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1. 发明申请

US20060002942A1 Calicheamicin conjugates 审中-公开
公开(公告)号：US20060002942A1
公开(公告)日：2006-01-05
申请号：US11080587
申请日：2005-03-15
申请人： Arthur Kunz , Justin Moran , Joseph Rubino , Neera Jain , Erwin Raymond Boghaert , Philip Hamann , Mark Ruppen , Nitin Damle , Eugene Vidunas
发明人： Arthur Kunz , Justin Moran , Joseph Rubino , Neera Jain , Erwin Raymond Boghaert , Philip Hamann , Mark Ruppen , Nitin Damle , Eugene Vidunas
IPC分类号： A61K39/395 , C07K16/46
CPC分类号： C07K16/30 , A61K39/395 , A61K47/6829 , A61K47/6849 , A61K47/6851 , C07K2317/24 , C07K2317/52 , C07K2317/73
摘要： Anti-Lewis Y antibodies are described. Methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative/antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. Specifically, monomeric calicheamicin derivative/anti-Lewis Y antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described.

2. 发明申请

US20070213511A1 Calicheamicin Conjugation by Antibody Deglycosylation 审中-公开
标题翻译：卡利加霉素结合抗体脱糖基化
公开(公告)号：US20070213511A1
公开(公告)日：2007-09-13
申请号：US10592438
申请日：2005-03-15
申请人： Arthur Kunz , Philip Hamann , Justin Moran , Eugene Vidunas
发明人： Arthur Kunz , Philip Hamann , Justin Moran , Eugene Vidunas
IPC分类号： C07K16/46
CPC分类号： C07K16/30 , A61K39/395 , A61K47/6829 , A61K47/6849 , A61K47/6851 , C07K2317/24 , C07K2317/52 , C07K2317/73
摘要： The present invention provides processed for preparing a calicheamicin conjugate comprising removing glycosylation of a protein and reacting (i) an activated calicheamicin—hydrolyzable linker derivative and (ii) the deglycosylated protein. In one embodiment, the protein is an antibody, such as an anti-CD33 antibody (e.g., hp67.6), an anti-CD22 antibody (e.g., G544), an anti-Lewis Y antibody (e.g., G193), an anti-5T4 antibody (e.g., H8) or an anti-CD20 antibody (e.g., rituximab). In another embodiment, the calicheamicin derivative is an N-acyl derivative of calicheamicin or a disulfide analog of calicheamicin, such as N-acetyl gamma calicheamicin dimethyl hydrazide (N-acetyl calicheamicin DMH) and the hydrolyzable linker is 4-(4-acetylephenoxy) butanoic acid (AcBut) or (3-Acetylphenyl) acetic acid (AcPAc). Also provided are calicheamicin conjugates produced by such processes.
摘要翻译：本发明提供加工用于制备加利车霉素缀合物的方法，包括除去蛋白质的糖基化并使（i）活化的加利车霉素可水解连接体衍生物和（ii）去糖基化蛋白质反应。在一个实施方案中，蛋白质是抗体，例如抗CD33抗体（例如hp67.6），抗CD22抗体（例如G544），抗Lewis Y抗体（例如G193），抗 - -5T4抗体（例如H8）或抗CD20抗体（如利妥昔单抗）。在另一个实施方案中，加利车霉素衍生物是加利车霉素的N-酰基衍生物或加利车霉素的二硫化物类似物，例如N-乙酰基γ-加利车霉素二甲基酰肼（N-乙酰加利车霉素DMH），可水解接头是4-（4-乙酰基苯氧基）丁酸（AcBut）或（3-乙酰基苯基）乙酸（AcPAc）。还提供了通过这些方法生产的加利车霉素缀合物。

