公开(公告)号：US20070254849A1

公开(公告)日：2007-11-01

申请号：US11728834

申请日：2007-03-26

Applicant: S.R. Chen ,  Thomas Back ,  Dawei Jiang ,  Kannan Vembaiyan

Inventor： S.R. Chen ,  Thomas Back ,  Dawei Jiang ,  Kannan Vembaiyan

IPC: C07D209/82 ,  A61K31/403 ,  A61K31/422 ,  A61K31/5377 ,  C07H15/20 ,  C07H3/08 ,  C07D413/12 ,  A61K31/7056 ,  A61P9/00

CPC classification number: C07D209/88 ,  C07D209/82 ,  C07D413/12

Abstract: The present invention provides novel ryanodine receptor type 2 (RyR2) inhibitors and methods of their use in the treatment of cardiac conditions. In general, the RyR2 inhibitors of the present invention assist in the normalization of intracellular calcium homeostasis. In certain embodiments, the RyR2 inhibitors are store-overload-induced Ca2+ release (SOICR) inhibitors that minimally inhibit or do not inhibit Ca2+-induced Ca2+ release (CICR), thereby providing beneficial effects in cardiac therapy.

Abstract translation: 本发明提供了新的兰诺定受体2型（RyR2）抑制剂及其用于治疗心脏病症的方法。 通常，本发明的RyR2抑制剂有助于细胞内钙稳态的归一化。 在某些实施方案中，RyR2抑制剂是储存过量诱导的Ca 2+释放（SOICR）抑制剂，其最低限度地抑制或不抑制Ca 2+诱导的Ca ^{2 + 释放（CICR），从而在心脏治疗中提供有益效果。}