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75 条记录 (耗时 0.049 秒)

    Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
    51.
    发明授权
    Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 失效

    公开(公告)号：US5624920A

    公开(公告)日：1997-04-29

    申请号：US342197

    申请日：1994-11-18

    申请人： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

    发明人： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

    IPC分类号： C07D205/08 ,  C07D401/12 ,  C07D409/12 ,  A61K31/395

    CPC分类号： C07D401/12 ,  C07D205/08 ,  C07D409/12

    摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is aryl or R.sup.10 -substituted aryl;Ar.sup.2 is aryl or R.sup.4 -substituted aryl;Ar.sup.3 is aryl or R.sup.5 -substituted aryl;X and Y are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;R is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 is hydrogen, lower alkyl or aryl; or R and R.sup.1 together are .dbd.O;q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5;R.sup.4 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sup.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)--COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2, halogen, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl;R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; andR.sup.10 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2 and halogen;are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

    Fused tetracyclic mGluR1 antagonists as therapeutic agents
    57.
    发明授权
    Fused tetracyclic mGluR1 antagonists as therapeutic agents 失效
    融合的四环mGluR1拮抗剂作为治疗剂

    公开(公告)号：US07482360B2

    公开(公告)日：2009-01-27

    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： A01N43/42 ,  A61K31/44 ,  C07D487/00 ,  C07D471/00 ,  C07D239/00 ,  C07D491/00

    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。

    Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
    58.
    发明申请
    Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof 有权
    取代的氮杂环丁酮化合物，其制备方法，制剂及其用途

    公开(公告)号：US20080200446A1

    公开(公告)日：2008-08-21

    申请号：US12108729

    申请日：2008-04-24

    申请人： Duane A. Burnett ,  John W. Clader

    发明人： Duane A. Burnett ,  John W. Clader

    IPC分类号： A61K31/397 ,  C07D205/08 ,  A61P9/10

    CPC分类号： C07D405/12 ,  C07D405/14 ,  Y10S930/28

    摘要： The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.

    摘要翻译： 本发明提供由结构式（I）表示的化合物或式（I）化合物的药学上可接受的异构体，盐，溶剂合物或酯，其中每个取代基如本文所述，包括上述化合物的制剂，方法 用于制备它们以及用于治疗动脉粥样硬化，高胆固醇血症或静脉麻醉的方法，以及用于降低甾醇和/或甾醇的血浆水平。