Novel anti-arrythmic and heart failure drugs that target the...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 281/02 (2006.01)

Patent

CA 2601541

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.

Cette invention apporte de nouveaux intermédiaires et dérivés de la 1,4-benzothiazépine, et des procédés pour leur synthétisation et leur dosage. Elle fournit également des procédés d~utilisation de ces nouveaux composés pour limiter ou prévenir une diminution du taux du complexe FKBP12.6-RyR2 chez un sujet ; afin de prévenir une mort cardiaque subite lors d~un exercice physique ; de traiter ou prévenir une défaillance cardiaque, une fibrillation auriculaire ou une arythmie cardiaque produite par un exercice. La présente invention apporte en outre des procédés de détection de l~agent qui accentue la liaison du RyR2 et du FKBP12.6, et les agents détectés par ces procédés. De plus, cette invention apporte un procédé de détection des agents pour le traitement et la prévention des défaillances cardiaques, la fibrillation auriculaire ou l~arythmie produite par un exercice, et la prévention d~une mort cardiaque subitelors d~un exercice. Elle fournit également les agents identifiés par de tels procédés.

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