QUINOKALINE COMPOUNDS AND THEIR USE

摘要

Heterocyclic dihydroxyquinoxaline compounds having the formula wherein R<1> is C1-12-alkyl, which may obtionally be substituted by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C3-8-cycloalkyl, aryl, aralkyl; and wherein R<6> is, hydrogen, halogen, CN, CF3, NO2, or OR min , wherein R min is C1-4-alkyl and R<5>, R<7> and R<8> is hydrogen, provided R<6> is not CF3, OCH3, NO2, CL or Br when R<1> is CH3; or R<6> and R<7> independently are NO2, halogen, CN, CF3, or OR min , wherein R min is C1-4-alkyl, and R<5> and R<8> are each hydrogen; or R<5> and R<6> together form a further fused aromatic ring, which may be substituted with halogen, NO2, CN, CF3 or OR min , wherein R min is C1-4-alkyl, and R<7> and R<8> independently are hydrogen, halogen, CN, CF3, NO2 or OR min wherein R min is C1-4-alkyl; or R<7> and R<8> together form a further fused aromatic ring, which may be substituted with halogen, NO2, CN, CF3 or OR min , wherein R min is C1-4-alkyl, and R<5> and R<6> independently are hydrogen, halogen, CN, CF3, NO2 or OR min , wherein R min is C1-4-alkyl. The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use. The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.