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参考文献:新型同手性美西律类似物的合成及其体外钠通道阻断活性评价
标题:新型同手性美西律类似物的合成及其体外钠通道阻断活性评价
摘要:以光学活性形式合成了新的手性美西律类似物,并在体外评估为使用依赖性的骨骼肌钠通道阻滞剂.对食用蛙(rana Esculenta)的单条肌纤维的钠电流进行的测试表明,与美西律相比,它们均发挥了更高的使用依赖性阻滞作用.最有效的类似物(S)-3-(2,6-二甲基苯氧基)-1-苯基丙-1-胺(S)-(5)在产生补品方面的效力比(R)-Mex高六倍堵塞.如用美西律观测到的那样,新合成的化合物表现出适度的对映选择性,这在3-(2,6-二甲基苯氧基)丁丹-1-胺中更为明显(3).<手性>,2010年.©2009 Wiley-Liss,Inc..
Doi:10.1002/chir.20741
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专利信息
专利号:US-8129411-B2
优先权日:2005-12-30
标题:Organic compounds
发明人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI
权利人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI; NOVARTIS AG
摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. n The compounds have the formula I′ n nwherein R1, R2, T, R3 and R4 are as defined in the specification.
专利号:CN-102126987-A
优先权日:2010-12-30
标 题:A kind of chiral allyl amine compound, synthesis method and use thereof