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    FUSED TETRACYCLIC MGLUR1 ANTAGONISTS AS THERAPEUTIC AGENTS
    32.
    发明申请
    FUSED TETRACYCLIC MGLUR1 ANTAGONISTS AS THERAPEUTIC AGENTS 失效

    公开(公告)号：US20080312218A1

    公开(公告)日：2008-12-18

    申请号：US11524867

    申请日：2006-09-21

    申请人： Duane A. Burnett ,  Wen-Lian Wu

    发明人： Duane A. Burnett ,  Wen-Lian Wu

    IPC分类号： A61K31/549 ,  A61K31/538 ,  A61K31/519 ,  A61K31/504 ,  C07D498/02 ,  C07D491/02

    CPC分类号： C07D495/14

    摘要： In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.

    摘要翻译： 在其许多实施方案中，本发明提供了可用作代谢型谷氨酸受体（mGluR）拮抗剂的式I或式II（其中各种部分如本文所定义）的四环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂，含有 化合物和使用化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
    37.
    发明授权
    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
    用作降胆固醇药的羟基取代的氮杂环丁酮化合物

    公开(公告)号：US5631365A

    公开(公告)日：1997-05-20

    申请号：US257593

    申请日：1994-06-09

    申请人： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    发明人： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    IPC分类号： A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61P3/06 ,  A61P7/00 ,  A61P9/10 ,  C07D205/08

    CPC分类号： C07D205/08 ,  Y02P20/55

    摘要： A process for preparing compounds of the formula ##STR1## wherein R and R.sup.2 are independently --OH, --O(lower alkyl) or --0-benzyl and the remaining variables are as defined in the specification, comprising(a) treating with a strong base in an anhydrous organic solvent a lactone of the formula ##STR2## respectively, wherein Ar.sup.10 is Ar.sup.1 or a suitably protected hydroxy- or amino-substituted aryl, and R' and R.sup.2' are R and R.sup.2 as defined above or are suitably protected hydroxy groups;(b) reacting a product of step (a) with an imine of the formula ##STR3## wherein Ar.sup.20 and Ar.sup.30 are Ar.sup.2 or Ar.sup.3 or suitably protected hydroxy- or amino-substituted aryl;c) quenching the reaction with an acid; andd) removing protecting groups as necssary.

    摘要翻译： 制备式IMA化合物的方法其中R和R 2独立地是-OH，-O（低级烷基）或-O-苄基，其余的变量如说明书中所定义，包括（a） 在无水有机溶剂中具有分子式为“IMAGE”的内酯的强碱，其中Ar10为Ar1或适当保护的羟基或氨基取代的芳基，R'和R2'为如上所定义的R和R 2，或者为 适当保护的羟基; （b）使步骤（a）的产物与下式的亚胺反应：其中Ar 20和Ar 30是Ar 2或Ar 3或适当保护的羟基或氨基取代的芳基; c）用酸淬灭反应; 和d）去除保护基团。