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公开(公告)号：US08236319B2
公开(公告)日：2012-08-07
申请号：US12433604
申请日：2009-04-30
申请人： Ravi V. J. Chari , Robert Yongxin Zhao , Yelena Kovtun , Rajeeva Singh , Wayne Charles Widdison
发明人： Ravi V. J. Chari , Robert Yongxin Zhao , Yelena Kovtun , Rajeeva Singh , Wayne Charles Widdison
CPC分类号： C07K16/28 , A61K31/5365 , A61K47/65 , A61K47/6809 , A61K47/6849 , C07D207/46 , C07K5/0202 , C07K5/06026 , C07K5/0806 , C07K5/0819 , Y02A50/423 , Y02A50/491
摘要： Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.
摘要翻译： 带电或带电荷的交联部分和细胞结合剂的缀合物和包含带电荷或带正电荷的交联部分的药物及其制备方法。
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公开(公告)号：US08613930B2
公开(公告)日：2013-12-24
申请号：US13542126
申请日：2012-07-05
申请人： Ravi V. J. Chari , Robert Yongxin Zhao , Yelena Kovtun , Rajeeva Singh , Wayne Charles Widdison
发明人： Ravi V. J. Chari , Robert Yongxin Zhao , Yelena Kovtun , Rajeeva Singh , Wayne Charles Widdison
CPC分类号： C07K16/28 , A61K31/5365 , A61K47/65 , A61K47/6809 , A61K47/6849 , C07D207/46 , C07K5/0202 , C07K5/06026 , C07K5/0806 , C07K5/0819 , Y02A50/423 , Y02A50/491
摘要： Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.
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3.发明授权Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same 有权携带反应性聚乙二醇部分的细胞毒性试剂，包含聚乙二醇连接基团的细胞毒性偶联物及其制备和使用方法公开(公告)号：US06716821B2
公开(公告)日：2004-04-06
申请号：US10024290
申请日：2001-12-21
IPC分类号： A61K3170
CPC分类号： A61K47/60
摘要： Cytotoxic agents bearing a polyethylene glycol (PEG) linking group having a terminal active ester, cytotoxic conjugates comprising one or more cytotoxic agents linked to a cell-binding agent via PEG linking groups, and methods for producing both are disclosed. A therapeutic composition comprising a therapeutically-effective amount of one of the cytotoxic conjugates of the present invention, and a method of killing selected cell populations comprising contacting target cells, or tissue containing target cells, with an effective amount of one of the cytotoxic conjugates, are also disclosed.
摘要翻译： 公开了具有末端活性酯的聚乙二醇（PEG）连接基团的细胞毒性剂，包含通过PEG连接基团与细胞结合剂连接的一种或多种细胞毒性剂的细胞毒性缀合物，以及用于生产两者的方法。 一种治疗组合物，其包含治疗有效量的本发明的细胞毒性偶联物之一，以及杀死所选细胞群的方法，包括将靶细胞或含有组织的靶细胞与有效量的一种细胞毒性缀合物， 也被披露。
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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：US07906545B2
公开(公告)日：2011-03-15
申请号：US12505175
申请日：2009-07-17
IPC分类号： A61K31/40 , C07D209/56
CPC分类号： C07D307/85 , A61K31/407 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/675 , A61K47/545 , A61K47/548 , A61K47/60 , C07D209/42 , C07D209/60 , C07D403/14 , C07D405/12 , C07F9/5728 , C07F9/65583 , Y02A50/423 , Y02A50/491 , Y02P20/55
摘要： Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
摘要翻译： 具有可切割保护基的抗肿瘤抗生素CC-1065类似物的前药，例如哌嗪基氨基甲酸酯，4-哌啶子基 - 哌啶子基氨基甲酸酯或磷酸酯，其中保护基团赋予增强的水溶性和在前药上的稳定性， 其中前药还具有可与细胞结合试剂例如抗体缀合的部分，例如二硫化物。 还描述了这种前药缀合物的治疗用途; 这种细胞毒性药物的前药具有治疗用途，因为它们可以将细胞毒性前体药物递送至特定细胞群体，以靶向方式酶促转化为细胞毒性药物。
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公开(公告)号：US07655661B2
公开(公告)日：2010-02-02
申请号：US12144612
申请日：2008-06-23
IPC分类号： A61K31/497 , C07D209/56
CPC分类号： C07D307/85 , A61K31/407 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/675 , A61K47/545 , A61K47/548 , A61K47/60 , C07D209/42 , C07D209/60 , C07D403/14 , C07D405/12 , C07F9/5728 , C07F9/65583 , Y02A50/423 , Y02A50/491 , Y02P20/55
摘要： Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.
