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    Ethanesulfonyl-piperidine derivatives
    1.
    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。

    Heterocyclic compounds useful as NMDA receptor selective subtype blockers
    9.
    发明授权
    Heterocyclic compounds useful as NMDA receptor selective subtype blockers 失效
    可用作NMDA受体选择亚型阻断剂的杂环化合物

    公开(公告)号：US06451819B2

    公开(公告)日：2002-09-17

    申请号：US09833450

    申请日：2001-04-12

    申请人： Alexander Alanine ,  Bernd Buettelmann ,  Marie-Paule Heitz Neidhart ,  Georg Jaeschke ,  Emmanuel Pinard ,  Rene Wyler

    发明人： Alexander Alanine ,  Bernd Buettelmann ,  Marie-Paule Heitz Neidhart ,  Georg Jaeschke ,  Emmanuel Pinard ,  Rene Wyler

    IPC分类号： A61K31435

    CPC分类号： C07D263/58 ,  C07D205/04 ,  C07D207/12 ,  C07D209/34 ,  C07D211/54 ,  C07D231/56

    摘要： The invention relates to treating neurodegeneration by selective blocking of NMDA receptor with compounds of formula wherein Ar1 is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z1 is a five membered heterocyclic ring, which contains one or two heteroatoms, selected from N or O; R1 is hydrogen, hydroxy or an oxo group; Ar2 is pyridyl or phenyl, optionally substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z2 is a five or six membered ring, which optionally contains one or two heteroatoms, selected from N or O; and Q, X, A, Y B are as defined in the specification.

    摘要翻译： 本发明涉及通过选择性阻断NMDA受体来治疗神经变性，其中化合物是由羟基，低级烷基，卤素，氨基，硝基，苄氧基或低级烷氧基 - 低级烷氧基取代的吡啶基或苯基，或其中Z 1为五 含有一个或两个选自N或O的杂原子; R 1是氢，羟基或氧代基; Ar 2是吡啶基或苯基，任选地被羟基，低级烷基，卤素，氨基，硝基，苄氧基或低级 烷氧基 - 低级烷氧基，或者是其中Z 2是五或六元环的基团，其任选地含有一个或两个选自N或O的杂原子; 且Q，X，A，Y B如说明书中所定义。