyl group or lower alkoxyl group which may be substituted by a halogen atom, a carboxyl group or an aryl group, (3) a phenyloxy group which may be substituted by a lower alkoxycarbonyl group or a carboxyl group, R2: a hydroxyl group, a lower alkoxyl group, an amino group or a mono- or di-lower alkylamino group, A: a lower alkylene group which may be substituted or a group represented by the formula -O-B-, and B: a lower alkylene group, with the proviso that the case wherein R represents an imidazolyl group, R1 represents a cyano group, A represents an ethylene group and R2 represents a hydroxyl group is excluded.

Dérivé de 1,2,3,4-tétrahydroquinoxalindione représenté par la formule générale (I) ou sel de ce composé, antagoniste du récepteur de NMDA-glycine et/ou du récepteur d'AMPA et inhibiteur de neurocytotoxicité du kaïnate contenant ledit composé, et composition médicinale comprenant ce dernier et des véhicules acceptables en pharmacologie. Dans la formule, X représente N ou CH; R représente imidazolyle ou di(alkyle inférieur)amino; R<1> représente (1) halogéno, nitro, cyano, carboxy, amino, mono- ou di(alkyle inférieur)amino, alcanoyle inférieur, alkylthio inférieur, alkylsulfinyle inférieur, alkylsulfonyle inférieur, ou carbamoyle, (2) alkyle inférieur ou alcoxy inférieur pouvant être substitué par halogéno, carboxy ou aryle, ou (3) phényloxy pouvant être substitué par alcoxycarbonyle inférieur ou carboxy; R<2> représente hydroxy, alcoxy inférieur, amino, ou mono- ou di(alkyle inférieur)amino; et A représente alkylène éventuellement substitué ou -O-B- (B étant alkylène inférieur); à condition que l'on excepte le cas où R représente imidazolyle, R<1> représente cyano, A représente éthylène et R<2> représente hydroxy.

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