Oxa- or thia-aliphatically bridged quinoxaline-2,3-diones

C - Chemistry – Metallurgy – 07 – D

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C07D 513/06 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/675 (2006.01) C07D 498/06 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2157231

Oxa- or thia-aliphatically bridged quinoxaline-2,3-diones of the general formula I Image (I), wherein A1 is lower alkylidene or a group of the formula >CH-A4-R4 (Ia), A2 is lower alkylidene or a group of the formula >CH-A4-R4 (Ia), >C=O (Ib) or >CH(OH)-As-R4 (Ic), A3 is oxy, optionally oxidised thio or a group >C(=O) (Ib), A4 is lower alkylene, A5 is lower alkylene or a direct bond, n is 0 or 1, R1 and R2 are each independently of the other hydrogen, unsubstituted or lower alkyl- and/or lower alkanoyl-substituted amino, nitro, lower alkanoyl, free or etherified or esterified hydroxy, free or esterified or amideated carboxy, cyano, optionally halogenated lower alkyl or halogen, R3 is hydrogen or hydroxy and R4 is hydrogen, cyano, free or esterified or amideated carboxy, free or esterified phosphono or 5- telldzolyl, and the pharmaceutically acceptable salts thereof have antagonistic properties with respect to excitatory amino acids and can be used as anticonvulsive and anti- neurodegenerative medicinal active ingredients.

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