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公开(公告)号：US09090629B2
公开(公告)日：2015-07-28
申请号：US13883344
申请日：2011-11-03
IPC分类号： A61K39/00 , C07D498/16 , A61K47/48 , A61K45/06
CPC分类号： A61K47/48384 , A61K45/06 , A61K47/60 , A61K47/6803 , A61K47/6849 , C07D498/16 , C07D498/18
摘要： New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.
摘要翻译： 公开了具有连接基团的新型安息霉素衍生物。 还公开了合成这些新的安沙霉素衍生物的方法及其与细胞结合剂的连接方法。 安曲霉素衍生物 - 细胞结合剂缀合物可用作治疗剂，其特异性递送至靶细胞并且是细胞毒性的。 与先前描述的试剂相比，这些缀合物在动物肿瘤模型中显示出显着改善的治疗功效。
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公开(公告)号：US09150649B2
公开(公告)日：2015-10-06
申请号：US12574466
申请日：2009-10-06
CPC分类号： A61K47/48215 , A61K31/5386 , A61K47/54 , A61K47/60 , A61K47/6803 , A61K47/6843 , A61K47/6849 , A61K47/6851 , A61K47/6863 , A61K47/6889 , A61K47/6891 , C07D498/18 , C07K16/2803 , C07K16/30 , C07K2317/24 , Y02A50/491
摘要： Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.
摘要翻译： 用于将药物与细胞结合剂结合的接头通过并入聚乙二醇间隔物而被修饰成亲水接头。 细胞结合剂 - 药物偶联物的效力或功效令人惊奇地增加了多种癌细胞类型的几倍，包括在细胞表面上表达低数目抗原的那些或对治疗有抗性的癌细胞。 还提供了一种制备具有硫醚部分的美登木素生物碱和允许美登木素生物碱在基本上单一步骤中与细胞结合剂连接的反应性基团的方法。
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公开(公告)号：US20130323268A1
公开(公告)日：2013-12-05
申请号：US13883344
申请日：2011-11-03
IPC分类号： A61K47/48 , A61K45/06 , C07D498/16
CPC分类号： A61K47/48384 , A61K45/06 , A61K47/60 , A61K47/6803 , A61K47/6849 , C07D498/16 , C07D498/18
摘要： New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.
摘要翻译： 公开了具有连接基团的新型安息霉素衍生物。 还公开了合成这些新的安沙霉素衍生物的方法及其与细胞结合剂的连接方法。 安曲霉素衍生物 - 细胞结合剂缀合物可用作治疗剂，其特异性递送至靶细胞并且是细胞毒性的。 与先前描述的试剂相比，这些缀合物在动物肿瘤模型中显示出显着改善的治疗功效。
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公开(公告)号：US20100129314A1
公开(公告)日：2010-05-27
申请号：US12574466
申请日：2009-10-06
IPC分类号： A61K39/395 , A61K38/19 , A61K38/43 , A61K38/22 , C07K14/52 , C07K16/28 , C07K14/575 , C07K14/00 , C07D498/18 , A61P31/12 , A61P35/00 , A61P37/00 , A61P37/06 , A61P33/00 , C12N9/96
CPC分类号： A61K47/48215 , A61K31/5386 , A61K47/54 , A61K47/60 , A61K47/6803 , A61K47/6843 , A61K47/6849 , A61K47/6851 , A61K47/6863 , A61K47/6889 , A61K47/6891 , C07D498/18 , C07K16/2803 , C07K16/30 , C07K2317/24 , Y02A50/491
摘要： Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.
摘要翻译： 用于将药物与细胞结合剂结合的接头通过并入聚乙二醇间隔物而被修饰成亲水接头。 细胞结合剂 - 药物偶联物的效力或功效令人惊奇地增加了多种癌细胞类型的几倍，包括在细胞表面上表达低数目抗原的那些或对治疗有抗性的癌细胞。 还提供了一种制备具有硫醚部分的美登木素生物碱和允许美登木素生物碱在基本上单一步骤中与细胞结合剂连接的反应性基团的方法。
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