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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：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：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：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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公开(公告)号：US08546425B2
公开(公告)日：2013-10-01
申请号：US13063889
申请日：2009-09-17
IPC分类号： A01N43/90 , A61K31/44 , C07D239/72
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.
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公开(公告)号：US09187521B2
公开(公告)日：2015-11-17
申请号：US12739579
申请日：2008-10-23
IPC分类号： A61K31/445 , C07K5/02
CPC分类号： C07K5/021 , C07K5/06139
摘要： Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.
摘要翻译： 描述了制备肾上腺素的方法。 这些方法可用于制备预混合的肾上腺素的混合物，由tubulininins混合物制备单一的tubulinins，并将一种tubulyin转化成不同的tubulysin。 本文所述的管状体素可用于治疗包括致病细胞群体的疾病和疾病状态。
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公开(公告)号：US20130116195A1
公开(公告)日：2013-05-09
申请号：US13507076
申请日：2012-06-01
IPC分类号： A61K38/08
CPC分类号： A61K38/08 , A61K47/551 , A61K47/595
摘要： Described herein are compounds, pharmaceutical compositions, and methods for treating pathogenic cell populations. Kits including the compounds or pharmaceutical compositions are described. The compounds described herein include conjugates of tubulysins and folates. The conjugates also include a releasable bivalent linker.
摘要翻译： 本文描述了用于治疗致病细胞群体的化合物，药物组合物和方法。 描述了包括化合物或药物组合物的试剂盒。 本文所述的化合物包括肾上腺素和叶酸盐的缀合物。 缀合物还包括可释放的二价连接体。
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公开(公告)号：US08288557B2
公开(公告)日：2012-10-16
申请号：US11632895
申请日：2005-07-22
IPC分类号： C07D213/64 , C07D249/18
CPC分类号： C07D213/71 , A61K47/551 , A61K47/6803 , A61K49/0002 , C07D401/12 , C07D475/04
摘要： Bivalent linkers derived from compounds of formulae (V), (VI), and (VII), where X1 and X2 are leaving groups and the other variables are as defined in the claims, to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.
摘要翻译： 衍生自式（V），（VI）和（VII）的化合物的二价连接体，其中X1和X2是离去基团，其它变量如权利要求中所定义，被包括在维生素，药物，诊断中 试剂和/或成像剂共轭物。
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