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1.发明申请公开(公告)号：US20200215206A1
公开(公告)日：2020-07-09
申请号：US16074981
申请日：2016-02-04
发明人： Robert Yongxin Zhao , Qingliang Yang , Yuanyuan Huang , Shun Gai , Linyao Zhao , Hangbo Ye , Huihui Guo , Qianqian Tong , Minjun Cao , Junxiang Jia , Chengyu Yang , Wenjun Li , Xiaomai Zhou , Hongsheng Xie , Chen Lin , Zhixiang Guo , Zhicang Ye
IPC分类号： A61K49/00 , A61K47/68 , C07D519/00 , C07D513/22 , C07D498/18 , C07D417/14 , C07D417/12
摘要： The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)-butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
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2.发明申请ACETYLENEDICARBOXYL LINKERS AND THEIR USES IN SPECIFIC CONJUGATION OF A CELL-BINDING MOLECULE 有权乙炔二羧酸连接体及其在细胞结合分子特异性结合中的应用公开(公告)号：US20150322155A1
公开(公告)日：2015-11-12
申请号：US14799666
申请日：2015-07-15
发明人： Robert Yongxin Zhao
IPC分类号： C07K16/28 , C07C59/76 , A61K47/48 , C07C237/52 , A61K45/06 , A61K39/395 , C07D207/46 , C07D417/14
CPC分类号： A61K47/6803 , A61K31/337 , A61K31/404 , A61K31/537 , A61K31/5517 , A61K38/05 , A61K39/395 , A61K39/3955 , A61K45/06 , A61K47/6809 , A61K47/6849 , A61K47/6851 , A61K47/6889 , A61K2039/505 , C07C59/76 , C07C233/20 , C07C237/52 , C07D207/46 , C07D277/56 , C07D309/14 , C07D403/14 , C07D407/12 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D493/04 , C07D498/14 , C07D519/00 , C07K16/28 , C07K16/2863 , C07K16/32 , C07K2317/24 , G01N33/5014 , Y02A50/473
摘要： The present invention relates to novel acetylenedicarboxyl linkers used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
摘要翻译： 本发明涉及用于通过桥连接细胞结合分子上的硫醇对化合物/细胞毒剂对细胞结合分子的特异性缀合的新的炔二羧酸接头。 本发明还涉及制备这种接头的方法，以及使用这种连接体制备均相共轭物的方法，以及缀合物在治疗癌症，感染和自身免疫疾病中的应用。
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公开(公告)号：US20150314017A1
公开(公告)日：2015-11-05
申请号：US14799712
申请日：2015-07-15
发明人： Robert Yongxin Zhao
IPC分类号： A61K47/48 , C07C243/28 , C07D207/452 , C07D403/14 , C07C311/55 , C07D213/71 , C07K5/065 , A61K45/06 , C07C275/50
CPC分类号： A61K31/337 , A61K31/404 , A61K31/5365 , A61K31/551 , A61K31/5513 , A61K45/06 , A61K47/6803 , A61K47/6889 , A61K49/0002 , C07C243/28 , C07C275/50 , C07C311/55 , C07D207/452 , C07D213/71 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D493/08 , C07D498/14 , C07D519/00 , C07K5/06078 , C07K5/06139 , Y02A50/385 , Y02A50/402 , Y02A50/414 , Y02A50/415 , Y02A50/463 , Y02A50/473 , Y02A50/49
摘要： The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
摘要翻译： 本发明涉及含有肼的新型二硫桥连接体，其通过将细胞结合分子上的一对硫醇连接起来将化合物/细胞毒性剂与细胞结合分子的特异性缀合用于肼。 本发明还涉及制备这种接头的方法，以及使用这种连接体制备均相共轭物的方法，以及缀合物在治疗癌症，感染和自身免疫疾病中的应用。
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4.发明授权公开(公告)号：US09839687B2
公开(公告)日：2017-12-12
申请号：US14799666
申请日：2015-07-15
发明人： Robert Yongxin Zhao
IPC分类号： C07D417/14 , C07D413/14 , C07D407/14 , C07D403/14 , C07D309/14 , C07C237/52 , C07C233/20 , C07C59/76 , A61K39/395 , C07K16/28 , A61K45/06 , A61K47/48 , C07D207/46 , C07D407/12 , C07D413/04 , C07D417/12 , C07D493/04 , C07D498/14 , C07D277/56 , C07D519/00 , A61K39/00
CPC分类号： A61K47/6803 , A61K31/337 , A61K31/404 , A61K31/537 , A61K31/5517 , A61K38/05 , A61K39/395 , A61K39/3955 , A61K45/06 , A61K47/6809 , A61K47/6849 , A61K47/6851 , A61K47/6889 , A61K2039/505 , C07C59/76 , C07C233/20 , C07C237/52 , C07D207/46 , C07D277/56 , C07D309/14 , C07D403/14 , C07D407/12 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D493/04 , C07D498/14 , C07D519/00 , C07K16/28 , C07K16/2863 , C07K16/32 , C07K2317/24 , G01N33/5014 , Y02A50/473
摘要： The present invention relates to novel acetylenedicarboxyl linkers used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
