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    • 10. 发明授权
    • Substituted pyrazolo[1,5-a]pyrimidines as potassium channel activators
    • 取代的吡唑并[1,5-a]嘧啶作为钾通道激活剂
    • US07507730B2
    • 2009-03-24
    • US11511154
    • 2006-08-28
    • Wei HanZilun Hu
    • Wei HanZilun Hu
    • C07D487/04C07D291/06A61K31/519A61K31/541C07D413/12A61K31/5355A61P25/06A61P9/06A61P25/08A61P1/04A61P11/08
    • C07D487/04
    • Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier, which have the structure stereoisomers including enantiomers thereof and diastereomers thereof, or a pharmaceutically acceptable salt thereof, wherein Q is alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl or which is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R3 is wherein R1, R2, R4, R5, R6, R7, R8, R9 and R10 are defined herein. Methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds are also provided.
    • 可用作钾通道功能抑制剂的新型杂环二氢嘧啶化合物(特别是电压门控K +通道的Kv1亚家族的抑制剂,特别是与超快速活化延迟整流剂连接的抑制剂Kv1.5,其具有包括其对映异构体的结构立体异构体 其中Q是烷基,取代的烷基,环烷基,取代的环烷基,环杂烷基,取代的环杂烷基或芳基,取代的芳基,杂芳基或取代的杂芳基; R3是其中R1,R2,R4, R5,R6,R7,R8,R9和R10如本文所定义。还提供了使用这些化合物预防和治疗心律失常和IKur相关病症的方法,以及含有这些化合物的药物组合物。