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公开(公告)号：US20130137139A1
公开(公告)日：2013-05-30
申请号：US13814336
申请日：2011-08-05
申请人： Iontcho Radoslavov Vlahov , Michael Groaning , Paul Joseph Kleindl , Hari Krishna R. Santhapuram , Fei You , Kevin Yu Wang , Le-Cun Xu , Katheryn Marie Stanford , Allen Ritter , Paul Christopher Leamon
发明人： Iontcho Radoslavov Vlahov , Michael Groaning , Paul Joseph Kleindl , Hari Krishna R. Santhapuram , Fei You , Kevin Yu Wang , Le-Cun Xu , Katheryn Marie Stanford , Allen Ritter , Paul Christopher Leamon
IPC分类号： C07K5/02
CPC分类号： C12P21/00 , A61K31/445 , C07D417/12 , C07K5/02 , C07K5/021
摘要： Tubulysins are a series of naturally occurring cytotoxic agents that are of interest as anticancer therapeutic agents. Processes and intermediates useful for preparing naturally occurring and non-naturally occurring tubulysins and analogs and derivatives thereof are described.
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公开(公告)号：US08889880B2
公开(公告)日：2014-11-18
申请号：US13814336
申请日：2011-08-05
申请人： Iontcho Radoslavov Vlahov , Michael Groaning , Paul Joseph Kleindl , Hari Krishna R. Santhapuram , Fei You , Kevin Yu Wang , Le-Cun Xu , Katheryn Marie Stanford , Allen Ritter , Christopher Paul Leamon
发明人： Iontcho Radoslavov Vlahov , Michael Groaning , Paul Joseph Kleindl , Hari Krishna R. Santhapuram , Fei You , Kevin Yu Wang , Le-Cun Xu , Katheryn Marie Stanford , Allen Ritter , Christopher Paul Leamon
IPC分类号： A61K31/425 , C07D277/04 , C07K5/02 , A61K31/445 , C07D417/12
CPC分类号： C12P21/00 , A61K31/445 , C07D417/12 , C07K5/02 , C07K5/021
摘要： Tubulysins are a series of naturally occurring cytotoxic agents that are of interest as anticancer therapeutic agents. Processes and intermediates useful for preparing naturally occurring and non-naturally occurring tubulysins and analogs and derivatives thereof are described.
摘要翻译： Tubulysins是一系列作为抗癌治疗剂感兴趣的天然存在的细胞毒性剂。 描述了可用于制备天然存在和非天然存在的管状体及其类似物及其衍生物的方法和中间体。
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公开(公告)号：US20100323973A1
公开(公告)日：2010-12-23
申请号：US12666712
申请日：2008-06-25
申请人： Christopher Paul Leamon , Iontcho Radoslavov Vlahov , Hari Krishna R. Santhapuram , Paul Joseph Kleindl , Yu Wang , Fei You
发明人： Christopher Paul Leamon , Iontcho Radoslavov Vlahov , Hari Krishna R. Santhapuram , Paul Joseph Kleindl , Yu Wang , Fei You
IPC分类号： A61K38/14 , C07K5/093 , A61K38/06 , A61K38/08 , A61P35/00 , C07K7/06 , C07K7/64 , A61K38/12 , C07K9/00 , A61P31/04 , A61P31/12 , A61P31/10 , A61P33/10 , A61P33/04 , A61P33/02
CPC分类号： C07K9/003 , A61K47/555 , A61K47/60 , A61K47/65 , C07H15/24
摘要： Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.
摘要翻译： 本文描述了使用含有用于成像，诊断和/或治疗由致病细胞群体引起的疾病和疾病状态的亲水性间隔物接头的细胞受体结合药物递送缀合物用于靶向药物递送的组合物和方法。
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公开(公告)号：US09138484B2
公开(公告)日：2015-09-22
申请号：US12666712
申请日：2008-06-25
申请人： Christopher Paul Leamon , Iontcho Radoslavov Vlahov , Hari Krishna R. Santhapuram , Paul Joseph Kleindl , Yu Wang , Fei You
发明人： Christopher Paul Leamon , Iontcho Radoslavov Vlahov , Hari Krishna R. Santhapuram , Paul Joseph Kleindl , Yu Wang , Fei You
IPC分类号： C07D239/95 , C07D519/04 , A61K47/48
CPC分类号： C07K9/003 , A61K47/555 , A61K47/60 , A61K47/65 , C07H15/24
摘要： Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.
摘要翻译： 本文描述了使用含有用于成像，诊断和/或治疗由致病细胞群体引起的疾病和疾病状态的亲水性间隔物接头的细胞受体结合药物递送缀合物用于靶向药物递送的组合物和方法。
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公开(公告)号：US20130065841A1
公开(公告)日：2013-03-14
申请号：US13698215
申请日：2011-05-19
CPC分类号： C07K7/02 , A61K47/551
摘要： The invention described herein pertains to an improved process for preparing the folate-targeted conjugate EC 145 and to the conjugate EC 145 prepared using the improved process, as well as to a pharmaceutical composition comprising the conjugate EC 145 prepared using the improved process.
