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    [1,2,4]triazolo[4,3-a]quinoxaline compounds
    1.
    发明授权
    [1,2,4]triazolo[4,3-a]quinoxaline compounds 失效
    [1,2,4]三唑并[4,3-a]喹喔啉化合物

    公开(公告)号：US5532236A

    公开(公告)日：1996-07-02

    申请号：US237518

    申请日：1994-05-03

    申请人： Poul Jacobsen ,  Flemming E. Nielsen ,  Lone Jeppesen

    发明人： Poul Jacobsen ,  Flemming E. Nielsen ,  Lone Jeppesen

    IPC分类号： A61K31/495 ,  A61P21/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  C07D487/04 ,  C07D487/14 ,  A61K31/505 ,  A61K31/54 ,  C07D417/14

    CPC分类号： C07D487/04

    摘要： The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which is optionally substituted with one, two or three substituents, wherein each substituent is independently phenyl or C.sub.1-6 -alkyl, or one of R.sup.1 and R.sup.2 is a fused ring system comprising a 5- or 6-membered nitrogen-containing heterocyclic ring and a benzene, pyridine, pyrimidine or pyrazine ring, wherein the fused ring system is optionally substituted with phenyl or C.sub.1-6 -alkyl; and the other of R.sup.1 and R.sup.2 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, COC.sub.1-6 -alkyl or SO.sub.2 NR'R", wherein R' and R" are independently hydrogen or C.sub.1-6 -alkyl; and X is O or S; and pharmaceutically acceptable salts thereof. The compounds have affinity for the AMPA receptors and are antagonists in connection with this type of receptors which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.

    摘要翻译： 本发明涉及式Ⅰ化合物[1,2,4]三唑并[4,3-a喹喔啉衍生物，其中R 1和R 2之一为5-或6-元含氮杂环，其中 任选地被一个，两个或三个取代基取代，其中每个取代基独立地是苯基或C 1-6 - 烷基，或者R 1和R 2中的一个是包含5或6元含氮杂环的稠环体系和 苯，吡啶，嘧啶或吡嗪环，其中稠环体系任选被苯基或C 1-6 - 烷基取代; R 1和R 2中的另一个为氢，C 1-6 - 烷基，C 1-6 - 烷氧基，卤素，NO 2，NH 2，CN，CF 3，COC 1-6 - 烷基或SO 2 NR'R“ '独立地是氢或C 1-6 - 烷基; X为O或S; 及其药学上可接受的盐。 这些化合物对AMPA受体具有亲和力，并且是与这种类型的受体有关的拮抗剂，这使得它们可用于治疗CNS疾病，特别是在治疗由兴奋性氨基酸的多动症引起的许多适应症中的任何一种。

    Heterocyclic compounds, their use and preparation
    2.
    发明授权
    Heterocyclic compounds, their use and preparation 失效
    杂环化合物，其使用和制备

    公开(公告)号：US5559106A

    公开(公告)日：1996-09-24

    申请号：US350744

    申请日：1994-12-07

    申请人： Poul Jacobsen ,  Flemming E. Nielsen ,  Lone Jeppesen

    发明人： Poul Jacobsen ,  Flemming E. Nielsen ,  Lone Jeppesen

    IPC分类号： A61K31/495 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  C07D487/04 ,  C07F9/6561 ,  A61K31/675 ,  C07F9/6524

    CPC分类号： C07D487/04 ,  C07F9/6561

    摘要： Quinoxaline compounds of the general formula ##STR1## wherein R.sup.1 is COX', POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently are hydrogen, alkyl, halogen, NH.sub.2, NO.sub.2, CN, CF.sub.3, SO.sub.2 NY'Y" or COZ' wherein Z' is NY'Y" or alkyl and Y' and Y" independently are hydrogen or alkyl, triazolyl, imidazolyl, imidazolyl substituted with phenyl or alkyl, or R.sup.6 and R.sup.7, or R.sup.8 and R.sup.9, together form a further fused ring, are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

    摘要翻译： 其中R1是COX'，POX'X“或被COX'或POX'X”取代的烷基的喹喔啉化合物，X'和X“独立地是羟基或烷氧基，R6，R7 ，R8和R9独立地是氢，烷基，卤素，NH2，NO2，CN，CF3，SO2NY'Y“或COZ”，其中Z'是NY'Y“或烷基，Y'和Y'独立地是氢或 烷基，三唑基，咪唑基，被苯基或烷基取代的咪唑基，或R6和R7或R8和R9一起形成另外的稠环，可用于治疗由兴奋性神经递质的多动症引起的适应症。