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公开(公告)号：US5616692A
公开(公告)日：1997-04-01
申请号：US436961
申请日：1995-05-08
申请人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
发明人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
IPC分类号： A61K51/04 , A61K51/08 , A61K51/10 , C07B59/00 , C07F13/00 , G01N33/534 , C07K5/08 , A61K39/385 , C07K17/00
CPC分类号： G01N33/534 , A61K51/0478 , A61K51/088 , A61K51/1066 , A61K51/1093 , C07B59/004 , C07F13/005 , A61K2121/00 , A61K2123/00
摘要： Chelated radionuclide compositions are provided for conjugation to polypeptides and carbohydrates. The resulting conjugates may be used in diagnosis and therapy.
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公开(公告)号：US5399710A
公开(公告)日：1995-03-21
申请号：US994939
申请日：1992-12-22
IPC分类号： A61K51/10 , C07C319/18 , C07C323/52 , C07D307/60 , C07D339/06 , C07D495/04 , C07D487/04 , C07D207/38 , C07C101/04
CPC分类号： C07D495/04 , A61K51/1093 , C07C319/18 , C07D307/60 , C07D339/06 , A61K2123/00 , Y02P20/55
摘要： Novel labeling reagents are useful for radiolabeling proteins such as antibodies with radionuclide metals such as .sup.99m Tc, .sup.186 Re, and .sup.188 Re. The reagents are of the following formula: ##STR1## wherein: each X is independently chosen from O, S, NH, or NR.sub.2, wherein R.sub.2 is a protecting group or an electron withdrawing group;R.sub.1 represents a protecting group, wherein each R.sub.1 is a separate protecting group or the two R.sub.1 symbols are taken together to represent a single protecting group; andeach T is independently chosen from hydrogen, lower alkyl groups of from 1 to about 6 carbon atoms, electron withdrawing groups, and lower alkyl groups of from 1 to about 6 carbon atoms substituted with electron withdrawing group(s).
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13.发明授权Metal-radionuclide-labeled proteins and glycoproteins for diagnosis and therapy 失效用于诊断和治疗的金属放射性核素标记的蛋白质和糖蛋白
公开(公告)号：US5091514A
公开(公告)日：1992-02-25
申请号：US494191
申请日：1990-03-15
申请人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
发明人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
CPC分类号： G01N33/534 , A61K51/0478 , A61K51/088 , A61K51/1066 , A61K51/1093 , C07B59/004 , C07F13/005 , A61K2121/00 , A61K2123/00
摘要： Chelated radionuclide compositions are provided for conjugation to polypeptides and carbohydrates. The resulting conjugates may be used in diagnosis and therapy.
摘要翻译： 螯合放射性核素组合物用于与多肽和碳水化合物结合。 所得到的缀合物可用于诊断和治疗。
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公开(公告)号：US4897255A
公开(公告)日：1990-01-30
申请号：US65011
申请日：1987-06-19
IPC分类号： A61K51/04 , A61K51/10 , A61K51/12 , C07C227/08 , C07C271/22
CPC分类号： C07C271/22 , A61K51/0478 , A61K51/1093 , A61K51/12 , B82Y5/00 , C07C227/08 , A61K2123/00 , Y10S530/866
摘要： Protein conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the polypeptide compositions efficiently.
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公开(公告)号：US5037630A
公开(公告)日：1991-08-06
申请号：US423180
申请日：1989-10-18
IPC分类号： A61K51/04 , A61K51/10 , A61K51/12 , C07C227/08 , C07C271/22
CPC分类号： C07C271/22 , A61K51/0478 , A61K51/1093 , A61K51/12 , B82Y5/00 , C07C227/08 , A61K2123/00 , Y10S530/866
摘要： Protein conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the polypeptide compositions efficiently.