3. 发明申请

US20090105461A1 Calicheamicin conjugates 审中-公开
标题翻译：加利西霉素共轭物
公开(公告)号：US20090105461A1
公开(公告)日：2009-04-23
申请号：US12221551
申请日：2008-08-04
申请人： Arthur Kunz , Justin Keith Moran , Joseph Thomas Rubino , Neera Jain , Erwin Raymond Arsene Boghaert , Philip Ross Hamann , Mark Edward Ruppen , Nitin Krishnaji Damle , Eugene Vidunas , Lyka Kalyandrug
发明人： Arthur Kunz , Justin Keith Moran , Joseph Thomas Rubino , Neera Jain , Erwin Raymond Arsene Boghaert , Philip Ross Hamann , Mark Edward Ruppen , Nitin Krishnaji Damle , Eugene Vidunas , Lyka Kalyandrug
IPC分类号： C07K16/00
CPC分类号： C07K16/30 , A61K39/395 , A61K47/6829 , A61K47/6849 , A61K47/6851 , C07K2317/24 , C07K2317/52 , C07K2317/73
摘要： Anti-Lewis Y antibodies are described. Methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative/antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. Specifically, monomeric calicheamicin derivative/anti-Lewis Y antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described.
摘要翻译：描述了抗Lewis Y抗体。描述了具有显着高于先前报道的程序并且具有降低的聚集和低共轭分数（LCF）的药物负载的单体细胞毒性药物/载体缀合物的方法。还描述了细胞毒性药物衍生物/抗体缀合物，包含缀合物的组合物和缀合物的用途。具体地，还描述了单体加利车霉素衍生物/抗 - 路易斯Y抗体缀合物，包含缀合物的组合物和缀合物的用途。

4. 发明申请

US20060088522A1 Humanized anti-5T4 antibodies and anti-5T4/calicheamicin conjugates 审中-公开
标题翻译：人源化抗5T4抗体和抗5T4 /加利车霉素缀合物
公开(公告)号：US20060088522A1
公开(公告)日：2006-04-27
申请号：US11221902
申请日：2005-09-09
申请人： Erwin Boghaert , Nitin Damle , Davinder Gill , Kimberly Marquette , Lioudmila Tchistiakova , Philip Hamann , Arthur Kunz
发明人： Erwin Boghaert , Nitin Damle , Davinder Gill , Kimberly Marquette , Lioudmila Tchistiakova , Philip Hamann , Arthur Kunz
IPC分类号： A61K39/395 , C07K16/46 , C07K16/30
CPC分类号： C07K16/3046 , A61K47/60 , A61K47/6809 , A61K47/6851 , A61K2039/505 , C07K16/30 , C07K16/3015 , C07K16/3023 , C07K2317/24 , C07K2317/56 , C07K2317/567 , C07K2317/622 , C07K2317/92
摘要： Chimeric and humanized anti-5T4 antibodies and antibody/drug conjugates and methods for preparing and using the same.
摘要翻译：嵌合和人源化抗5T4抗体和抗体/药物共轭物及其制备和使用方法。

5. 发明授权

US5714586A Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates 失效
标题翻译：单体加利车霉衍生物/载体缀合物的制备方法
公开(公告)号：US5714586A
公开(公告)日：1998-02-03
申请号：US654505
申请日：1996-05-28
申请人： Martin P. Kunstmann , Irwin J. Hollander , Philip Hamann , Arthur Kunz
发明人： Martin P. Kunstmann , Irwin J. Hollander , Philip Hamann , Arthur Kunz
IPC分类号： A61K47/48 , C07K16/00 , A61K31/70 , A61K31/715 , C12P21/08
CPC分类号： A61K47/48369 , A61K47/48407 , A61K47/48684
摘要： A method is provided for preparing monomeric calicheamicin derivative/carrier conjugates with higher drug loading/yield and decreased aggregation. These conjugates are prepared by incubating a calicheamicin derivative and a proteinaceous carrier in a solution comprising a non-nucleophilic, protein-compatible, buffered solution, a cosolvent selected from the group consisting of propylene glycol, ethanol, DMSO, and combinations thereof, and an additive comprising at least one C.sub.6 -C.sub.18 carboxylic acid having a pH in the range from about 4.0 to 8.5 and at a temperature ranging from about 25.degree. C. to about 37.degree. C. for a period of time ranging from about 15 minutes to about 24 hours, and recovering monomeric calicheamicin derivative/carrier conjugates. Alternatively, the conjugates can be prepared by incubating the calicheamicin derivative and a proteinaceous carrier in a solution comprising a non-nucleophilic, protein-compatible, buffered solution and a cosolvent comprising t-butanol.
摘要翻译：提供了用于制备具有更高的药物负荷/产率和降低的聚集的单体加利车霉衍生物/载体缀合物的方法。这些缀合物通过将加利车霉素衍生物和蛋白质载体在包含非亲核性，蛋白质相容性缓冲溶液，选自丙二醇，乙醇，DMSO及其组合的共溶剂的溶液中孵育来制备，以及添加剂，其包含至少一种pH为约4.0-8.5，温度为约25℃至约37℃的C 6 -C 18羧酸，时间为约15分钟至约 24小时，并回收单体加利车霉衍生物/载体缀合物。或者，可以通过将加利车霉素衍生物和蛋白质载体温育在包含非亲核，蛋白质相容的缓冲溶液和包含叔丁醇的助溶剂的溶液中来制备缀合物。

