NOVEL ANTI-ARRHYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RyR2)
    4.
    发明申请
    NOVEL ANTI-ARRHYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RyR2) 审中-公开
    靶向RYANODE受体(RyR2)的新型抗神经和心脏衰竭药物

    公开(公告)号:US20100152440A1

    公开(公告)日:2010-06-17

    申请号:US12480396

    申请日:2009-06-08

    IPC分类号: C07D417/06 C07D281/08

    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。

    Novel anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2)
    6.
    发明申请
    Novel anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) 失效
    针对雷诺定受体(RyR2)漏出的新型抗心律失常药物和心力衰竭药物

    公开(公告)号:US20050187386A1

    公开(公告)日:2005-08-25

    申请号:US11088058

    申请日:2005-03-23

    IPC分类号: C07D267/02

    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。