摘要翻译： 具有可切割保护基的抗肿瘤抗生素CC-1065类似物的前药，例如哌嗪基氨基甲酸酯，4-哌啶子基 - 哌啶子基氨基甲酸酯或磷酸酯，其中保护基团赋予增强的水溶性和在前药上的稳定性， 其中前药还具有可与细胞结合试剂例如抗体缀合的部分，例如二硫化物。 还描述了这种前药缀合物的治疗用途; 这种细胞毒性药物的前药具有治疗用途，因为它们可以将细胞毒性前药递送至特定的细胞群，以靶向方式酶促转化成细胞毒性药物。
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公开(公告)号：US07329760B2
公开(公告)日：2008-02-12
申请号：US10265452
申请日：2002-10-07
IPC分类号： C07D209/56 , C07D487/02
CPC分类号： C07D209/60 , Y02P20/55
摘要： Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.
摘要翻译： （ - ）CBI（5-羟基-3-氨基-1- [S] - （氯甲基）-1,2-二氢-3H-苯并（e）吲哚）的改进的合成： 的CC-1065类似物，其包含环丙烷苯偶姻（CBI）烷基化部分，并且它们共同为DC1及其衍生物，用于合成细胞靶向治疗剂。
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公开(公告)号：US07049316B2
公开(公告)日：2006-05-23
申请号：US10692856
申请日：2003-10-27
IPC分类号： A61K31/497 , C07D241/04 , A61P35/00
CPC分类号： C07D307/85 , A61K31/407 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/675 , A61K47/545 , A61K47/548 , A61K47/60 , C07D209/42 , C07D209/60 , C07D403/14 , C07D405/12 , C07F9/5728 , C07F9/65583 , Y02A50/423 , Y02A50/491 , Y02P20/55
摘要： Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
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公开(公告)号：US06586618B1
公开(公告)日：2003-07-01
申请号：US10265329
申请日：2002-10-07
IPC分类号： C07C6976
CPC分类号： C07D209/60 , Y02P20/55
摘要： Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.
摘要翻译： （ - ）CBI（5-羟基-3-氨基-1- [S] - （氯甲基）-1,2-二氢-3H-苯并（e）吲哚）的改进的合成： 的CC-1065类似物，其包含环丙烷苯偶姻（CBI）烷基化部分，并且它们共同为DC1及其衍生物，用于合成细胞靶向治疗剂。
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公开(公告)号：US08809320B2
公开(公告)日：2014-08-19
申请号：US13774059
申请日：2013-02-22
申请人： Wei Li , Nathan Elliott Fishkin , Robert Yongxin Zhao , Michael Louis Miller , Ravi V. J. Chari
发明人： Wei Li , Nathan Elliott Fishkin , Robert Yongxin Zhao , Michael Louis Miller , Ravi V. J. Chari
IPC分类号： C07D519/00 , A61K31/5517 , A61P35/00 , A61K47/48 , C07D487/04 , A61K38/07 , A61K45/06 , C07D498/04 , C07K5/103 , C07K16/28
CPC分类号： C07K16/2896 , A61K31/5517 , A61K38/07 , A61K45/06 , A61K47/60 , A61K47/6835 , A61K47/6849 , A61K47/6863 , A61P35/00 , C07D487/04 , C07D498/04 , C07D519/00 , C07K5/0202 , C07K5/1008 , C07K16/2803 , C07K16/46 , C07K19/00
摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译： 本发明涉及具有抗增殖活性的新型苯并二氮杂衍生物，更具体地涉及式（I）和（II）的新型苯并二氮杂，其中二氮杂环（B）与杂环（CD）稠合，其中杂环是双环的 或其中二氮杂环（B）与杂环（C）稠合的式（III）化合物，其中杂环是单环的。 本发明提供这些化合物的细胞毒二聚体。 本发明还提供了单体和二聚体的共轭物。 本发明还提供了使用本发明的化合物或缀合物来抑制哺乳动物异常细胞生长或治疗增殖性病症的组合物和方法。 本发明还涉及将化合物或缀合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。
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