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公开(公告)号：US20100329982A1
公开(公告)日：2010-12-30
申请号：US12822857
申请日：2010-06-24
Applicant: Andreas LENDLEIN , Christian Wischke , Axel Thomas Neffe
Inventor： Andreas LENDLEIN , Christian Wischke , Axel Thomas Neffe
IPC: A61K49/00 , A61K9/48 , A61K47/14 , A61K39/395 , A61K39/00 , C12Q1/68 , G01N33/53 , C12Q1/02 , A61K38/14 , A61K38/17 , A61K48/00 , A61K31/715 , A61K31/56 , A61K47/30 , A61K47/32
CPC classification number: A61K9/0009 , A61K9/146 , A61K9/1629 , A61K9/5021 , A61K47/46 , C12N15/88
Abstract: The invention relates to particles which exhibit a stimulable shape change and allow control of their uptake in active cells. The particles can be used as carrier systems for bioactive molecules or as diagnostic agents, and the spherical shape thereof has a size permitting uptake in a cell. Each particle assumes a temporary, non-spherical and thus non-uptakeable or only slightly uptakeable shape which can be transformed into a spherical and thus uptakeable shape by a suitable stimulus.
Abstract translation: 本发明涉及具有刺激性形状变化并允许控制其在活性细胞中的摄取的颗粒。 该颗粒可以用作生物活性分子或诊断剂的载体系统，其球形形状具有允许细胞吸收的尺寸。 每个颗粒呈现临时的，非球形的，因此不可吸收的或只有轻微可吸收的形状，其可以通过合适的刺激转化成球形并因此可吸收的形状。
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公开(公告)号：US20110021434A1
公开(公告)日：2011-01-27
申请号：US12446053
申请日：2007-10-18
Applicant: 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
Inventor： 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
CPC classification number: C07K5/0808 , C07K14/8125
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US08710178B2
公开(公告)日：2014-04-29
申请号：US12446053
申请日：2007-10-18
Applicant: 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
Inventor： 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
CPC classification number: C07K5/0808 , C07K14/8125
Abstract: 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.
Abstract translation: 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。
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