6. 发明申请

US20070231333A1 ANTI-5T4 ANTIBODIES AND USES THEREOF 有权
标题翻译： ANTI-5T4抗体及其用途
公开(公告)号：US20070231333A1
公开(公告)日：2007-10-04
申请号：US11684329
申请日：2007-03-09
申请人： Erwin BOGHAERT , Nitin Damle , Philip Hamann , Kiran Khandke , Arthur Kunz , Kimberly Marquette , Lioudmila Tchistiakova , Davinder Gill , Kodangattil Sreekumar
发明人： Erwin BOGHAERT , Nitin Damle , Philip Hamann , Kiran Khandke , Arthur Kunz , Kimberly Marquette , Lioudmila Tchistiakova , Davinder Gill , Kodangattil Sreekumar
IPC分类号： C07K16/44 , C07K16/30 , A61K39/395
CPC分类号： C07K16/28 , A61K47/6849 , A61K51/1027 , A61K2039/505 , C07K14/82 , C07K16/30 , C07K16/32 , C07K2317/24 , C07K2317/33 , C07K2317/34 , C07K2317/52 , C07K2317/56 , C07K2317/565 , C07K2317/77 , C07K2317/92
摘要： Anti-5T4 antibodies, anti-5T4 antibody/drug conjugates, and methods for preparing and using the same.
摘要翻译：抗5T4抗体，抗5T4抗体/药物偶联物，以及制备和使用该抗体的方法。

7. 发明申请

US20100173382A1 HUMANIZED ANTI-5T4 ANTIBODIES AND ANTI-5T4/CALICHEAMICIN CONJUGATES 审中-公开
标题翻译：抗人抗原5T4抗体和抗-5T4 /卡培他滨联合
公开(公告)号：US20100173382A1
公开(公告)日：2010-07-08
申请号：US12580702
申请日：2009-10-16
申请人： Erwin R. Boghaert , Nitin K. Damle , Davinder S. Gill , Kimberly A. Marquette , Lioudmila Tchistiakova , Philip Ross Hamann , Arthur Kunz
发明人： Erwin R. Boghaert , Nitin K. Damle , Davinder S. Gill , Kimberly A. Marquette , Lioudmila Tchistiakova , Philip Ross Hamann , Arthur Kunz
IPC分类号： C12N9/96 , C07K16/00
CPC分类号： C07K16/3046 , A61K47/60 , A61K47/6809 , A61K47/6851 , A61K2039/505 , C07K16/30 , C07K16/3015 , C07K16/3023 , C07K2317/24 , C07K2317/56 , C07K2317/567 , C07K2317/622 , C07K2317/92
摘要： Chimeric and humanized anti-5T4 antibodies and antibody/drug conjugates and methods for preparing and using the same.
摘要翻译：嵌合和人源化抗5T4抗体和抗体/药物共轭物及其制备和使用方法。

