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293 条记录 (耗时 0.033 秒)

    Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2)
    8.
    发明授权
    Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) 失效
    针对雷诺地尔受体（RyR2）泄漏的抗心律失常药物和心力衰竭药物

    公开(公告)号：US07544678B2

    公开(公告)日：2009-06-09

    申请号：US11088058

    申请日：2005-03-23

    申请人： Andrew Robert Marks ,  Donald W. Landry ,  Shixian Deng ,  Zhen Zhuang Cheng

    发明人： Andrew Robert Marks ,  Donald W. Landry ,  Shixian Deng ,  Zhen Zhuang Cheng

    IPC分类号： A61P9/00 ,  A61K31/553 ,  A61K31/554 ,  A61K31/675 ,  C07F9/553 ,  C07D281/02

    CPC分类号： C07D281/10 ,  C07D267/14 ,  C07D417/06 ,  C07D417/12 ,  G01N2800/325 ,  G01N2800/326

    摘要： The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods.

    摘要翻译： 本发明提供新的1,4-苯并硫氮杂中间体及其衍生物，其合成方法及其测定方法。 本发明还提供了使用这些新化合物来限制或防止受试者中RyR2结合的FKBP12.6水平降低的方法; 以防止受试者运动性心源性猝死; 并且治疗或预防受试者的心力衰竭，心房颤动或运动引起的心律失常。 本发明还提供用于鉴定增强RyR2和FKBP12.6的结合的试剂以及通过这些方法鉴定的试剂的方法。 此外，本发明提供用于鉴定用于治疗或预防心力衰竭，心房颤动或运动诱导的心律失常以及预防运动性心源性猝死的药剂的方法。 还提供了通过这种方法鉴定的药剂。

    Phosphatase activated crosslinking conjugating and reducing agents; methods of using such agents; and reagents comprising phosphatase activated crosslinking and conjugating
    10.
    发明授权
    Phosphatase activated crosslinking conjugating and reducing agents; methods of using such agents; and reagents comprising phosphatase activated crosslinking and conjugating 失效
    磷酸酶活化交联共轭和还原剂; 使用这种药剂的方法; 和包含磷酸酶活化的交联和缀合剂的试剂

    公开(公告)号：US6160153A

    公开(公告)日：2000-12-12

    申请号：US498388

    申请日：2000-02-03

    申请人： Christopher Bieniarz ,  Douglas F. Young ,  Michael J. Cornwell ,  Zbigniew Skrzypczynski

    发明人： Christopher Bieniarz ,  Douglas F. Young ,  Michael J. Cornwell ,  Zbigniew Skrzypczynski

    IPC分类号： A61K47/48 ,  C07F9/165 ,  C07F9/553 ,  G01N33/543

    CPC分类号： G01N33/54353 ,  C07F9/1651 ,  C07F9/1652 ,  C07F9/5537 ,  Y10S530/811 ,  Y10S530/816

    摘要： The present invention provides crosslinking, conjugating and reducing agents which are functional with at least one phosphorothioate monoester group (--SPO.sub.3.sup.--2). Crosslinking and conjugation methods as well as solid phase reagents and conjugates which are useful in immunoassays are also provided.Crosslinking and conjugating agents of the invention generally comprise a compound corresponding to the formula (I), shown below, wherein n at least 1 and Q is a straight or branched monomer, polymer or oligomer having an average molecular weight between about 200 and about 1,000,000. Additionally, when n is 1, Q comprises at least 1 additional reactive functionality.Q--(S--PO.sub.3.sup.-2).sub.n (I)The reducing agents that are provided conform to a compound of the formula (Y), shown below, wherein (A) and (Z) can be independently selected from C.sub.1 -C.sub.5 alkyl and CONH(CH.sub.2).sub.p wherein p is an integer between 1 and 5. ##STR1##

    摘要翻译： 本发明提供了与至少一种硫代磷酸酯单酯基团（-SPO3-2）起作用的交联，缀合和还原剂。 还提供了可用于免疫测定的交联和缀合方法以及固相试剂和缀合物。 本发明的交联和缀合剂通常包含对应于下式（I）的化合物，其中n至少为1且Q为直链或支链单体，平均分子量为约200至约1,000,000的聚合物或低聚物 。 另外，当n为1时，Q包含至少1个额外的反应性官能团。Q-（S-PO3-2）n（I）提供的还原剂符合下面所示的式（Y）化合物，其中 （A）和（Z）可以独立地选自C 1 -C 5烷基和CONH（CH 2）p，其中p是1和5之间的整数。