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1. 发明申请

WO2007098124A3 PROCESSES FOR THE CONVERGENT SYNTHESIS OF CALICHEAMICIN DERIVATIVES 审中-公开
公开(公告)号：WO2007098124A3
公开(公告)日：2007-08-30
申请号：PCT/US2007/004301
申请日：2007-02-16
申请人： WYETH , MORAN, Justin, Keith , GU, Jianxin
发明人： MORAN, Justin, Keith , GU, Jianxin
IPC分类号： C07H15/203
摘要： This invention describes processes for the convergent synthesis of calicheamicin derivatives of Formula (I)1 and similar analogs using bifunctional and trifunctional linker intermediates.

2. 发明申请

WO2003092623A3 CALICHEAMICIN DERIVATIVE-CARRIER CONJUGATES 审中-公开
公开(公告)号：WO2003092623A3
公开(公告)日：2003-11-13
申请号：PCT/US2003/013910
申请日：2003-05-02
申请人： WYETH HOLDINGS CORPORATION , KUNZ, Arthur , MORAN, Justin, Keith , RUBINO, Joseph, Thomas , JAIN, Neera , VIDUNAS, Eugene, Joseph , SIMPSON, John, McLean , ROBBINS, Paul, David , MERCHANT, Nishith , DIJOSEPH, John, Francis , RUPPEN, Mark, Edward , DAMLE, Nitin, Krishnaji , POPPLEWELL, Andrew, George
发明人： KUNZ, Arthur , MORAN, Justin, Keith , RUBINO, Joseph, Thomas , JAIN, Neera , VIDUNAS, Eugene, Joseph , SIMPSON, John, McLean , ROBBINS, Paul, David , MERCHANT, Nishith , DIJOSEPH, John, Francis , RUPPEN, Mark, Edward , DAMLE, Nitin, Krishnaji , POPPLEWELL, Andrew, George
IPC分类号： A61K39/395
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.

3. 发明申请

WO2007149560A2 FERMENTATION AND PURIFICATION OF ACTINOMADURA CHROMOPROTEIN AND RELATED SPECIES 审中-公开
标题翻译： ACTINOMADURA CHROMOPROTEIN和相关物种的发酵和纯化
公开(公告)号：WO2007149560A2
公开(公告)日：2007-12-27
申请号：PCT/US2007/014568
申请日：2007-06-21
申请人： WYETH , VIDUNAS, Eugene, Joseph , TSAI, Gow-Jen , CAI, Ping , MORAN, Justin, Keith , CHARBONNEAU, Pamela, Sue, Fink , GORDON, Lourdes, Jeannette
发明人： VIDUNAS, Eugene, Joseph , TSAI, Gow-Jen , CAI, Ping , MORAN, Justin, Keith , CHARBONNEAU, Pamela, Sue, Fink , GORDON, Lourdes, Jeannette
IPC分类号： A61K47/48 , C07D491/08 , C07K14/36
CPC分类号： C07D413/12 , A61K47/6829 , A61K47/6849 , A61K47/6851 , C07K14/36 , C12N1/20 , C12P17/16 , C12R1/03
摘要： The present invention provides methods for production and purification of active chromoproteins produced by Actinomadura sp. 21G792. The chromoproteins are useful for developing pharmaceutical compositions and treating diseases such as cancer or bacterial infections.
摘要翻译：本发明提供了由Actinomadura sp。生产和生产活性色素的方法。 21G792。生色蛋白可用于开发药物组合物和治疗疾病如癌症或细菌感染。

4. 发明申请

WO2005089808A2 CALICHEAMICIN CONJUGATES 审中-公开
标题翻译：加利福尼亚联合
公开(公告)号：WO2005089808A2
公开(公告)日：2005-09-29
申请号：PCT/US2005/008508
申请日：2005-03-15
申请人： WYETH , KUNZ, Arthur , MORAN, Justin, Keith , RUBINO, Joseph, Thomas , JAIN, Neera , BOGHAERT, Erwin, Raymond, Arsene , HAMANN, Philip, Ross , RUPPEN, Mark, Edward , DAMLE, Nitin, Krishnaji , VIDUNAS, Eugene
发明人： KUNZ, Arthur , MORAN, Justin, Keith , RUBINO, Joseph, Thomas , JAIN, Neera , BOGHAERT, Erwin, Raymond, Arsene , HAMANN, Philip, Ross , RUPPEN, Mark, Edward , DAMLE, Nitin, Krishnaji , VIDUNAS, Eugene
IPC分类号： A61K47/48
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。

5. 发明申请

WO2005089809A2 IMPROVED CALICHEAMICIN CONJUGATION BY ANTIBODY DEGLYCOSYLATION 审中-公开
标题翻译：通过抗体降解改善钙化蛋白结合
公开(公告)号：WO2005089809A2
公开(公告)日：2005-09-29
申请号：PCT/US2005/008509
申请日：2005-03-15
申请人： WYETH , KUNZ, Arthur , HAMANN, Philip, Ross , MORAN, Justin, Keith , VIDUNAS, Eugene
发明人： KUNZ, Arthur , HAMANN, Philip, Ross , MORAN, Justin, Keith , VIDUNAS, Eugene
IPC分类号： A61K47/48
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-(4acetylephenoxy) 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-乙烯基苯氧基）丁酸酸（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。

6. 发明申请

WO2003092623A2 CALICHEAMICIN DERIVATIVE-CARRIER CONJUGATES 审中-公开
标题翻译：卡利辛胺衍生物载体结合物
公开(公告)号：WO2003092623A2
公开(公告)日：2003-11-13
申请号：PCT/US2003/013910
申请日：2003-05-02
申请人： WYETH HOLDINGS CORPORATION , KUNZ, Arthur , MORAN, Justin, Keith , RUBINO, Joseph, Thomas , JAIN, Neera , VIDUNAS, Eugene, Joseph , SIMPSON, John, McLean , ROBBINS, Paul, David , MERCHANT, Nishith , DIJOSEPH, John, Francis , RUPPEN, Mark, Edward , DAMLE, Nitin, Krishnaji , POPPLEWELL, Andrew, George
发明人： KUNZ, Arthur , MORAN, Justin, Keith , RUBINO, Joseph, Thomas , JAIN, Neera , VIDUNAS, Eugene, Joseph , SIMPSON, John, McLean , ROBBINS, Paul, David , MERCHANT, Nishith , DIJOSEPH, John, Francis , RUPPEN, Mark, Edward , DAMLE, Nitin, Krishnaji , POPPLEWELL, Andrew, George
IPC分类号： A61K
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。

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