摘要翻译： 提供蛋白质共轭螯合金属放射性核素用于体内。 提供中间体有效地制备多肽组合物。
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公开(公告)号：US4965392A
公开(公告)日：1990-10-23
申请号：US172004
申请日：1988-03-23
申请人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
发明人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
CPC分类号： G01N33/534 , A61K51/0478 , A61K51/1066 , A61K51/1093 , C07B59/004 , C07F13/005 , C07K5/0819 , A61K2121/00 , A61K2123/00
摘要： Chelated radionuclide compositions are provided for conjugation to polypeptides and carbohydrates. The resulting conjugates may be used in diagnosis and therapy. Chelating compounds are disclosed.
摘要翻译： 螯合放射性核素组合物用于与多肽和碳水化合物结合。 所得到的缀合物可用于诊断和治疗。 公开了螯合化合物。
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公开(公告)号：US5202451A
公开(公告)日：1993-04-13
申请号：US157284
申请日：1988-02-17
IPC分类号： A61K51/00 , A61K51/04 , A61K51/10 , C07C313/28 , C07C323/25 , C07C323/41 , C07C323/60 , C07C331/28 , C07K1/113 , C07K5/06 , C07K14/00 , C07K16/00 , C09K3/00 , G01N33/534 , G01N33/60
CPC分类号： G01N33/534 , A61K51/0478 , A61K51/1093 , C07C313/28 , C07C331/28 , A61K2123/00
摘要： Anchimeric chelates are disclosed which are capable of rapidly forming stable chelates with radionuclide metals at or below physiological temperature. Bifunctional anchimeric chelates having these same properties are also disclosed which are useful for radiolabeling target specific molecules such as monoclonal antibodies and fragments thereof.
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公开(公告)号：US5606028A
公开(公告)日：1997-02-25
申请号：US532041
申请日：1995-09-21
IPC分类号： A61K51/00 , A61K51/04 , A61K51/10 , C07C313/28 , C07C323/25 , C07C323/41 , C07C323/60 , C07C331/28 , C07K1/113 , C07K5/06 , C07K14/00 , C07K16/00 , C09K3/00 , G01N33/534 , G01N33/60 , C07K17/02 , A61K51/08
CPC分类号： G01N33/534 , A61K51/0478 , A61K51/1093 , C07C313/28 , C07C331/28 , A61K2123/00
摘要： Anchimeric chelates are disclosed which are capable of rapidly forming stable chelates with radionuclide metals at or below physiological temperature. Bifunctional anchimeric chelates having these same properties are also disclosed which are useful for radiolabeling target specific molecules such as monoclonal antibodies and fragments thereof.
摘要翻译： 公开了能够在或低于生理温度下用放射性核素金属快速形成稳定的螯合物的嵌合螯合物。 还公开了具有这些相同特性的双功能锚定螯合物，其可用于放射性标记靶特异性分子，例如单克隆抗体及其片段。
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公开(公告)号：US5059541A
公开(公告)日：1991-10-22
申请号：US187714
申请日：1988-04-29
IPC分类号： A61K51/10
CPC分类号： A61K51/1093 , A61K2123/00 , Y10S436/804 , Y10S436/819
摘要： There is disclosed a process for minimally derivatizing a targeting protein with a radionuclide such that the predominant species of derivatized targeting protein contains one radionuclide group as a single radiolabeled ligand, and whereby the binding characteristics of the targeting protein are minimally affected. There is further disclosed ligands that can chelate a metal radionuclide or bind a halogen radionuclide while providing a means for separating radiolabeled ligand from unradiolabeled ligand.
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20.发明授权
公开(公告)号：US4988496A
公开(公告)日：1991-01-29
申请号：US201134
申请日：1988-05-31
IPC分类号： A61K47/48 , A61K51/10 , C07C327/30 , C07C327/32 , C07D207/46 , C07D209/48 , C07D307/18 , C07D405/12
CPC分类号： C07D209/48 , A61K47/48707 , A61K51/1093 , C07C327/30 , C07C327/32 , C07D207/46 , C07D307/18 , C07D405/12 , A61K2121/00 , A61K2123/00
摘要： The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.Another aspect of the invention provides kits for producing chelate-targeting agent comjugates for radiopharmaceutical use.An additional aspect of the invention provides methods for using the chelate-targeting agent conjugates for diagnostic and therapeutic purposes, such as detection of a target site and delivery of a radionuclide to the site, respectively.
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