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公开(公告)号：US08034904B2
公开(公告)日：2011-10-11
申请号：US10729441
申请日：2003-12-08
IPC分类号： C12P21/08
CPC分类号： C07K16/2863 , A61K39/39541 , A61K2039/505 , C07K2317/24 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/76 , C07K2317/92 , A61K2300/00
摘要： Antibodies, humanized antibodies, resurfaced antibodies, antibody fragments, derivatized antibodies, and conjugates of these molecules with cytotoxic agents, which specifically bind to and inhibit insulin-like growth factor-I receptor, antagonize the effects of IGF-I and are substantially devoid of agonist activity toward the insulin-like growth factor-I receptor. These molecules can be conjugated to cytotoxic agents for use in the treatment of tumors that express elevated levels of IGF-I receptor, such as breast cancer, colon cancer, lung cancer, ovarian carcinoma, synovial sarcoma and pancreatic cancer. These molecules can also be labeled for in vitro and in vivo diagnostic uses, such as in the diagnosis and imaging of tumors that express elevated levels of IGF-I receptor.
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2.发明授权Anti-IGF-I receptor antibodies, DNAs, vectors, host cells and genetic constructs 有权抗IGF-I受体抗体，DNAs，载体，宿主细胞和遗传构建体公开(公告)号：US08268617B2
公开(公告)日：2012-09-18
申请号：US12547543
申请日：2009-08-26
IPC分类号： C12N5/16 , C12N5/07 , C12N15/113 , C07H21/04 , C07K16/28
CPC分类号： A61K39/39558 , A61K31/337 , A61K31/4745 , A61K39/39541 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K16/2863 , C07K2317/24 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/76 , C07K2317/92 , A61K2300/00
摘要： DNAs, vectors, host cells and genetic constructs of antibodies, humanized antibodies, resurfaced antibodies, antibody fragments, derivatized antibodies, and conjugates of these molecules with cytotoxic agents, which specifically bind to and inhibit insulin-like growth factor-I receptor, antagonize the effects of IGF-I and are substantially devoid of agonist activity toward the insulin-like growth factor-I receptor. These molecules can be conjugated to cytotoxic agents for use in the treatment of tumors that express elevated levels of IGF-I receptor, such as breast cancer, colon cancer, lung cancer, ovarian carcinoma, synovial sarcoma and pancreatic cancer. These molecules can also be labeled for in vitro and in vivo diagnostic uses, such as in the diagnosis and imaging of tumors that express elevated levels of IGF-I receptor.
摘要翻译： DNA，载体，宿主细胞和抗体的遗传构建体，人源化抗体，表面抗体，抗体片段，衍生化抗体，以及这些分子与细胞毒性剂的缀合物，其特异性结合并抑制胰岛素样生长因子-I受体拮抗 IGF-I的作用并且对胰岛素样生长因子-I受体基本上没有激动剂活性。 这些分子可以与细胞毒性剂结合，用于治疗表达IGF-1受体水平升高的肿瘤，例如乳腺癌，结肠癌，肺癌，卵巢癌，滑膜肉瘤和胰腺癌。 这些分子也可以用于体外和体内诊断用途的标记，例如在表达IGF-1受体水平升高的肿瘤的诊断和成像中。
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公开(公告)号：US07985842B2
公开(公告)日：2011-07-26
申请号：US12276586
申请日：2008-11-24
IPC分类号： C12P21/08 , C07K16/00 , A61K39/395 , A61K49/00 , C07H21/04 , G01N33/574
CPC分类号： A61K39/39558 , A61K31/337 , A61K31/4745 , A61K39/39541 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K16/2863 , C07K2317/24 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/76 , C07K2317/92 , A61K2300/00
摘要： Antibodies, humanized antibodies, resurfaced antibodies, antibody fragments, derivatized antibodies, and conjugates of these molecules with cytotoxic agents, which specifically bind to and inhibit insulin-like growth factor-I receptor, antagonize the effects of IGF-I and are substantially devoid of agonist activity toward the insulin-like growth factor-I receptor. These molecules can be conjugated to cytotoxic agents for use in the treatment of tumors that express elevated levels of IGF-I receptor, such as breast cancer, colon cancer, lung cancer, ovarian carcinoma, synovial sarcoma and pancreatic cancer. These molecules can also be labeled for in vitro and in vivo diagnostic uses, such as in the diagnosis and imaging of tumors that express elevated levels of IGF-I receptor.
