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219 条记录 (耗时 0.019 秒)

    Quinoxaline compounds and their preparation and use
    35.
    发明公开
    Quinoxaline compounds and their preparation and use 失效
    喹喔啉化合物及其制备和使用

    公开(公告)号：EP0374534A1

    公开(公告)日：1990-06-27

    申请号：EP89121912.3

    申请日：1989-11-28

    申请人： NOVO NORDISK A/S

    发明人： Honoré, Tage ,  Jacobsen, Poul ,  Nielsen, Flemming Elmelund ,  Naerum, Lars

    IPC分类号： C07D241/52 ,  A61K31/495 ,  C07D471/04 ,  C07D491/06

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

    摘要： 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.

    摘要翻译： 具有下式的杂环二羟基喹喔啉化合物：其中R 1是羟基，烷氧基，芳氧基，芳烷氧基，环烷基烷氧基，环烷氧基或酰氧基; R 5和R 6一起形成另一个被氢，卤素或CN取代的稠合环，R 6和R 7独立地为氢，NO 2，卤素，CN，SO 2 NR'R'，SO 2 R'，CF 3或OR'，其中R '是氢或C 1-4烷基; 或R 9和R 9一起形成另一个被氢，卤素或CN取代的稠环，R 5和R 6独立地为氢，NO 2，卤素，CN，SO 2 NR'R'，SO 2 R'，CF 3或OR'，其中 R'是氢或C 1-4 - 烷基。 本发明还涉及制备该化合物的方法，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，特别是奎曲拉特受体活动过度引起的适应症，特别是作为神经安定药。

    5,6,6a,7-Tetrahydro-4H-dibenz(de,g)isoquinoline derivatives, process for their preparation and pharmaceutical compositions containing them
    36.
    发明公开
    5,6,6a,7-Tetrahydro-4H-dibenz(de,g)isoquinoline derivatives, process for their preparation and pharmaceutical compositions containing them 失效
    5,6,6a -7-四氢-4H-二苯并（DE，克）异喹啉衍生物，它们的制备方法和含有它们的药物制剂。

    公开(公告)号：EP0042659A1

    公开(公告)日：1981-12-30

    申请号：EP81301271.3

    申请日：1981-03-25

    申请人： GÖDECKE AKTIENGESELLSCHAFT

    发明人： Hartenstein, Johannes ,  Fritschi, Edgar ,  Satzinger, Gerhard

    IPC分类号： C07D221/18 ,  A61K31/47

    CPC分类号： C07D491/06 ,  C07D221/18

    摘要： The present invention provides compounds of the general formula:-
    wherein R,, R 2 , R 3 , R 4 and R 5 may be the same or different and are hydroxy, straight or branched-chain alkoxy of from 1 to 5 carbon atoms, phenoxy, benzyloxy, two adjacent groups may be methylenedioxy, or hydrogen provided R 4 and R 5 are not simultaneously hydrogen; R 6 is hydrogen, straight or branched-chain alkyl of from 1 to 5 carbon atoms, straight or branched-chain alkenyl of from 2 to 5 carbon atoms, cycloalkylalkyl of from 4 to 7 carbon atoms, alkoxy carbonyl of from 2 to 6 carbon atoms, trifluoroacetyl, aralkyl of from 5 to 11 carbon atoms, or acyl which is derived from an aiiphatic, araliphatic or aromatic carboxylic acid of from 1 to 11 carbon atoms; and the pharmaceutically acceptable salts thereof; excluding 5,6,6a,7-tetrahydro-1-hydroxy-2,9,10 trimethoxy-5-methyl-4H-dibenz(de,g)-isoquinoline and 5,6,6a,7-tetrahydro-1,2,9,10-tetra-methoxy-5-methyl-4H-dibenz (de,g)isoquinoline.
    The present invention also provides a process for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for treating diseases of the central nervous system.