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公开(公告)号：US20120148610A1
公开(公告)日：2012-06-14
申请号：US13397656
申请日：2012-02-15
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07K16/00
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.
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公开(公告)号：US20120148608A1
公开(公告)日：2012-06-14
申请号：US13397644
申请日：2012-02-15
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , C07K16/00
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.
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公开(公告)号：US20120003248A1
公开(公告)日：2012-01-05
申请号：US13098393
申请日：2011-04-29
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07K19/00
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y02A50/491 , Y02A50/492 , 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.
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公开(公告)号：US07745394B2
公开(公告)日：2010-06-29
申请号：US11833964
申请日：2007-08-03
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K38/00
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y02A50/491 , Y02A50/492 , 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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5.发明授权Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus 有权在C末端具有苯丙氨酸羧基修饰的单甲基缬氨酸化合物公开(公告)号：US08871720B2
公开(公告)日：2014-10-28
申请号：US11994459
申请日：2006-07-07
CPC分类号： A61K47/48415 , A61K38/00 , A61K39/3955 , A61K47/6811 , A61K2039/505 , C07K5/0205 , C07K7/02 , C07K16/2866 , C07K2317/76 , Y02A50/40 , Y02A50/401 , Y02A50/406 , Y02A50/48
摘要： Auristatin peptide analogs of MeVal-Val-Dil-Dap-Phe (MMAF) having a carboxylic acid equivalent at the C-terminal phenylalanine 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： 制备具有C-末端苯丙氨酸羧酸当量的MeVal-Val-Dil-Dap-Phe（MMAF）的Auristatin肽类似物，并通过各种接头包括马来酰亚氨基己酰基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：US20120027784A1
公开(公告)日：2012-02-02
申请号：US13189452
申请日：2011-07-22
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07K17/00
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.
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公开(公告)号：US07964567B2
公开(公告)日：2011-06-21
申请号：US11833961
申请日：2007-08-03
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
CPC分类号： C07K16/32 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K2039/505 , C07K7/02 , C07K2317/24 , Y02A50/414 , Y02A50/423 , Y02A50/469 , Y02A50/491 , Y02A50/492 , 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.
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公开(公告)号：US20120141509A1
公开(公告)日：2012-06-07
申请号：US13397654
申请日：2012-02-15
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07K16/00
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.
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公开(公告)号：US20120141508A1
公开(公告)日：2012-06-07
申请号：US13397650
申请日：2012-02-15
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07K16/00
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：US20120034247A1
公开(公告)日：2012-02-09
申请号：US13189456
申请日：2011-07-22
申请人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
发明人： Svetlana O. Doronina , Peter D. Senter , Brian E. Toki , Allen J. Ebens , Toni Beth Kline , Paul Polakis , Mark X. Sliwkowski , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07K16/18
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.
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