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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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2.发明授权Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates and methods of making said conjugates 有权使用通过不可切割接头连接的细胞结合剂美登木素生物碱缀合物靶向特定细胞群的方法，所述缀合物和制备所述缀合物的方法公开(公告)号：US08685920B2
公开(公告)日：2014-04-01
申请号：US13178728
申请日：2011-07-08
IPC分类号： C07D498/00
CPC分类号： C07K16/3092 , A61K47/6803 , A61K47/6851 , A61K47/6855 , A61K47/6889 , A61K2039/505 , C07K16/18 , C07K16/32 , C07K2317/24 , C07K2317/92
摘要： The present invention discloses a method for targeting maytansinoids to a selected cell population, the method comprising contacting a cell population or tissue suspected of containing the selected cell population with a cell-binding agent maytansinoid conjugate, wherein one or more maytansinoids is covalently linked to the cell-binding agent via a non-cleavable linker and the cell-binding agent binds to cells of the selected cell population.
摘要翻译： 本发明公开了一种将美登木素生物素靶向选定的细胞群体的方法，所述方法包括将怀疑含有所选细胞群的细胞群体或组织与细胞粘附剂美登木素生物碱缀合物接触，其中一种或多种美登木素生物碱共价连接到 细胞结合剂通过不可切割的接头和细胞结合剂结合所选细胞群的细胞。
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公开(公告)号：US08435528B2
公开(公告)日：2013-05-07
申请号：US11778451
申请日：2007-07-16
IPC分类号： A61K39/395
CPC分类号： A61K39/39558 , A61K31/5365 , A61K47/6803 , A61K2039/505 , C07D498/16
摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-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.
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公开(公告)号：US07473796B2
公开(公告)日：2009-01-06
申请号：US11778464
申请日：2007-07-16
IPC分类号： C07C229/00 , C07C315/00 , C07D267/22
CPC分类号： A61K39/39558 , A61K31/5365 , A61K47/6803 , A61K2039/505 , C07D498/16
摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-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： 公开了在带有硫原子的α-碳原子上带有单或二烷基取代的新的含硫醇和二硫化物的美登木素生物碱。 还公开了合成这些新的美登木素生物碱的方法和将这些新的美登木素生物素连接到细胞结合剂的方法。 美登木素生物碱 - 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：US08388960B2
公开(公告)日：2013-03-05
申请号：US13229422
申请日：2011-09-09
申请人： Viktor S. Goldmakher , Robert J. Lutz , Ravi V. J. Chari , Yelena V. Kovtun , John M. Lambert , Rita Steeves , Hans K. Erickson , Wayne C. Widdison
发明人： Viktor S. Goldmakher , Robert J. Lutz , Ravi V. J. Chari , Yelena V. Kovtun , John M. Lambert , Rita Steeves , Hans K. Erickson , Wayne C. Widdison
IPC分类号： A61K39/00
CPC分类号： C07K16/3046 , A61K31/5383 , A61K31/58 , A61K47/6803 , A61K47/6849 , A61K2039/505 , C07D498/18 , C07K2317/24
摘要： Methods of killing or inhibiting tumors comprising of heterogeneous or mixed cell populations is described. The killing or inhibition of tumors is achieved by selectively targeting a unique ligand suspected of being expressed on a particular cell population to also kill a cell population lacking the unique ligand. These conjugates have therapeutic use as they are delivered to a specific cell population to kill these cells and the cytotoxic drug is released to kill non-targeted cells, thereby eliminating the tumor.
摘要翻译： 描述了杀死或抑制包含异源或混合细胞群的肿瘤的方法。 通过选择性地靶向疑似在特定细胞群体上表达的独特配体也杀死缺乏独特配体的细胞群体来实现肿瘤的杀伤或抑制。 这些缀合物具有治疗用途，因为它们被递送到特定细胞群以杀死这些细胞，并释放细胞毒性药物以杀死非靶向细胞，从而消除肿瘤。
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公开(公告)号：US07411063B2
公开(公告)日：2008-08-12
申请号：US11594156
申请日：2006-11-08
IPC分类号： C07D491/12 , C07D498/06
CPC分类号： C07D498/14 , C07D491/14
摘要： The present invention describes the preparation of maytansinol by methods that minimize processing steps, and reduce solvent volumes, making the process more efficient, and scaleable. This process comprises a step of converting bridged acetals of maytansinol to maytansinol. The simplified processing also aids in lowering the potential for human exposure to chemicals. Also provided is an isolated C3 to C9 bridged acetal of maytansinol.
