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    Tricyclic pyridone derivatives
    2.
    发明授权
    Tricyclic pyridone derivatives 失效
    三环吡啶酮衍生物

    公开(公告)号：US5258387A

    公开(公告)日：1993-11-02

    申请号：US889029

    申请日：1992-05-26

    申请人： Serge Burner ,  Ulrich Widmer

    发明人： Serge Burner ,  Ulrich Widmer

    IPC分类号： C07D213/80 ,  C07D213/82 ,  C07D401/12 ,  C07D471/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  A61K31/38

    CPC分类号： C07D213/80 ,  C07D213/82 ,  C07D401/12 ,  C07D471/04 ,  C07D495/14

    摘要： The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-piperazinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by a taken together is a group of the formula >C.sub..alpha. --S--CH.dbd.CH-- or >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine,can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.

    摘要翻译： 式（I）所示的吡啶酮衍生物，其中R a是氢或卤素，R b是-OR 1或-NR 2 R 3; R 1是未取代的低级烷基或被羟基，低级烷氧基，氨基，低级烷基氨基，二（低级烷基）氨基，二（低级烷基）氨基甲酰基或低级烷氧基羰基氨基取代的低级烷基; R 2是氢或未被取代或被羟基，低级烷氧基，氨基，低级烷基氨基，二（低级烷基） - 氨基，二（低级烷基）氨基甲酰基或低级烷氧基羰基 - 氨基取代的低级烷基; 并且R 3是氢或低级烷基或R 2和R 3与它们所连接的氮原子一起是1-取代的1-氮杂环丁烷基，1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基或1-哌嗪基， 或被低级烷基，羟基，低级烷氧基，低级羟烷基，低级烷氧基烷基或苯基单取代或二取代; B和由一起代表的碳原子是式> C a -S-CH = CH-或> C a -CR 4 = CH-CH = CH-并且R 4是氢，氟或氯的基团可以是 用于控制或预防疾病。 特别是，它们具有肌肉松弛剂，镇静催眠剂，抗焦虑药和/或抗惊厥活性，因此可用于控制或预防肌肉紧张，压力状况，失眠，焦虑状态和/或惊厥。

    Ethanesulfonyl-piperidine derivatives
    3.
    发明授权
    Ethanesulfonyl-piperidine derivatives 有权
    乙磺酰基 - 哌啶衍生物

    公开(公告)号：US06310213B1

    公开(公告)日：2001-10-30

    申请号：US09585755

    申请日：2000-06-02

    申请人： Alexander Alanine ,  Serge Burner ,  Bernd Büttelmann ,  Marie-Paule Heitz Neidhart ,  Georg Jaeschke ,  Emmanuel Pinard ,  René Wyler

    发明人： Alexander Alanine ,  Serge Burner ,  Bernd Büttelmann ,  Marie-Paule Heitz Neidhart ,  Georg Jaeschke ,  Emmanuel Pinard ,  René Wyler

    IPC分类号： C07D21120

    CPC分类号： C07D211/46 ,  C07D211/14

    摘要： The invention relates to compounds of the general formula wherein R1 signifies hydrogen or hydroxy; R2 signifies hydrogen or methyl; and X signifies —O— or —CH2— and their pharmaceutically acceptable acid addition salts. It has been shown that these compounds have a good affitity to the NMDA receptor and they are therefore useful in the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused, e.g., by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.

    摘要翻译： 本发明涉及一般化学式R 1表示氢或羟基的化合物; R2表示氢或甲基; 并且X表示-O-或-CH 2 - 及其药学上可接受的酸加成盐。已经显示这些化合物对NMDA受体具有良好的依赖性，因此它们可用于治疗疾病，其中治疗适应症包括急性 形成神经退行性疾病，例如中风或脑外伤; 慢性形式的神经变性如阿尔茨海默病，帕金森病，亨廷顿病或ALS（肌萎缩性侧索硬化）; 与细菌或病毒感染相关的神经变性，以及精神分裂症，焦虑症，抑郁症和慢性/急性疼痛等疾病。

    Tricyclic pyridone derivatives
    4.
    发明授权
    Tricyclic pyridone derivatives 失效
    三聚吡啶衍生物

    公开(公告)号：US5143912A

    公开(公告)日：1992-09-01

    申请号：US739757

    申请日：1991-08-02

    申请人： Serge Burner ,  Ulrich Widmer

    发明人： Serge Burner ,  Ulrich Widmer

    IPC分类号： A61K31/435 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D213/80 ,  C07D213/82 ,  C07D401/12 ,  C07D471/04 ,  C07D495/14 ,  C07D498/04

    CPC分类号： C07D213/80 ,  C07D213/82 ,  C07D401/12 ,  C07D471/04 ,  C07D495/14

    摘要： The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.

    摘要翻译： 其中R a为氢或卤素，R 2为-NR 2 R 3的新颖的吡啶酮衍生物，其中R 2和R 3与它们所连接的氮原子一起为1-氮杂环丁烷基，1-吡咯烷基，1-哌啶基 低级烷基，羟基，低级烷氧基，低级羟烷基，低级烷氧基烷基或苯基单取代或二取代; B和由α表示的碳原子一起是式> Cα-CR 4 = CH-CH = CH-并且R 4是氢，氟或氯的基团可用于控制或预防疾病。 特别是，它们具有肌肉松弛剂，镇静催眠剂，抗焦虑药和/或抗惊厥活性，因此可用于控制或预防肌肉紧张，压力状况，失眠，焦虑状态和/或惊厥。

    Tricyclic pyridone derivatives
    6.
    发明授权
    Tricyclic pyridone derivatives 失效
    三环吡啶酮衍生物

    公开(公告)号：US5362738A

    公开(公告)日：1994-11-08

    申请号：US70124

    申请日：1993-06-01

    申请人： Serge Burner ,  Ulrich Widmer

    发明人： Serge Burner ,  Ulrich Widmer

    IPC分类号： A61K31/435 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D213/80 ,  C07D213/82 ,  C07D401/12 ,  C07D471/04 ,  C07D495/14 ,  C07D498/04 ,  A61K31/44 ,  C07D221/06

    CPC分类号： C07D213/80 ,  C07D213/82 ,  C07D401/12 ,  C07D471/04 ,  C07D495/14

    摘要： The pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl optionally unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, that can be used for the control or treatment of muscle tension, stress, insomnia, anxiety and/or convulsions.

    摘要翻译： 式I的吡啶酮衍生物其中R a是氢或卤素，R b是-OR 1或-NR 2 R 3; R 1是未取代的低级烷基或被羟基，低级烷氧基，氨基，低级烷基氨基，二（低级烷基）氨基，二（低级烷基）氨基甲酰基或低级烷氧基羰基氨基取代的低级烷基; R 2是氢或未被取代或被羟基，低级烷氧基，氨基，低级烷基氨基，二（低级烷基） - 氨基，二（低级烷基）氨基甲酰基或低级烷氧基羰基 - 氨基取代的低级烷基; 羟基，低级烷氧基，低级羟基烷基，低级烷氧基烷基或苯基单或二取代; B和由α表示的碳原子一起是式可以用于控制或治疗肌肉紧张的式> Cα-CR 4 = CH-CH = CH-和R 4是氢，氟或氯， 压力，失眠，焦虑和/或抽搐。