摘要翻译： 抗体，人源化抗体，表面抗体，抗体片段，衍生抗体，以及这些分子与细胞毒性剂的结合物，其特异性结合并抑制胰岛素样生长因子-I受体拮抗IGF-1的作用，并且基本上没有 对胰岛素样生长因子-I受体的激动剂活性。 这些分子可以与细胞毒性剂结合，用于治疗表达IGF-1受体水平升高的肿瘤，例如乳腺癌，结肠癌，肺癌，卵巢癌，滑膜肉瘤和胰腺癌。 这些分子也可以用于体外和体内诊断用途的标记，例如在表达IGF-1受体水平升高的肿瘤的诊断和成像中。
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公开(公告)号：US07538195B2
公开(公告)日：2009-05-26
申请号：US10170390
申请日：2002-06-14
IPC分类号： C12P21/08 , C07K16/00 , A61K39/395 , A61K49/00 , C07H21/04 , G01N33/574
CPC分类号： A61K39/39558 , A61K31/337 , A61K31/4745 , A61K39/39541 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K16/2863 , C07K2317/24 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/76 , C07K2317/92 , A61K2300/00
摘要： Antibodies, humanized antibodies, resurfaced antibodies, antibody fragments, derivatized antibodies, and conjugates of these molecules with cytotoxic agents, which specifically bind to and inhibit insulin-like growth factor-I receptor, antagonize the effects of IGF-I and are substantially devoid of agonist activity toward the insulin-like growth factor-I receptor. These molecules can be conjugated to cytotoxic agents for use in the treatment of tumors that express elevated levels of IGF-I receptor, such as breast cancer, colon cancer, lung cancer, ovarian carcinoma, synovial sarcoma and pancreatic cancer. These molecules can also be labeled for in vitro and in vivo diagnostic uses, such as in the diagnosis and imaging of tumors that express elevated levels of IGF-I receptor.
摘要翻译： 抗体，人源化抗体，表面抗体，抗体片段，衍生抗体，以及这些分子与细胞毒性剂的结合物，其特异性结合并抑制胰岛素样生长因子-I受体拮抗IGF-1的作用，并且基本上没有 对胰岛素样生长因子-I受体的激动剂活性。 这些分子可以与细胞毒性剂结合，用于治疗表达IGF-1受体水平升高的肿瘤，例如乳腺癌，结肠癌，肺癌，卵巢癌，滑膜肉瘤和胰腺癌。 这些分子也可以用于体外和体内诊断用途的标记，例如在表达IGF-1受体水平升高的肿瘤的诊断和成像中。
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公开(公告)号：US09353127B2
公开(公告)日：2016-05-31
申请号：US13397205
申请日：2012-02-15
申请人： Nathan Fishkin , Michael Miller , Wei Li , Rajeeva Singh
发明人： Nathan Fishkin , Michael Miller , Wei Li , Rajeeva Singh
IPC分类号： A61K38/00 , C07D519/00 , A61K47/48 , C07D487/04 , A61K45/06 , A61K31/5517
CPC分类号： C07K16/30 , A61K31/5517 , A61K45/06 , A61K47/545 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6867 , A61K2039/505 , C07D487/04 , C07D519/00 , C07K2317/24 , C07K2317/92 , C07K2317/94
摘要： The present invention is directed to methods of preparing a conjugate of a cell-binding agent and a drug (such as a cytotoxic compound). The methods comprise the use of an imine reactive compound to enable efficient conjugations of cytotoxic compounds with cell binding agents.
摘要翻译： 本发明涉及制备细胞结合剂和药物（例如细胞毒性化合物）的缀合物的方法。 所述方法包括使用亚胺反应性化合物以使细胞毒性化合物与细胞结合剂的有效缀合。
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公开(公告)号：US09238690B2
公开(公告)日：2016-01-19
申请号：US13882059
申请日：2011-10-28
CPC分类号： C07K16/40 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6871 , A61K2039/505 , C07K16/2863 , C07K16/30 , C07K2317/14 , C07K2317/21 , C07K2317/24 , C07K2317/33 , C07K2317/565 , C07K2317/567 , C07K2317/73 , C07K2317/732 , C07K2317/74 , C07K2317/75 , C07K2317/76 , C07K2317/92 , G01N33/74 , G01N2333/71 , G01N2333/912
摘要： Novel anti-cancer agents, including, but not limited to, antibodies and immunoconjugates, that bind to EGFR are provided. Methods of using the agents, antibodies, or immunoconjugates, such as methods of inhibiting tumor growth are further provided.
摘要翻译： 提供了与EGFR结合的新型抗癌剂，包括但不限于抗体和免疫偶联物。 进一步提供使用试剂，抗体或免疫缀合物的方法，例如抑制肿瘤生长的方法。
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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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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：US20140178416A1
公开(公告)日：2014-06-26
申请号：US14080377
申请日：2013-11-14
IPC分类号： C07D207/46 , A61K31/5365
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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10.发明申请公开(公告)号：US20140023662A1
公开(公告)日：2014-01-23
申请号：US13882059
申请日：2011-10-28
CPC分类号： C07K16/40 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6871 , A61K2039/505 , C07K16/2863 , C07K16/30 , C07K2317/14 , C07K2317/21 , C07K2317/24 , C07K2317/33 , C07K2317/565 , C07K2317/567 , C07K2317/73 , C07K2317/732 , C07K2317/74 , C07K2317/75 , C07K2317/76 , C07K2317/92 , G01N33/74 , G01N2333/71 , G01N2333/912
摘要： Novel anti-cancer agents, including, but not limited to, antibodies and immunoconjugates, that bind to EGFR are provided. Methods of using the agents, antibodies, or immunoconjugates, such as methods of inhibiting tumor growth are further provided.
摘要翻译： 提供了与EGFR结合的新型抗癌剂，包括但不限于抗体和免疫偶联物。 进一步提供使用试剂，抗体或免疫缀合物的方法，例如抑制肿瘤生长的方法。
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