摘要翻译： 本发明描述了通过使加工步骤最小化并减少溶剂体积，使该方法更有效和可扩缩的方法制备美登素的方法。 该方法包括将美登醇的桥联缩醛转化为美登素。 简化的处理也有助于降低人类接触化学品的可能性。 还提供了美登醇的分离的C3至C9桥连缩醛。
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公开(公告)号：US08841425B2
公开(公告)日：2014-09-23
申请号：US13043879
申请日：2011-03-09
IPC分类号： C07K16/00 , C07K14/00 , C07D498/16 , A61K47/48
CPC分类号： A61K39/39558 , A61K31/5365 , A61K47/6803 , A61K2039/505 , C07D498/16
摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-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： 公开了在带有硫原子的α-碳原子上具有一或二烷基取代基的新的硫醇和二硫化物的美登木素生物碱。 还公开了合成这些新的美登木素生物碱的方法和将这些新的美登木素生物素连接到细胞结合剂的方法。 美登木素生物碱 - 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：US07851432B2
公开(公告)日：2010-12-14
申请号：US11778437
申请日：2007-07-16
IPC分类号： A01N61/00
CPC分类号： A61K39/39558 , A61K31/5365 , A61K47/6803 , A61K2039/505 , C07D498/16
摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-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： 公开了在带有硫原子的α-碳原子上具有一或二烷基取代基的新的硫醇和二硫化物的美登木素生物碱。 还公开了合成这些新的美登木素生物碱的方法和将这些新的美登木素生物素连接到细胞结合剂的方法。 美登木素生物碱 - 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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9.发明授权Methods for preparation of cytotoxic conjugates of maytansinoids and cell binding agents 有权美登木素生物碱和细胞粘附剂的细胞毒性偶联物的制备方法公开(公告)号：US07368565B2
公开(公告)日：2008-05-06
申请号：US10161651
申请日：2002-06-05
IPC分类号： A61K39/00
CPC分类号： C07D498/18
摘要： The present invention discloses a one-step process for the production of cytotoxic conjugates of maytansinoids and cell binding agents. Maytansinoids having a disulfide linker that bears a reactive moiety are linked to cell binding agents, such as antibodies, without prior modification of the cell binding agent. These conjugates are useful as therapeutic agents which are delivered specifically to target cells and are cytotoxic.
摘要翻译： 本发明公开了一种用于生产美登木素生物碱和细胞结合剂的细胞毒性缀合物的一步法。 具有带有反应性部分的二硫键连接体的美登木素生物碱与细胞结合剂（例如抗体）连接，而无需先前修饰细胞结合剂。 这些缀合物可用作特异性递送至靶细胞并具有细胞毒性的治疗剂。
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公开(公告)号：US07301019B2
公开(公告)日：2007-11-27
申请号：US11334478
申请日：2006-01-19
IPC分类号： C07D491/12 , C07D498/06
CPC分类号： C07D498/18
摘要： Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process of making a maytansinoid ester comprising forming an anion of maytansinol or a maytansinoid bearing a free C-3 hydroxyl moiety and reacting the anion with an activated carboxyl compound to thereby produce the maytansinoid ester.
摘要翻译： 描述了用于制备和纯化美登木素生物碱酯，特别是硫醇和二硫化物的美登木素生物碱的改进方法。 在一个方面，该方法包括制备美登木素生物碱酯的方法，其包括形成美登醇的阴离子或含有游离C-3羟基部分的美登木素生物碱，并使阴离子与活化的羧基化合物反应，从而产生美登木酯生物酯。
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