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公开(公告)号：US08399403B2
公开(公告)日：2013-03-19
申请号：US12610952
申请日：2009-11-02
申请人： Sharon E. Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Kilian Horgan , Zhi-Hong Li , Bilal Sufi
发明人： Sharon E. Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Kilian Horgan , Zhi-Hong Li , Bilal Sufi
IPC分类号： A61K38/00
CPC分类号： C07D487/04 , A61K47/65 , B82Y30/00 , C07D405/14 , C07D417/12
摘要： The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
摘要翻译： 本公开提供了药物 - 配体缀合物，其是有效的细胞毒素，其中药物通过肽基，肼或二硫键接头与配体连接。 本公开还涉及含有药物 - 配体缀合物的组合物以及使用它们的治疗方法。
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公开(公告)号：US07691962B2
公开(公告)日：2010-04-06
申请号：US11134826
申请日：2005-05-19
申请人： Sharon E. Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Killian Horgan , Zhi-Hong Li , Bilal Sufi
发明人： Sharon E. Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Killian Horgan , Zhi-Hong Li , Bilal Sufi
CPC分类号： C07D487/04 , A61K47/65 , B82Y30/00 , C07D405/14 , C07D417/12
摘要： The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
摘要翻译： 本公开提供了药物 - 配体缀合物，其是有效的细胞毒素，其中药物通过肽基，肼或二硫键接头与配体连接。 本公开还涉及含有药物 - 配体缀合物的组合物以及使用它们的治疗方法。
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公开(公告)号：US20100092496A1
公开(公告)日：2010-04-15
申请号：US12610952
申请日：2009-11-02
申请人： Sharon E. Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Killian Horgan , Zhi-Hong Li , Bilal Sufi
发明人： Sharon E. Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Killian Horgan , Zhi-Hong Li , Bilal Sufi
IPC分类号： A61K31/403 , C07K16/00 , C07D209/56 , C07D403/14 , A61K31/40 , A61K31/497 , A61P35/00
CPC分类号： C07D487/04 , A61K47/65 , B82Y30/00 , C07D405/14 , C07D417/12
摘要： The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
摘要翻译： 本公开提供了药物 - 配体缀合物，其是有效的细胞毒素，其中药物通过肽基，肼或二硫键接头与配体连接。 本公开还涉及含有药物 - 配体缀合物的组合物以及使用它们的治疗方法。
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公开(公告)号：US20060024317A1
公开(公告)日：2006-02-02
申请号：US11134826
申请日：2005-05-19
申请人： Sharon Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Killian Horgan , Zhi-Hong Li , Bilal Sufi
发明人： Sharon Boyd , Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Killian Horgan , Zhi-Hong Li , Bilal Sufi
IPC分类号： A61K39/395 , C07K16/46 , C07D487/02 , C07D405/14
CPC分类号： C07D487/04 , A61K47/65 , B82Y30/00 , C07D405/14 , C07D417/12
摘要： The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
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公开(公告)号：US07517903B2
公开(公告)日：2009-04-14
申请号：US11134685
申请日：2005-05-19
申请人： Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Zhi-Hong Li , Bilal Sufi
发明人： Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Zhi-Hong Li , Bilal Sufi
IPC分类号： A61K31/403
CPC分类号： A61K31/403 , A61K47/556 , A61K47/6803 , A61K47/6889 , B82Y5/00 , C07D403/14 , C07D405/06 , C07D405/14 , C07D417/14 , C07D487/04 , C07D501/34 , C07K5/1008
摘要： The present disclosure provides drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-cleavable substrate conjugates, and to methods of treatment using them.
摘要翻译： 本公开提供了药物可切割底物共轭物，其是有效的细胞毒素。 本公开还涉及含有药物可切割底物缀合物的组合物，以及使用它们的治疗方法。
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公开(公告)号：US20060004081A1
公开(公告)日：2006-01-05
申请号：US11134685
申请日：2005-05-19
申请人： Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Zhi-Hong Li , Bilal Sufi
发明人： Liang Chen , Sanjeev Gangwar , Vincent Guerlavais , Zhi-Hong Li , Bilal Sufi
IPC分类号： A61K31/403 , C07D43/02
CPC分类号： A61K31/403 , A61K47/556 , A61K47/6803 , A61K47/6889 , B82Y5/00 , C07D403/14 , C07D405/06 , C07D405/14 , C07D417/14 , C07D487/04 , C07D501/34 , C07K5/1008
摘要： The present disclosure provides drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-cleavable substrate conjugates, and to methods of treatment using them.
