Quinoxaline compounds and their preparation and use

C - Chemistry – Metallurgy – 07 – D

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C07D 241/44 (2006.01) A61K 31/495 (2006.01) C07D 241/38 (2006.01) C07D 241/52 (2006.01) C07D 403/06 (2006.01)

Patent

CA 1321587

ABSTRACT Heterocyclic dihydroxyquinoxaline compounds having the formula Image wherein R1 is C1-12-alkyl, which may obtionally be substituted by hydroxy, formyl, carboxy, carboxylic esters, amides or ami- nes, C3-8-cycloalkyl, aryl, aralkyl; and wherein R6 is, hy- drogen, halogen, CN, CF3, NO2, or OR', wherein R' is C1-4- alkyl and R5, R7 and R8 is hydrogen, provided R6 is not CF3, OCH3, NO2, CL or Br when R1 is CH3; or R6 and R7 independently are NO2, halogen, CN, CF3, or OR', wherein R' is C1-4-alkyl, and R5 and R8 are each hydrogen; or R5 and R6 together form a further fused aromatic ring, which may be substituted with halogen, NO2, CN, CF3 or OR', wherein R' is C1-4-alkyl, and R7 and R8 independently are hydrogen, halogen, CN, CF3, NO2 or OR', wherein R' is C1-4-alkyl; or R7 and R8 together form a further fused aromatic ring, which may be substituted with halogen, NO2, CN, CF3 or OR', wherein R' is C1-4-alkyl, and R5 and R6 independently are hydrogen, halogen, CN, CF3, NO2 or OR', wherein R' 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.

582104

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