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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

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。

3. 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。

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