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51.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：US5681927A
公开(公告)日：1997-10-28
申请号：US075305
申请日：1993-06-11
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 , C07K5/093 , G01N33/534 , C07K5/08 , A61K39/44 , C07K17/06
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.
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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52.发明授权Stable therapeutic radionuclide compositions and methods for preparation thereof 失效稳定的治疗放射性核素组合物及其制备方法
公开(公告)号：US5679318A
公开(公告)日：1997-10-21
申请号：US342838
申请日：1994-11-21
IPC分类号： A61K51/04 , A61K51/10 , A61K51/12 , C07C227/08 , C07C271/22 , A61K51/00
CPC分类号： C07C271/22 , A61K51/0478 , A61K51/1093 , A61K51/12 , B82Y5/00 , C07C227/08 , A61K2123/00 , Y10S530/866
摘要： Stable therapeutic radionuclide compositions comprising, for example, .sup.186 Re, .sup.188 Re and .sup.131 I stably bound to a proteinaceous targeting moiety and suitable for human in vivo administration are disclosed. Stabilizing agents preferably comprise antioxidants and challenging agents, and combination of HSA with an antioxidant and/or challenging agent provides enhanced long term stability. Ascorbic acid is an especially preferred stabilizing agent, which provides stability of therapeutic radionuclide compositions at levels of at least about 90% for several hours up to several days.
摘要翻译： 公开了稳定的治疗放射性核素组合物，其包含例如稳定结合蛋白质靶向部分并适于人体内施用的186Re，188Re和131I。 稳定剂优选包含抗氧化剂和挑战性试剂，并且HSA与抗氧化剂和/或挑战性试剂的组合提供增强的长期稳定性。 抗坏血酸是一种特别优选的稳定剂，其在至少约90％的水平下提供几个小时至几天的治疗性放射性核素组合物的稳定性。
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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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55.发明授权Covalently-linked complexes and methods for enhanced cytotoxicity and imaging 失效共价连接的复合物和增强细胞毒性和成像的方法
公开(公告)号：US5169933A
公开(公告)日：1992-12-08
申请号：US390241
申请日：1989-08-07
申请人： David C. Anderson , A. Charles Morgan, Jr. , Paul G. Abrams , Alan R. Fritzberg , Everett J. Nichols
发明人： David C. Anderson , A. Charles Morgan, Jr. , Paul G. Abrams , Alan R. Fritzberg , Everett J. Nichols
IPC分类号： A61K47/48 , A61K51/10 , C07K14/415 , C12N15/62
CPC分类号： C07K14/415 , A61K47/48238 , A61K51/1093 , A61K51/1096 , C12N15/62 , A61K2123/00 , C07K2319/00 , C07K2319/10 , C07K2319/55
摘要： Covalently-linked complexes (CLCs) for targeting a defined population of cells, comprising a targeting protein; a cytotoxic agent; and an enhancing moiety, wherein the enhancing moiety is capable of promoting CLC-target cell interaction are disclosed. Methods for using the claimed CLCs to obtain enhanced in vivo cytotoxicity and enhanced in vivo imaging are also described.
摘要翻译： 用于靶向定义的细胞群的共价连接复合物（CLC），其包含靶向蛋白; 细胞毒性剂 和增强部分，其中增强部分能够促进CLC靶细胞相互作用。 还描述了使用所要求保护的CLC以获得增强的体内细胞毒性和增强的体内成像的方法。
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公开(公告)号：US5106951A
公开(公告)日：1992-04-21
申请号：US332610
申请日：1989-03-31
申请人： Alton C. Morgan, Jr. , Ananthachari Srinivasan , John M. Reno , Alan R. Fritzberg , David C. Anderson
发明人： Alton C. Morgan, Jr. , Ananthachari Srinivasan , John M. Reno , Alan R. Fritzberg , David C. Anderson
IPC分类号： A61K31/495 , A61K31/505 , A61K31/675 , A61K31/70 , A61K39/395 , A61K47/48 , A61P35/00 , C07K14/00 , C07K16/00
CPC分类号： A61K47/48369 , A61K47/48384
摘要： There is disclosed an antibody and antibody-drug conjugate for targeting drug delivery as well as a class of chemicals, termed a drug-binding molecule of complementary structure (csDBM). The csDBM is designed to "fit" the drug by combining multiple non-covalent interactions between functional groups on the drug and opposing functional groups on the csDBM. The net result on the antibody-csDBM-drug conjugate is a drug stably bound to the csDBM so as not to dissociate during in vivo administration, but not so tightly bound to allow drug dissociation from the conjugate without significant loss of activity and retaining the drug's ability to bind to a higher affinity site on or within the target cell.
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57.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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