公开(公告)号：US20110021434A1

公开(公告)日：2011-01-27

申请号：US12446053

申请日：2007-10-18

申请人： Andrew David Abell ,  James Morriss Coxon ,  Matthew Alan Jones ,  Stephen Brian McNabb ,  Axel Thomas Neffe ,  Steven Geoffrey Aitken ,  Blair Gibb Stuart ,  Janna Marie Nikkel ,  Joanna Kimberley Duncan ,  Mutita Klanchantra ,  James David Morton ,  Roy Bickerstaffe ,  Lucinda Jane Goodricke Robertson ,  Hannah Yun Young Lee ,  Matthew Stewart Muir

发明人： Andrew David Abell ,  James Morriss Coxon ,  Matthew Alan Jones ,  Stephen Brian McNabb ,  Axel Thomas Neffe ,  Steven Geoffrey Aitken ,  Blair Gibb Stuart ,  Janna Marie Nikkel ,  Joanna Kimberley Duncan ,  Mutita Klanchantra ,  James David Morton ,  Roy Bickerstaffe ,  Lucinda Jane Goodricke Robertson ,  Hannah Yun Young Lee ,  Matthew Stewart Muir

IPC分类号： A61K38/06 ,  C07K5/08 ,  A61P9/00 ,  A61P25/02 ,  A61P35/00 ,  A61P31/12

CPC分类号： C07K5/0808 ,  C07K14/8125

摘要： The present invention provides a novel class of macrocyclic compounds, which are useful as cysteine protease inhibitors. Also provided are novel intermediates and methods of preparing the compounds. The invention also provides pharmaceutical compositions comprising the compounds. The compounds and compositions are useful in methods of treating or preventing one or more diseases associated with cysteine protease activity, particularly those associated with calpain activity.

摘要翻译： 本发明提供了一类新的大环化合物，其可用作半胱氨酸蛋白酶抑制剂。 还提供了新的中间体和制备化合物的方法。 本发明还提供包含该化合物的药物组合物。 化合物和组合物可用于治疗或预防与半胱氨酸蛋白酶活性相关的一种或多种疾病，特别是与钙蛋白酶活性相关的疾病的方法。

公开(公告)号：US08710178B2

公开(公告)日：2014-04-29

申请号：US12446053

申请日：2007-10-18

申请人： Andrew David Abell ,  James Morriss Coxon ,  Matthew Alan Jones ,  Stephen Brian McNabb ,  Axel Thomas Neffe ,  Steven Geoffrey Aitken ,  Blair Gibb Stuart ,  Janna Marie Nikkel ,  Joanna Kimberley Duncan ,  Mutita Klanchantra ,  James David Morton ,  Roy Bickerstaffe ,  Lucinda Jane Goodricke Robertson ,  Hannah Yun Young Lee ,  Matthew Stewart Muir

发明人： Andrew David Abell ,  James Morriss Coxon ,  Matthew Alan Jones ,  Stephen Brian McNabb ,  Axel Thomas Neffe ,  Steven Geoffrey Aitken ,  Blair Gibb Stuart ,  Janna Marie Nikkel ,  Joanna Kimberley Duncan ,  Mutita Klanchantra ,  James David Morton ,  Roy Bickerstaffe ,  Lucinda Jane Goodricke Robertson ,  Hannah Yun Young Lee ,  Matthew Stewart Muir

IPC分类号： A61K38/06 ,  A61P9/00 ,  A61P25/02 ,  C07K5/08

CPC分类号： C07K5/0808 ,  C07K14/8125

摘要： The present invention provides a novel class of macrocyclic compounds, which are useful as cysteine protease inhibitors. Also provided are novel intermediates and methods of preparing the compounds. The invention also provides pharmaceutical compositions comprising the compounds. The compounds and compositions are useful in methods of treating or preventing one or more diseases associated with cysteine protease activity, particularly those associated with calpain activity.

摘要翻译： 本发明提供了一类新的大环化合物，其可用作半胱氨酸蛋白酶抑制剂。 还提供了新的中间体和制备化合物的方法。 本发明还提供包含该化合物的药物组合物。 化合物和组合物可用于治疗或预防与半胱氨酸蛋白酶活性相关的一种或多种疾病，特别是与钙蛋白酶活性相关的疾病的方法。