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35 条记录 (耗时 0.025 秒)

    6,7-disubstituted-2,3-dihydroxyquinoxaline compounds, pharmaceutical compositions thereof, and their use as neuroleptics
    1.
    发明授权
    6,7-disubstituted-2,3-dihydroxyquinoxaline compounds, pharmaceutical compositions thereof, and their use as neuroleptics 失效
    6,7-二取代-2,3-二羟基喹喔啉化合物及其药物组合物及其作为精神安定药的用途

    公开(公告)号：US4812458A

    公开(公告)日：1989-03-14

    申请号：US92034

    申请日：1987-09-02

    申请人： Tage Honore ,  Jorgen Drejer ,  Poul Jacobsen ,  Flemming E. Nielsen

    发明人： Tage Honore ,  Jorgen Drejer ,  Poul Jacobsen ,  Flemming E. Nielsen

    IPC分类号： C07D241/44 ,  A61K31/495

    CPC分类号： C07D241/44

    摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is halogen, CN, CF.sub.3, ethynyl, or N.sub.3 andR.sup.2 is SO.sub.2 C.sub.1-3 -alkyl, CF.sub.3, NO.sub.2, ethynyl, or CN.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.

    摘要翻译： 其中R 1是卤素，CN，CF 3，乙炔基或N 3和R 2的具有式“IMAGE”的杂环二羟基喹喔啉化合物是SO 2 C 1-3 - 烷基，CF 3，NO 2，乙炔基或CN。 本发明还涉及制备化合物的方法，其药物组合物及其用途。 该化合物可用于治疗由兴奋性神经递质特别是quisqualate受体的多动症引起的适应症，特别是作为精神安定药物。

    Benzo[f]quinoxaline-2,3(1H,4H)-diones
    6.
    发明授权
    Benzo[f]quinoxaline-2,3(1H,4H)-diones 失效
    苯并[f]喹喔啉-2,3（1H，4H） - 二酮

    公开(公告)号：US5026704A

    公开(公告)日：1991-06-25

    申请号：US456325

    申请日：1989-12-26

    申请人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    发明人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    IPC分类号： A61K31/495 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  C07D20060101 ,  C07D241/38 ,  C07D241/44 ,  C07D241/52 ,  C07D403/06

    CPC分类号： C07D241/38 ,  C07D241/44 ,  C07D241/52 ,  C07D403/06

    摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substututed by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, Cl or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 - alkyl; orR.sup.7 and R.sup.8 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.6 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 -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.

    Quinoxaline compounds and their preparation and use
    8.
    发明授权
    Quinoxaline compounds and their preparation and use 失效
    喹喔啉化合物及其制备和用途

    公开(公告)号：US5153195A

    公开(公告)日：1992-10-06

    申请号：US794262

    申请日：1991-11-15

    申请人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    发明人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    IPC分类号： C07D241/52 ,  C07D471/04 ,  C07D491/06

    CPC分类号： C07D241/52 ,  C07D471/04 ,  C07D491/06

    摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy; andR.sup.5 and R.sup.6 together form a fused phenyl, cyclohexyl or pyridyl ring, which is optionally substituted with halogen or CN; and R.sup.7 and R.sup.8 independently are hydrogen, hydroxy, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.5 and R.sup.6 independently are hydroxy, hydrogen, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; and R.sup.7 and R.sup.8 together form a fused phenyl, cyclohexyl or pyridyl ring which is optionally substituted with halogen or CN.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.

    摘要翻译： 具有式“IMAGE”的杂环二羟基喹喔啉化合物，其中R 1是羟基; 并且R 5和R 6一起形成稠合的苯基，环己基或吡啶环，其任选被卤素或CN取代; 并且R 7和R 8独立地是氢，羟基，NO 2，卤素，CN，CF 3，C 1-4 - 烷氧基，乙酰基，SO 2 NHCOCO 2Et，SO 2 NR'R'或SO 2 R'，其中R'是氢或C 1-4烷基; 或R 5和R 6独立地为羟基，氢，NO 2，卤素，CN，CF 3，C 1-4 - 烷氧基，乙酰基，SO 2 NHCOCO 2 Et，SO 2 NR'R'或SO 2 R'，其中R'为氢或C 1-4 - 烷基; 并且R 7和R 8一起形成任选被卤素或CN取代的稠合的苯基，环己基或吡啶基环。 本发明还涉及制备化合物的方法，其药物组合物及其用途。 该化合物可用于治疗由兴奋性神经递质特别是quisqualate受体的多动症引起的适应症，特别是作为精神安定药物。

    Quinoxaline compound and their preparation and use
    9.
    发明授权
    Quinoxaline compound and their preparation and use 失效
    喹啉化合物及其制备和使用

    公开(公告)号：US5081123A

    公开(公告)日：1992-01-14

    申请号：US451382

    申请日：1989-12-15

    申请人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    发明人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    IPC分类号： A61K31/495 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  C07D241/52 ,  C07D471/04 ,  C07D487/04 ,  C07D491/06

    CPC分类号： C07D241/52 ,  C07D471/04 ,  C07D491/06

    摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy;R.sup.5 and R.sup.6 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.7 and R.sup.8 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.7 and R.sup.8 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.5 and r.sup.6 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -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.