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公开(公告)号：US09085536B2
公开(公告)日：2015-07-21
申请号：US13421809
申请日：2012-03-15
IPC分类号： A61K31/439 , C07D221/22
CPC分类号： C07D221/22 , A61K31/439 , A61K31/695
摘要： Compound derivatives of aconitine are provided, in particular derivatives that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. The subject compounds are useful in treatments, including treatments to modulate neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the aconitine derivatives.
摘要翻译： 提供乌头碱的复合衍生物，特别是调节钠通道活性的衍生物。 还提供了包含本发明化合物和药学上可接受的载体的药物组合物。 主题化合物可用于治疗，包括调节神经元活动或引起肌肉松弛的治疗。 该化合物还可用于治疗患有电压门控钠通道增强性疾病或疼痛的受试者。 提供了用于制备乌头碱衍生物的其它方法。
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公开(公告)号：US08476451B2
公开(公告)日：2013-07-02
申请号：US12669364
申请日：2008-07-21
IPC分类号： A61K31/426 , A61K31/427 , C07D277/30 , A01N43/78
CPC分类号： A61K38/07 , C07D277/28 , C07D277/30 , C07D277/56 , C07D417/12
摘要： The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The compounds of the invention are highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
摘要翻译： 本发明提供新型的微管蛋白酶类似物，制备方法以及使用其类似物和缀合物的方法。 本发明的化合物是高度有效的细胞生长抑制剂，其已被开发出比管状蛋白D更小和更稳定。
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公开(公告)号：US20110263650A1
公开(公告)日：2011-10-27
申请号：US12669672
申请日：2008-07-21
IPC分类号： A61K31/454 , A61P17/06 , A61K31/426 , A61P35/00 , C07D401/12 , C07D277/587
CPC分类号： C07D277/56 , C07D417/12 , C07K5/06078
摘要： The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The essential features for the potent cytotoxicity of tubulysin D have been established for the first time by the synthesis and evaluation of a series of analogues. By identifying functionality that surprisingly is not necessary for activity, highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
摘要翻译： 本发明提供新型的微管蛋白酶类似物，制备方法以及使用其类似物和缀合物的方法。 通过合成和评估一系列类似物，首次建立了管状细胞毒素D的有效细胞毒性的基本特征。 通过鉴定出令人惊讶地不是活性必需的功能，已经开发出高效的细胞生长抑制剂，它们比小管状蛋白酶D更小和更稳定。
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公开(公告)号：US20110021568A1
公开(公告)日：2011-01-27
申请号：US12669364
申请日：2008-07-21
IPC分类号： A61K31/426 , C07D401/12 , A61K31/454 , A61P35/00
CPC分类号： A61K38/07 , C07D277/28 , C07D277/30 , C07D277/56 , C07D417/12
摘要： The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The compounds of the invention are highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.
摘要翻译： 本发明提供新型的微管蛋白酶类似物，制备方法以及使用其类似物和缀合物的方法。 本发明的化合物是高度有效的细胞生长抑制剂，其已被开发出比管状蛋白D更小和更稳定。
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5.发明授权Sleeves for use in systems for supporting platform-like objects on casters and posts 失效用于在脚轮和支柱上支撑平台状物体的系统中使用的套筒公开(公告)号：US06932314B2
公开(公告)日：2005-08-23
申请号：US10758690
申请日：2004-01-15
CPC分类号： B60B33/0005 , B60B33/0002 , B60B33/0007 , B60B33/0021 , B60B33/0039 , B60B33/0049 , F16M11/42 , F16M2200/08 , Y10T16/204
摘要： Sleeves for use in systems for supporting platform-like objects on casters and posts and described. The sleeves support caster-and-post junctions and inhibit deformation of the stems of the casters and the ends of posts in directions radially outward from the longitudinal axes of the stems and posts.
摘要翻译： 用于在脚轮和支柱上支撑平台状物体的系统中使用的套筒，并描述。 袖子支撑脚轮和后接头，并且阻止脚轮的杆部和杆的端部沿从杆和柱的纵向轴线径向向外的方向的变形。
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