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1. 发明申请

WO2012112687A1 METHODS OF PREPARATION OF CONJUGATES 审中-公开
标题翻译：共混物的制备方法
公开(公告)号：WO2012112687A1
公开(公告)日：2012-08-23
申请号：PCT/US2012/025257
申请日：2012-02-15
申请人： IMMUNOGEN, INC. , FISHKIN, Nathan , MILLER, Michael , LI, Wei , SINGH, Rajeeva
发明人： FISHKIN, Nathan , MILLER, Michael , LI, Wei , SINGH, Rajeeva
IPC分类号： A61K47/48 , C07D487/04 , C07D519/00 , A61P35/00
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。

2. 发明申请

WO2012128868A1 CYTOTOXIC BENZODIAZEPINE DERIVATIVES 审中-公开
公开(公告)号：WO2012128868A1
公开(公告)日：2012-09-27
申请号：PCT/US2012/025252
申请日：2012-02-15
申请人： IMMUNOGEN, INC. , LI, Wei , MILLER, Michael , FISHKIN, Nathan , CHARI, Ravi, V. J.
发明人： LI, Wei , MILLER, Michael , FISHKIN, Nathan , CHARI, Ravi, V. J.
IPC分类号： A61K47/48 , C07D487/04 , C07D519/00 , A61P35/00
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 invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. 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.
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） - （VII）的新型苯并二氮杂化合物。本发明还提供了与细胞结合剂连接的苯并二氮杂类化合物的缀合物。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。

3. 发明申请

WO2012145112A2 NOVEL MAYTANSINOID DERIVATIVES WITH SULFOXIDE LINKER 审中-公开
标题翻译：新型可可三唑衍生物与SULFOXIDE连接器
公开(公告)号：WO2012145112A2
公开(公告)日：2012-10-26
申请号：PCT/US2012/029791
申请日：2012-03-20
申请人： IMMUNOGEN, INC. , FISHKIN, Nathan
发明人： FISHKIN, Nathan
IPC分类号： C07D491/14
CPC分类号： C07D498/04 , A61K31/5365 , A61K31/537 , A61K45/06 , A61K47/6803 , A61K47/6849 , C07D498/18 , Y02A50/423 , Y02A50/491 , A61K2300/00
摘要： The invention relates to novel maytansinoid compounds having sulfoxide linkers and more specifically to novel maytansinoid compounds of structural formula (I) and (II). The invention also provides conjugates of the maytansinoid compounds linked to a cell-binding agent. 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.
摘要翻译：本发明涉及具有亚砜接头的新型美登木素生物化合物，更具体地涉及结构式（I）和（II）的新型美登木素生物碱化合物。本发明还提供与细胞结合剂连接的美登木素生物碱化合物的缀合物。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。

4. 发明申请

WO2015085003A1 COMPOSITIONS AND METHODS FOR ANTIBODY PRODUCTION 审中-公开
标题翻译：用于抗体生产的组合物和方法
公开(公告)号：WO2015085003A1
公开(公告)日：2015-06-11
申请号：PCT/US2014/068440
申请日：2014-12-03
申请人： IMMUNOGEN, INC.
发明人： SINGH, Rajeeva , FISHKIN, Nathan , KITCHENER, Seth , MESHULAM, Deborah
IPC分类号： C12P1/00
CPC分类号： C12P21/005 , C07K1/1133 , C07K16/00 , C07K2317/14 , C12N2500/30 , C12N2500/44 , C12P21/00
摘要： Compositions and methods for minimizing antibody disulfide bond reduction are described. In one aspect, a composition is provided for culturing mammalian host cells to express an antibody including an anti-reduction agent that minimizes reduction of a disulfide bond in the antibody or fragment thereof. In some other aspects, methods for minimizing disulfide bond reduction; increasing production of an antibody or fragment thereof with intact native disulfide bonds; increasing a ratio of non-reduced to reduced antibody or fragment thereof; producing a therapeutic antibody or fragment thereof by adding a sufficient amount of an anti-reduction agent to a cell culture media, pre-harvest cell culture fluid, or harvest cell culture fluid are described. In another aspect, minimizing disulfide bond reduction in an antibody or fragment thereof culturing the host cell in a concentration of at least about 20% O 2 is described.
摘要翻译：描述了最小化抗体二硫键还原的组合物和方法。一方面，提供了一种组合物，用于培养哺乳动物宿主细胞以表达包含使抗体或其片段中二硫键还原最小化的抗还原剂的抗体。在一些其它方面，使二硫键还原最小化的方法; 增加具有完整天然二硫键的抗体或其片段的产生; 增加未还原抗体或其片段的比例; 通过向细胞培养基，收获前细胞培养液或收获细胞培养液中添加足够量的抗还原剂来制备治疗性抗体或其片段。在另一方面，描述了以至少约20％O 2的浓度培养宿主细胞的抗体或其片段中的二硫键还原最小化。

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