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公开(公告)号：US20170151346A1
公开(公告)日：2017-06-01
申请号：US15431154
申请日：2017-02-13
发明人： Robert Yongxin Zhao
IPC分类号： A61K45/00 , A61K31/337 , A61K31/5513 , A61K31/5365 , A61K31/404
CPC分类号： A61K31/337 , A61K31/404 , A61K31/5365 , A61K31/551 , A61K31/5513 , A61K45/06 , A61K47/6803 , A61K47/6889 , A61K49/0002 , C07C243/28 , C07C275/50 , C07C311/55 , C07D207/452 , C07D213/71 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D493/08 , C07D498/14 , C07D519/00 , C07K5/06078 , C07K5/06139 , Y02A50/385 , Y02A50/402 , Y02A50/414 , Y02A50/415 , Y02A50/463 , Y02A50/473 , Y02A50/49
摘要： The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
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公开(公告)号：US10307391B2
公开(公告)日：2019-06-04
申请号：US15479903
申请日：2017-04-05
发明人： Robert Yongxin Zhao
IPC分类号： A61K31/5365 , A61K31/337 , A61K45/06 , C07C243/28 , C07D207/452 , C07C275/50 , C07C311/55 , C07D213/71 , C07K5/065 , C07D403/14 , C07K5/078 , C07D405/14 , C07D413/14 , C07D417/14 , C07D493/08 , C07D498/14 , C07D519/00 , A61K31/404 , A61K31/5513 , A61K31/551 , A61K49/00 , A61K47/68
摘要： The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
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7.发明授权公开(公告)号：US10232051B2
公开(公告)日：2019-03-19
申请号：US15448639
申请日：2017-03-03
发明人： Robert Yongxin Zhao
IPC分类号： A61K38/05 , A61K38/06 , A61K47/68 , C07K16/28 , C07C59/76 , C07D417/14 , C07C237/52 , A61K39/395 , A61K45/06 , C07D207/46 , C07C233/20 , C07D413/14 , C07D309/14 , C07D403/14 , C07D407/12 , C07D407/14 , C07D413/04 , C07D417/12 , C07D493/04 , C07D498/14 , C07D277/56 , C07D519/00 , A61K31/337 , A61K31/404 , A61K31/537 , A61K31/5517 , G01N33/50 , C07K16/32 , A61K39/00
摘要： Cell binding agent-drug conjugates comprising bridge linkers, and methods of using such linkers and conjugates are provided.
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8.发明授权公开(公告)号：US10293055B2
公开(公告)日：2019-05-21
申请号：US15448634
申请日：2017-03-03
发明人： Robert Yongxin Zhao
IPC分类号： A61K47/68 , C07K16/28 , C07C59/76 , C07D417/14 , C07C237/52 , A61K39/395 , A61K45/06 , C07D207/46 , C07C233/20 , C07D413/14 , C07D309/14 , C07D403/14 , C07D407/12 , C07D407/14 , C07D413/04 , C07D417/12 , C07D493/04 , C07D498/14 , C07D277/56 , C07D519/00 , A61K31/337 , A61K31/404 , A61K31/537 , A61K31/5517 , G01N33/50 , A61K38/05 , C07K16/32 , A61K39/00
摘要： Cell binding agent-drug conjugates comprising bridge linkers, and methods of using such linkers and conjugates are provided.
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公开(公告)号：US10975112B2
公开(公告)日：2021-04-13
申请号：US14740403
申请日：2015-06-16
发明人： Robert Yongxin Zhao
IPC分类号： C07F9/6558 , C07F9/572 , C07F9/6561 , C07F9/6584 , A61K45/06 , A61K47/68 , C07F9/58
摘要： Cell binding agent-drug conjugates comprising hydrophilic linkers, and methods of using such linkers and conjugates are provided.
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10.发明授权公开(公告)号：US10328157B2
公开(公告)日：2019-06-25
申请号：US15423695
申请日：2017-02-03
发明人： Robert Yongxin Zhao
IPC分类号： A61K47/68 , C07K16/28 , C07C59/76 , C07D417/14 , C07C237/52 , A61K39/395 , A61K45/06 , C07D207/46 , C07C233/20 , C07D413/14 , C07D309/14 , C07D403/14 , C07D407/12 , C07D407/14 , C07D413/04 , C07D417/12 , C07D493/04 , C07D498/14 , C07D277/56 , C07D519/00 , A61K31/337 , A61K31/404 , A61K31/537 , A61K31/5517 , G01N33/50 , A61K38/05 , C07K16/32 , A61K39/00
摘要： Cell binding agent-drug conjugates comprising bridge linkers, and methods of using such linkers and conjugates are provided.
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