申请人:NOVO NORDISK A/S
公开号:EP0374534A1
公开(公告)日:1990-06-27
Heterocyclic dihydroxyquinoxaline compounds having the formula
wherein
R¹ is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy;
R⁵ and R⁶ together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R⁷ and R⁸ independently are hydrogen, NO₂, halogen, CN, SO₂NR′R′, SO₂R′, CF₃, or OR′, wherein R′ is hydrogen or C₁₋₄-alkyl; or
R⁷ and R⁸ together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R⁵ and R⁶ independently are hydrogen, NO₂, halogen, CN, SO₂NR′R′, SO₂R′, CF₃, or OR′, wherein R′ is hydrogen or 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.
具有以下式子的杂环二羟基喹喔啉化合物
其中
R¹ 是羟基、烷氧基、芳氧基、烷氧基、环烷氧基、环烷氧基或酰氧基;
R⁵ 和 R⁶ 共同形成另一个被氢、卤素或 CN 取代的融合环,且 R⁷ 和 R⁸ 独立为氢、NO₂、卤素、CN、SO₂NR′R′、SO₂R′、CF₃或 OR′,其中 R′是氢或 C₁₋₄-烷基;或
R⁷ 和 R⁸ 共同形成另一个被氢、卤素或 CN 取代的融合环,且 R⁵ 和 R⁶ 独立为氢、NO₂、卤素、CN、SO₂NR′R′、SO₂R′、CF₃或 OR′,其中 R′是氢或 C₁₋₄-烷基。
本发明还涉及化合物的制备方法、其药物组合物及其用途。
本发明化合物可用于治疗兴奋性神经递质,特别是喹乙醇受体的过度活跃引起的症状,尤其是作为神经抑制剂。