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公开(公告)号：US10414826B2
公开(公告)日：2019-09-17
申请号：US15811190
申请日：2017-11-13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
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公开(公告)号：US20170000897A1
公开(公告)日：2017-01-05
申请号：US15188843
申请日：2016-06-21
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6803 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y10T428/13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
摘要翻译： 制备包括MeVal-Val-Dil-Dap-Norephedrine（MMAE）和MeVal-Val-Dil-Dap-Phe（MMAF）的Auristatin肽，并通过各种接头包括马来酰亚胺酰基val-cit-PAB连接到配体上。 所得配体药物偶联物在体外和体内都是活性的。
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公开(公告)号：US20140220047A1
公开(公告)日：2014-08-07
申请号：US14194106
申请日：2014-02-28
IPC分类号： A61K47/48
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6803 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y10T428/13
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
摘要翻译： 制备包括MeVal-Val-Dil-Dap-Norephedrine（MMAE）和MeVal-Val-Dil-Dap-Phe（MMAF）的Auristatin肽，并通过各种接头包括马来酰亚胺酰基val-cit-PAB连接到配体上。 所得配体药物偶联物在体外和体内都是活性的。
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4.发明授权公开(公告)号：US10000555B2
公开(公告)日：2018-06-19
申请号：US13666766
申请日：2012-11-01
IPC分类号： C07K16/00 , C07K5/02 , C07K7/02 , C07K16/28 , C07K5/10 , C07K7/06 , A61K47/65 , A61K47/68 , A61K38/00
CPC分类号： C07K16/00 , A61K38/00 , A61K47/65 , A61K47/6811 , A61K47/6849 , C07K5/0205 , C07K5/10 , C07K7/02 , C07K7/06 , C07K16/2878 , Y02A50/402 , Y02A50/411 , Y02A50/422 , Y02A50/471 , Y02A50/483
摘要： Auristatin peptide analogs of MeVal-Val-Dil-Dap-Phe (MMAF) are provided having C-terminal phenylalanine residue side chain replacements or modifications which are provided alone or attached to ligands through various linkers. The related conjugates can target specific cell types to provide therapeutic benefit.
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公开(公告)号：US09504756B2
公开(公告)日：2016-11-29
申请号：US13799244
申请日：2013-03-13
发明人： Robert Lyon , Svetlana O. Doronina , Timothy Bovee
IPC分类号： A61K39/00 , C07K7/02 , A61K47/48 , C07K5/062 , C07D207/36
CPC分类号： A61K47/6803 , A61K47/65 , C07D207/36 , C07K5/06052 , C07K7/02
摘要： The present invention provides Ligand-Drug Conjugates, Drug-Linkers, Linkers, and Ligand-Linker Conjugates comprising a self-stabilizing linker assembly component.
摘要翻译： 本发明提供了包含自稳定接头组件组分的配体药物偶联物，药物连接子，连接体和配体 - 连接子缀合物。
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公开(公告)号：US20210008099A1
公开(公告)日：2021-01-14
申请号：US16968749
申请日：2019-02-20
摘要： Ligand Drug Conjugates of hydrophobically-modified auristatin F compounds that exhibit cytotoxic activities towards targeted cells, including abnormal cells such as cancer cells, that are MDR+ while also exhibiting bystander activities towards nearby cells having lower expression of the moeity targeted by the Conjugate.
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公开(公告)号：US20150320879A1
公开(公告)日：2015-11-12
申请号：US14727340
申请日：2015-06-01
发明人： Robert Lyon , Svetlana O. Doronina , Timothy Bovee
IPC分类号： A61K47/48 , C07K5/062 , C07D207/36 , C07K7/02
CPC分类号： A61K47/6803 , A61K47/65 , C07D207/36 , C07K5/06052 , C07K7/02
摘要： The present invention provides Ligand-Drug Conjugates, Drug-Linkers, Linkers, and Ligand-Linker Conjugates comprising a self-stabilizing linker assembly component.
摘要翻译： 本发明提供了包含自稳定接头组件组分的配体药物偶联物，药物连接子，连接子和配体 - 连接子缀合物。
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公开(公告)号：US20130309256A1
公开(公告)日：2013-11-21
申请号：US13799244
申请日：2013-03-13
发明人： Robert Lyon , Svetlana O. Doronina , Timothy Bovee
IPC分类号： C07K7/02
CPC分类号： A61K47/6803 , A61K47/65 , C07D207/36 , C07K5/06052 , C07K7/02
摘要： The present invention provides Ligand-Drug Conjugates, Drug-Linkers, Linkers, and Ligand-Linker Conjugates comprising a self-stabilizing linker assembly component.
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公开(公告)号：US10808039B2
公开(公告)日：2020-10-20
申请号：US16507839
申请日：2019-07-10
摘要： Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
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10.发明申请MONOMETHYLVALINE COMPOUNDS HAVING PHENYLALANINE SIDE-CHAIN MODIFICATIONS AT THE C-TERMINUS 有权在C-TERMINUS上具有苯乙酰胺侧链修饰的单甲基化合物公开(公告)号：US20130123465A1
公开(公告)日：2013-05-16
申请号：US13666766
申请日：2012-11-01
CPC分类号： C07K16/00 , A61K38/00 , A61K47/65 , A61K47/6811 , A61K47/6849 , C07K5/0205 , C07K5/10 , C07K7/02 , C07K7/06 , C07K16/2878 , Y02A50/402 , Y02A50/411 , Y02A50/422 , Y02A50/471 , Y02A50/483
摘要： Auristatin peptide analogs of MeVal-Val-Dil-Dap-Phe (MMAF) are provided having C-terminal phenylalanine residue side chain replacements or modifications which are provided alone or attached to ligands through various linkers. The related conjugates can target specific cell types to provide therapeutic benefit.
摘要翻译： 提供MeVal-Val-Dil-Dap-Phe（MMAF）的Auristatin肽类似物，其具有C端苯丙氨酸残基侧链取代或修饰，其单独提供或通过各种接头与配体连接。 相关的缀合物可以靶向特定细胞类型以提供治疗益处。
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