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公开(公告)号：USRE41252E1
公开(公告)日：2010-04-20
申请号：US12126731
申请日：2008-05-23
申请人： Howard P. Ng , Danny P. C. McGee , Guoxian Wu , Jimmie Moore , Zhi-Hong Li , Sanjeev Gangwar , Oliver L. Saunder , Irina Astafieva , Valeri Martichonok
发明人： Howard P. Ng , Danny P. C. McGee , Guoxian Wu , Jimmie Moore , Zhi-Hong Li , Sanjeev Gangwar , Oliver L. Saunder , Irina Astafieva , Valeri Martichonok
IPC分类号： A61K31/535 , A61K31/407 , C07D487/02
CPC分类号： C07D405/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D405/14 , C07D487/04 , C07D487/10 , C07F7/1804 , C07F9/6561
摘要： The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
摘要翻译： 本发明提供了作为有效的细胞毒素的杜卡霉素的类似物。 还提供了在体内被切割的肽基和二硫键接头。 连接体可用于形成本发明的细胞毒素的前药和缀合物以及其它诊断和治疗部分。 本发明提供了杜卡霉素类似物与本发明连接臂的前药和缀合物。
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公开(公告)号：US07507420B2
公开(公告)日：2009-03-24
申请号：US11224580
申请日：2005-09-12
申请人： Howard P. Ng , Danny P. C. McGee , Guoxian Wu , Jimmie Moore , Zhi-Hong Li , Sanjeev Gangwar , Oliver L. Saunders , Irina Astafieva
发明人： Howard P. Ng , Danny P. C. McGee , Guoxian Wu , Jimmie Moore , Zhi-Hong Li , Sanjeev Gangwar , Oliver L. Saunders , Irina Astafieva
CPC分类号： C07D405/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D405/14 , C07D487/04 , C07D487/10 , C07F7/1804 , C07F9/6561
摘要： The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
摘要翻译： 本发明提供了作为有效的细胞毒素的杜卡霉素的类似物。 还提供了在体内被切割的肽基和二硫键接头。 连接体可用于形成本发明的细胞毒素的前药和缀合物以及其它诊断和治疗部分。 本发明提供了杜卡霉素类似物与本发明的连接臂的前药和缀合物。
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公开(公告)号：US07977465B2
公开(公告)日：2011-07-12
申请号：US12397834
申请日：2009-03-04
申请人： Howard P. Ng , Danny P. C. McGee , Guoxian Wu , Jimmie Moore , Zhi-Hong Li , Sanjeev Gangwar , Oliver L. Saunders , Irina Astafieva
发明人： Howard P. Ng , Danny P. C. McGee , Guoxian Wu , Jimmie Moore , Zhi-Hong Li , Sanjeev Gangwar , Oliver L. Saunders , Irina Astafieva
IPC分类号： C07K16/00 , C12P21/08 , C07D487/02
CPC分类号： C07D405/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D405/14 , C07D487/04 , C07D487/10 , C07F7/1804 , C07F9/6561
摘要： The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
摘要翻译： 本发明提供了作为有效的细胞毒素的杜卡霉素的类似物。 还提供了在体内被切割的肽基和二硫键接头。 连接体可用于形成本发明的细胞毒素的前药和缀合物以及其它诊断和治疗部分。 本发明提供了杜卡霉素类似物与本发明的连接臂的前药和缀合物。
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公开(公告)号：US08034959B2
公开(公告)日：2011-10-11
申请号：US12396266
申请日：2009-03-02
申请人： Howard P. Ng , Zhi-Hong Li , Danny P. C. McGee , Oliver L. Saunders , Guoxian Wu , David John King , Valeri Martichonok , Sharon Elaine Boyd , Thomas J. Lobl
发明人： Howard P. Ng , Zhi-Hong Li , Danny P. C. McGee , Oliver L. Saunders , Guoxian Wu , David John King , Valeri Martichonok , Sharon Elaine Boyd , Thomas J. Lobl
IPC分类号： C07D487/02 , A61K39/00
CPC分类号： C07D405/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12 , C07D405/14 , C07D487/04 , C07D487/10 , C07F7/1804 , C07F9/6561
摘要： The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
摘要翻译： 本发明提供了作为有效的细胞毒素的杜卡霉素的类似物。 还提供了在体内被切割的肽基和二硫键接头。 连接体可用于形成本发明的细胞毒素的前药和缀合物以及其它诊断和治疗部分。 本发明提供了杜卡霉素类似物与本发明的连接臂的前药和缀合物。
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