| abstract |
The present invention relates to novel indole-2,3-dione-3-oxime derivatives capable of antagonising the effect of excitatory amino acids, such as glutamate. More specifically the novel indole-2,3-dione-3-oxime derivatives of the invention may be described by general formula (I), wherein R 3 represents “Het”, or a group of formula (II), wherein “Het” represents a saturated or unsaturated, 4 to 7 membered, monocyclic, heterocyclic ring, at least one of R 31 , R 32 , and R 33 independendy represents hydrogen, alkyl, or hydroxyalkyl, and at least one of R 31 , R 32 , and R 33 independently represents (CH 2 ) n R 34 ; wherein R 34 represents hydroxy, carboxy, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, cycloalkoxycarbonyl, cycloalkylalkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, CONR 35 R 36 , or “Het”; wherein n is 0, 1, 2, or 3; and R 5 represents phenyl, naphthyl, thienyl, or pyridyl, all of which may be substituted. “A” represents a ring of five to seven atoms fused with the benzo ring at the positions marked “a” and “b”, and formed by the following bivalent radicals: a-NR 6 —CH 2 —CH 2 -b; a-CH 2 —NR 6 —CH 2 -b; a-CH 2 —CH 2 —NR 6 -b; a-NR 6 —CH 2 —CH 2 —H 2 -b; a-CH 2 —NR 6 —CH 2 —CH 2 -b; a—CH 2 —CH 2 —NR 6 —CH 2 -b; a-CH 2 —CH 2 —CH 2 —NR 6 -b; a-NR 6 —CH 2 —CH 2 —CH 2 —CH 2 -b; a-CH 2 —NR 6 —CH 2 —CH 2 —CH 2 -b; a-CH 2 —CH 2 —NR 6 —CH 2 —CH 2 -b; a-CH 2 —CH 2 —CH 2 —NR 6 —CH 2 -b; or a-CH 2 —CH 2 —CH 2 —CH 2 —NR 6 -b; wherein R 6 represents hydrogen alkyl or CH 2 CH 2 OH; or a pharmaceutically acceptable salt thereof. |