摘要翻译： 本文描述的本发明涉及用于制备叶酸靶向缀合物EC 145和使用改进方法制备的缀合物EC 145的改进方法，以及包含使用改进方法制备的缀合物EC 145的药物组合物。
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公开(公告)号：US08044200B2
公开(公告)日：2011-10-25
申请号：US11908695
申请日：2006-03-14
申请人： Le-Cun Xu , Iontcho Radoslavov Vlahov , Christopher Paul Leamon , Hari Krishna Santhapuram , Chunhong Li
发明人： Le-Cun Xu , Iontcho Radoslavov Vlahov , Christopher Paul Leamon , Hari Krishna Santhapuram , Chunhong Li
IPC分类号： C07D475/04 , A61P35/00
CPC分类号： C07D475/08
摘要： Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and folic acid analogs are also described. Purified forms of pteroic acid, derivatives and analogs of pteroic acid, and conjugates thereof are also described.
摘要翻译： 描述了纯化庚酸的方法，辛酸的类似物和辛酸的衍生物。 还描述了合成和纯化维生素的缀合物的方法，包括叶酸，叶酸类似物的FITC缀合物和叶酸和叶酸类似物的衍生物。 还描述了蝶啶酸，庚酸的衍生物和类似物及其共轭物的纯化形式。
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公开(公告)号：US20080207625A1
公开(公告)日：2008-08-28
申请号：US11908695
申请日：2006-03-14
申请人： Le-Cun Xu , Iontcho Radoslavov Vlahov , Christopher Paul Leamon , Hari Krishna Santhapuram , Chunhong Li
发明人： Le-Cun Xu , Iontcho Radoslavov Vlahov , Christopher Paul Leamon , Hari Krishna Santhapuram , Chunhong Li
IPC分类号： A61K31/502 , C07D475/00 , A61P43/00 , B01D15/08
CPC分类号： C07D475/08
摘要： Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and folic acid analogs are also described. Purified forms of pteroic acid, derivatives and analogs of pteroic acid, and conjugates thereof are also described.
摘要翻译： 描述了纯化庚酸的方法，辛酸的类似物和辛酸的衍生物。 还描述了合成和纯化维生素的缀合物的方法，包括叶酸，叶酸类似物的FITC缀合物，以及叶酸和叶酸类似物的衍生物。 还描述了蝶啶酸，庚酸的衍生物和类似物及其共轭物的纯化形式。
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公开(公告)号：US20120022245A1
公开(公告)日：2012-01-26
申请号：US13124408
申请日：2009-10-16
申请人： Philip Stewart Low , Mini Thomas , Christopher Paul Leamon , Iontcho Radoslavov Vlahov , Paul Joseph Kleindl , Longwu Qi
发明人： Philip Stewart Low , Mini Thomas , Christopher Paul Leamon , Iontcho Radoslavov Vlahov , Paul Joseph Kleindl , Longwu Qi
CPC分类号： A61K31/70 , C12N15/111 , C12N2310/351 , C12N2320/32
摘要： The present invention relates to compounds, compositions, kits, and methods of use in targeting nucleotides, such as siRNA's, to cancer cells or to immune system cells involved in inflammation. More particularly, the invention is directed to receptor binding ligand-nucleotide delivery conjugates for use in specifically targeting the conjugates to cancer cells or to immune system cells, methods of treatment with these conjugates, methods of preparation of these conjugates, and methods of reducing the expression of a gene in vitro or in vivo with the conjugates described herein.
摘要翻译： 本发明涉及用于靶向核苷酸（例如siRNA）的癌细胞或涉及炎症的免疫系统细胞的化合物，组合物，试剂盒和方法。 更具体地，本发明涉及用于特异性靶向癌细胞或免疫系统细胞的缀合物的受体结合配体 - 核苷酸递送缀合物，用这些缀合物处理的方法，这些缀合物的制备方法和减少 用本文所述的缀合物在体外或体内表达基因。
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公开(公告)号：US20120270791A1
公开(公告)日：2012-10-25
申请号：US13440641
申请日：2012-04-05
CPC分类号： A61K51/04 , A61K47/551 , A61K47/552 , A61K49/0002 , A61K51/00 , C07D475/04 , C07D519/00 , C07K7/02
摘要： The invention relates to a method for diagnosing a kidney disease state. The method comprises the steps of administering to a patient a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises a diagnostic marker, and diagnosing the kidney disease state. The invention also relates to a method for treating a kidney disease state. The method comprises the steps of administering to a patient suffering from the disease state an effective amount of a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises an antigen, a cytotoxin, or a cell growth inhibitor, and eliminating the disease state.
摘要翻译： 本发明涉及诊断肾脏疾病状态的方法。 该方法包括以下步骤：向患者施用包含通式VLD的缀合物或复合物的组合物，其中组V包含结合肾近端小管细胞的维生素受体结合配体，D组包括诊断标记物，并诊断 肾脏疾病状态。 本发明还涉及治疗肾脏疾病状态的方法。 该方法包括以下步骤：向患有疾病状态的患者施用有效量的包含通式VLD的缀合物或复合物的组合物，其中组V包含结合肾近端小管细胞的维生素受体结合配体， D组包含抗原，细胞毒素或细胞生长抑制剂，并消除疾病状态。
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公开(公告)号：US20110172254A1
公开(公告)日：2011-07-14
申请号：US13063889
申请日：2009-09-17
IPC分类号： A61K31/519 , A61K31/517 , C07D471/04 , C07D239/72 , A61P35/00
CPC分类号： A61K47/48338 , A61K31/475 , A61K31/517 , A61K47/55 , A61K47/551 , C07D487/04
摘要： Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.
摘要翻译： 描述了抗叶酸剂，可释放接头和药物的结合物，以及含有它们的药物组合物。 缀合物可用于治疗由致病细胞群体引起的疾病。 还描述了治疗这些疾病的方法。
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