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公开(公告)号：US5886143A
公开(公告)日：1999-03-23
申请号：US351651
申请日：1994-12-07
IPC分类号： A61K31/7028 , A61K47/48 , A61K51/08 , A61P1/16 , C07H15/04 , C07H15/14 , C07H15/26 , A61K38/14 , C07H15/02 , C07K9/00
CPC分类号： B82Y5/00 , A61K47/4873 , A61K51/0465 , C07H15/04 , C07H15/14 , A61K2121/00
摘要： Hepatic-directed compounds, reagents useful in making such compounds and associated methods and compositions are discussed. Hepatic-directed compounds are processed by metabolic mechanisms, which generally differ in degree or in kind from the metabolic mechanisms encountered by compounds which are not so directed. Reagents useful in the preparation of hepatic-directed compounds include a hexose cluster characterized by multiple hexose residues connected in an iteratively branched configuration. In one embodiment, the hexose cluster comprises at least four hexose residues with each branch of the configuration having two prongs. In another embodiment, the hexose cluster comprises at least nine hexose residues with each branch of the configuration having three prongs.
摘要翻译： 讨论了肝取向化合物，可用于制备这些化合物的试剂和相关方法和组合物。 肝取向化合物通过代谢机制进行处理，其代谢机制通常在程度上或种类上不同于未被引导的化合物所遇到的代谢机制。 可用于制备肝取向化合物的试剂包括以反复分支构型连接的多个己糖残基为特征的己糖簇。 在一个实施方案中，己糖簇包含至少四个己糖残基，其中每个分支具有两个分支。 在另一个实施方案中，己糖簇包含至少九个己糖残基，其中每个分支具有三个分支。
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公开(公告)号：US5616690A
公开(公告)日：1997-04-01
申请号：US133613
申请日：1993-10-08
申请人： Donald B. Axworthy , John M. Reno
发明人： Donald B. Axworthy , John M. Reno
IPC分类号： A61K47/48 , A61K51/04 , A61K51/12 , C07K14/765 , C07D235/02 , C07K1/107
CPC分类号： A61K47/48023 , A61K47/48146 , A61K47/48353 , A61K47/48707 , A61K47/4873 , A61K47/48746 , A61K47/48753 , A61K51/0497 , A61K51/1268 , B82Y5/00 , A61K2121/00 , A61K2123/00
摘要： Novel clearing agents comprising hexose derivatized human serum albumin and ligand molecule(s) are provided. These clearing agents are useful in pretargeting methods to clear previously administered anti-ligand containing conjugates. Preferably, the hexose is mannose or galactose and the ligand and anti-ligand are respectively biotin and avidin or streptavidin.
摘要翻译： 提供了包含己糖衍生的人血清白蛋白和配体分子的新型清除剂。 这些清除剂可用于预先靶向的方法以清除先前施用的含有抗配体的缀合物。 优选地，己糖是甘露糖或半乳糖，配体和抗配体分别是生物素和抗生物素蛋白或链霉亲和素。
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公开(公告)号：US5283342A
公开(公告)日：1994-02-01
申请号：US895588
申请日：1992-06-09
申请人： Linda M. Gustavson , Ananthachari Srinivasan , Alan R. Fritzberg , John M. Reno , Donald B. Axworthy
发明人： Linda M. Gustavson , Ananthachari Srinivasan , Alan R. Fritzberg , John M. Reno , Donald B. Axworthy
IPC分类号： A61K47/48 , A61K51/04 , A61K51/12 , A61K43/00 , A61K49/02 , C07D235/00 , C07D495/04
CPC分类号： B82Y5/00 , A61K47/48146 , A61K47/48353 , A61K47/48707 , A61K47/4873 , A61K47/48753 , A61K51/0497 , A61K51/1268 , A61K2121/00 , A61K2123/00 , Y10S436/804 , Y10S436/808
摘要： Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin and for improved radiohalogenation of biotin, as well as related compounds, are described.
摘要翻译： 公开了与诊断和治疗剂的预靶向递送相关的方法，化合物，组合物和试剂盒。 特别地，描述了用于生物素的放射性金属标记和改善生物素的放射性卤化的方法以及相关化合物。
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公开(公告)号：US06172045B2
公开(公告)日：2001-01-09
申请号：US08659761
申请日：1996-06-06
IPC分类号： A01N4304
CPC分类号： B82Y5/00 , A61K47/557 , A61K47/6893 , A61K47/6898 , A61K51/1268
摘要： Cluster clearing agents (CCAs) and the use thereof are discussed. CCAs are composed of a hepatic clearance directing moiety which directs the biodistribution of a CCA-containing construct to hepatic clearance; and a binding moiety which mediates binding of the CCA to a compound for which rapid hepatic clearance is desired.
摘要翻译： 讨论了群集清除代理（CCAs）及其使用。 CCA由肝间隙导向部分组成，其指导含CCA构建体的生物分布为肝脏清除; 以及介导CCA与需要快速肝清除的化合物的结合的结合部分。
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公开(公告)号：US5624896A
公开(公告)日：1997-04-29
申请号：US462765
申请日：1995-06-05
申请人： Donald B. Axworthy , John M. Reno
发明人： Donald B. Axworthy , John M. Reno
IPC分类号： A61K47/48 , A61K51/12 , A61K38/38 , C07D235/02
CPC分类号： B82Y5/00 , A61K47/48146 , A61K47/48353 , A61K47/48707 , A61K47/4873 , A61K47/48746 , A61K47/48753 , A61K51/1268
摘要： Novel clearing agents are provided which comprise biotin analog containing clearance-directing moieties. Preferably such clearance-directing moieties endogenously contain or a rederivatized to expose galactose and/or mannose residues.
