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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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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：US20100240701A1
公开(公告)日：2010-09-23
申请号：US12739579
申请日：2008-10-23
IPC分类号： A61K31/4545 , C07D417/12 , A61K31/454 , C07D417/14 , A61P31/12
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：US09555139B2
公开(公告)日：2017-01-31
申请号：US12530952
申请日：2008-03-13
CPC分类号： C07K7/06 , A61K47/55 , A61K47/551 , A61K47/64 , A61K47/65 , A61K47/6811 , A61K51/0497 , C07K5/021 , C07K5/06078
摘要： Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations. The compounds described herein include conjugates of tubulysins and vitamin receptor binding ligands. 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。 本文所述的化合物包括管状蛋白和维生素受体结合配体的缀合物。 缀合物还包括可释放的二价连接体。
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公开(公告)号：US09192682B2
公开(公告)日：2015-11-24
申请号：US14010122
申请日：2013-08-26
IPC分类号： C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00 , A61K47/48 , C07D487/04 , A61K31/517
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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