8. 发明授权

US08747857B2 Calicheamicin derivative-carrier conjugates 有权
标题翻译：加利车霉衍生物 - 载体缀合物
公开(公告)号：US08747857B2
公开(公告)日：2014-06-10
申请号：US10699874
申请日：2003-11-03
申请人： Arthur Kunz , Justin Keith Moran , Joseph Thomas Rubino , Neera Jain , Eugene Joseph Vidunas , John McLean Simpson , Nishith Merchant , John Francis Dijoseph , Mark Edward Ruppen , Nitin Krishnaji Damle , Paul David Robbins , Andrew George Popplewell
发明人： Arthur Kunz , Justin Keith Moran , Joseph Thomas Rubino , Neera Jain , Eugene Joseph Vidunas , John McLean Simpson , Nishith Merchant , John Francis Dijoseph , Mark Edward Ruppen , Nitin Krishnaji Damle , Paul David Robbins , Andrew George Popplewell
IPC分类号： A61K39/00 , C07K16/00
CPC分类号： A61K31/704 , A61K47/48384 , A61K47/48407 , A61K47/48507 , A61K47/48561 , A61K47/6803 , A61K47/6809 , A61K47/6849 , C07K16/2803 , C07K2317/21 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/565 , C07K2317/622 , C07K2317/76
摘要： Methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative/antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. Monomeric calicheamicin derivative/anti-CD22 antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described.
摘要翻译：描述了具有显着高于先前报道的程序并且具有降低的聚集和低共轭分数（LCF）的药物负载的单体细胞毒性药物/载体缀合物的方法。还描述了细胞毒性药物衍生物/抗体缀合物，包含缀合物的组合物和缀合物的用途。还描述了单体加利车霉素衍生物/抗-CD22抗体缀合物，包含缀合物的组合物和缀合物的用途。

9. 发明授权

US08153768B2 Calicheamicin derivative-carrier conjugates 有权
标题翻译：加利车霉衍生物 - 载体缀合物
公开(公告)号：US08153768B2
公开(公告)日：2012-04-10
申请号：US10428894
申请日：2003-05-02
申请人： Arthur Kunz , Justin Keith Moran , Joseph Thomas Rubino , Neera Jain , Eugene Joseph Vidunas , John McLean Simpson , Paul David Robbins , Nishith Merchant , John Francis DiJoseph , Mark Edward Ruppen , Nitin Krishnaji Damle , Andrew George Popplewell
发明人： Arthur Kunz , Justin Keith Moran , Joseph Thomas Rubino , Neera Jain , Eugene Joseph Vidunas , John McLean Simpson , Paul David Robbins , Nishith Merchant , John Francis DiJoseph , Mark Edward Ruppen , Nitin Krishnaji Damle , Andrew George Popplewell
IPC分类号： C07K16/00 , C07K17/00 , C07K16/28
CPC分类号： A61K31/704 , A61K47/48384 , A61K47/48407 , A61K47/48507 , A61K47/48561 , A61K47/6803 , A61K47/6809 , A61K47/6849 , C07K16/2803 , C07K2317/21 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/565 , C07K2317/622 , C07K2317/76
摘要： Methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative/antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. Monomeric calicheamicin derivative/anti-CD22 antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described.
摘要翻译：描述了具有显着高于先前报道的程序并且具有降低的聚集和低共轭分数（LCF）的药物负载的单体细胞毒性药物/载体缀合物的方法。还描述了细胞毒性药物衍生物/抗体缀合物，包含缀合物的组合物和缀合物的用途。还描述了单体加利车霉素衍生物/抗-CD22抗体缀合物，包含缀合物的组合物和缀合物的用途。

10. 发明授权

US08044178B2 Anti-5T4 antibodies and uses thereof 有权
标题翻译：抗-5T4抗体及其用途
公开(公告)号：US08044178B2
公开(公告)日：2011-10-25
申请号：US11684329
申请日：2007-03-09
申请人： Erwin R. Boghaert , Nitin K. Damle , Philip Ross Hamann , Kiran Khandke , Arthur Kunz , Kimberly A. Marquette , Lioudmila Tchistiakova , Davinder Gill , Kodangattil Sreekumar
发明人： Erwin R. Boghaert , Nitin K. Damle , Philip Ross Hamann , Kiran Khandke , Arthur Kunz , Kimberly A. Marquette , Lioudmila Tchistiakova , Davinder Gill , Kodangattil Sreekumar
IPC分类号： C07K16/00 , C07K17/00 , C07K17/14 , C12P21/08 , A61K39/395 , A61K39/00
CPC分类号： C07K16/28 , A61K47/6849 , A61K51/1027 , A61K2039/505 , C07K14/82 , C07K16/30 , C07K16/32 , C07K2317/24 , C07K2317/33 , C07K2317/34 , C07K2317/52 , C07K2317/56 , C07K2317/565 , C07K2317/77 , C07K2317/92
摘要： Anti-5T4 antibodies, anti-5T4 antibody/drug conjugates, and methods for preparing and using the same.
摘要翻译：抗5T4抗体，抗5T4抗体/药物偶联物，以及制备和使用该抗体的方法。

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