摘要翻译： 提供了包含含有间隙导向部分的生物素类似物的新型清除剂。 优选地，这种间隙指导部分内源性地含有或被递归化以暴露半乳糖和/或甘露糖残基。
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公开(公告)号：US6075010A
公开(公告)日：2000-06-13
申请号：US350551
申请日：1994-12-07
CPC分类号： C07D495/04 , A61K47/48146 , A61K47/48353 , A61K47/48369 , A61K47/48707 , A61K47/4873 , A61K47/48746 , A61K47/48753 , A61K51/0497 , A61K51/1268 , B82Y5/00 , A61K2121/00 , A61K2123/00
摘要： Small molecule weight clearing agents containing ligands such as biotin or biotin analogs and hexose residue, in particular galactose or N-acetyl galactosamine residues are taught. These clearing agents effectively clear anti-ligand containing conjugates in vivo via hepatocyte receptor mediated clearance mechanisms.
摘要翻译： 教导了含有配体例如生物素或生物素类似物和己糖残基，特别是半乳糖或N-乙酰半乳糖胺残基的小分子量清除剂。 这些清除剂通过肝细胞受体介导的清除机制在体内有效地清除含有配体的缀合物。
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7.发明授权Pretargeting protocols for the enhanced localization of cytotoxins to target sites and cytotoxic combinations useful therefore 失效用于增强细胞毒素定位到靶位点和细胞毒性组合的预靶向方案因此有用
公开(公告)号：US5976535A
公开(公告)日：1999-11-02
申请号：US468513
申请日：1995-06-06
申请人： Alan R. Fritzberg , Paul G. Abrams , John M. Reno , Donald B. Axworthy , Scott S. Graves , Sudhakar Kasina
发明人： Alan R. Fritzberg , Paul G. Abrams , John M. Reno , Donald B. Axworthy , Scott S. Graves , Sudhakar Kasina
IPC分类号： A61K38/00 , A61K47/48 , A61K48/00 , A61K51/04 , A61K51/10 , A61K51/12 , C07F13/00 , C07K14/765 , C07K16/30 , C12N15/87 , A61K45/05
CPC分类号： B82Y5/00 , A61K47/48146 , A61K47/48353 , A61K47/48369 , A61K47/48569 , A61K47/48707 , A61K47/4873 , A61K47/48746 , A61K47/48753 , A61K48/00 , A61K51/0497 , A61K51/1093 , A61K51/1268 , C07F13/005 , C07K14/765 , C07K16/30 , C12N15/87 , A61K2039/505 , A61K2121/00 , A61K2123/00 , A61K38/00 , C07K2317/77
摘要： Methods for targeting cytotoxins to target sites by administration of a combination of conjugates are provided. Novel cytotoxic combinations for use in such methods are also provided.
摘要翻译： 提供了通过给予缀合物的组合将细胞毒素靶向靶位点的方法。 还提供了用于这些方法的新型细胞毒素组合。
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公开(公告)号：US5955605A
公开(公告)日：1999-09-21
申请号：US695940
申请日：1996-08-12
IPC分类号： A61K51/04 , C07D495/04 , C07H7/033 , C07D257/02 , A61K31/415 , C07H17/04
CPC分类号： C07D495/04 , A61K51/0497 , C07H7/033
摘要： Biotinidase-resistant biotin-DOTA conjugates, and methods of use thereof in diagnostic and therapeutic pretargeting methods are provided. These conjugates are useful in diagnosis and treatment of cancer.
摘要翻译： 提供了生物素抗性生物素-DTOTA缀合物及其在诊断和治疗预靶向方法中的应用方法。 这些缀合物可用于诊断和治疗癌症。
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公开(公告)号：US06416738B1
公开(公告)日：2002-07-09
申请号：US09561736
申请日：2000-04-25
IPC分类号： A61K4900
CPC分类号： B82Y5/00 , A61K47/557 , A61K47/665 , A61K47/6887 , A61K47/6893 , A61K47/6898 , A61K51/0497 , A61K51/1268 , A61K2121/00 , A61K2123/00
摘要： Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin, as well as related compounds, are described. Clearing agents and clearance mechanisms are also discussed.
摘要翻译： 公开了与诊断和治疗剂的预靶向递送相关的方法，化合物，组合物和试剂盒。 特别地，描述了用于生物素的放射性标记的方法以及相关的化合物。 还讨论了清理机构和清理机制。
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10.发明授权Pretargeting protocols for enhanced localization of active agents to target sites 失效预定位协议，用于增强活动代理到目标站点的本地化
公开(公告)号：US5911969A
公开(公告)日：1999-06-15
申请号：US329617
申请日：1994-10-26
CPC分类号： B82Y5/00 , A61K47/48146 , A61K47/48353 , A61K47/48369 , A61K47/48707 , A61K47/4873 , A61K47/48753 , A61K51/0497 , A61K51/1268 , A61K2121/00 , A61K2123/00 , Y10S530/825
摘要： Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin and for improved radiohalogenation of biotin, as well as related compounds, are described. Also, clearing agents, anti-ligand-targeting moiety conjugates, target cell retention enhancing moieties and additional methods are discussed.
摘要翻译： 公开了涉及诊断和治疗剂的预靶向递送的方法，化合物，组合物和试剂盒。 特别地，描述了用于生物素的放射性金属标记和改善生物素的放射性卤化的方法以及相关化合物。 此外，讨论了清除剂，抗配体靶向部分缀合物，靶细胞保留增强部分和另外的方法。
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