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31. 发明授权

US4980147A Radiolabeled technetium chelates for use in renal function determinations 失效
标题翻译：放射性标记的锝螯合物用于肾功能测定
公开(公告)号：US4980147A
公开(公告)日：1990-12-25
申请号：US733481
申请日：1985-05-14
申请人： Alan Fritzberg , Sudhakar Kasina , Dennis L. Johnson
发明人： Alan Fritzberg , Sudhakar Kasina , Dennis L. Johnson
IPC分类号： A61K51/00 , A61K51/08 , C07C233/56 , C07C237/22 , C07C309/15 , C07C311/45 , C07C323/60 , C07F13/00 , C07K5/02
CPC分类号： C07C233/56 , A61K51/0478 , A61K51/08 , C07F13/005 , C07K5/0202 , A61K2123/00 , Y02P20/55
摘要： The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: ##STR1## wherein X is S or N; and wherein Y is--H or wherein Y is ##STR2## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof. Of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. ##STR3## where X and Y have the same definitions as above, and wherein Y' is --H.sub.2 when X is N, or wherein Y' is --H, or a suitable protective group such as --COCH.sub.3, --COC.sub.6 H.sub.5, --CH.sub.2 NHCOCH.sub.3, --COCF.sub.3, or --COCH.sub.2 OH when X is S. The present invention also provides methods for preparing and using the novel Tc-99m compounds.
摘要翻译：本发明涉及包含Tc-99m作为放射性标记的新型放射性药物显像剂。特别地，本文公开的新型成像剂具有相对高的肾提取效率，因此可用于进行肾功能成像过程。本发明的新型Tc-99m化合物具有以下通式：其中X为S或N; 并且其中Y是-H或其中Y是＆lt; IMAGE＆gt;其中R 1是-H，-CH 3或-CH 2 CH 3; R2是-H，-CH2CO2H，-CH2CONH2，-CH2CH2CO2H，-CH2CH2CONH2，-CH3，-CH2CH3，CH2C6H5或-CH2OH; Z是-H，-CO 2 H，-CONH 2，-SO 3 H，-SO 2 NH 2或-CONHCH 2 CO 2 H; Tc为Tc-99m; 及其水溶性盐。在上述中，本发明优选的Tc-99m化合物是Tc-99m-巯基乙酰基甘氨酰甘氨酰甘氨酸（Tc-99m-MAGGG）。本发明还涉及可与Tc-99m反应形成前述化合物的新型螯合剂。这种新型螯合剂具有以下通式。其中X和Y具有与上述相同的定义，并且其中当X是N时Y'是-H2，或其中Y'是-H，或合适的保护基如-COCH 3，-COC 6 H 5，-CH 2 NHCOCH 3， -COCF 3或-COCH 2 OH。本发明还提供了制备和使用新型Tc-99m化合物的方法。

32. 发明授权

US4965392A Chelating compounds for metal-radionuclide labeled proteins 失效
标题翻译：金属放射性核素标记蛋白质的螯合化合物
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
IPC分类号： A61K51/04 , A61K51/08 , A61K51/10 , C07B59/00 , C07F13/00 , C07K5/093 , G01N33/534
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。

33. 发明授权

US07744853B2 Radiolabeled annexins 失效
标题翻译：放射性标记的膜联蛋白
公开(公告)号：US07744853B2
公开(公告)日：2010-06-29
申请号：US11236272
申请日：2005-09-27
申请人： Sudhakar Kasina , John M. Reno , Alan R. Fritzberg , Jonathan Tait
发明人： Sudhakar Kasina , John M. Reno , Alan R. Fritzberg , Jonathan Tait
IPC分类号： A61K51/00 , C07F13/00 , C07K1/00 , C07H1/00
CPC分类号： C07K7/06 , A61K47/54 , A61K47/547 , A61K47/549 , A61K51/087 , A61K51/088 , A61K2123/00 , C07K1/13 , C07K14/4721
摘要： Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.
摘要翻译：描述了可用于成像血管血栓的放射性标记的膜联蛋白和修饰的膜联蛋白缀合物。还提供了制备和使用这种放射性标记的膜联蛋白缀合物的方法。

34. 发明授权

US07674886B2 Bridged aromatic substituted amine ligands with donor atoms 失效
标题翻译：具有供体原子的桥连的芳族取代的胺配体
公开(公告)号：US07674886B2
公开(公告)日：2010-03-09
申请号：US11849769
申请日：2007-09-04
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： A61K51/04
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.
摘要翻译：本发明提供了取代的金属螯合化合物，其中至少两个螯合原子是直接连接到芳环上的氮，并且一个或多个这些氮原子连接有除氢之外的取代基，以及制备和使用方法这些化合物。

35. 发明授权

US07268220B2 Bridged aromatic substituted amine ligands with donor atoms 失效
标题翻译：具有供体原子的桥连的芳族取代的胺配体
公开(公告)号：US07268220B2
公开(公告)日：2007-09-11
申请号：US11061110
申请日：2005-02-18
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： C07F13/00
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.
摘要翻译：本发明提供了取代的金属螯合化合物，其中至少两个螯合原子是直接连接到芳环上的氮，并且一个或多个这些氮原子连接有除氢之外的取代基，以及制备和使用方法这些化合物。

36. 发明授权

US07115248B2 Radiolabeled annexins 失效
公开(公告)号：US07115248B2
公开(公告)日：2006-10-03
申请号：US10820653
申请日：2004-04-08
申请人： Sudhakar Kasina , John M Reno , Louis J Theodore
发明人： Sudhakar Kasina , John M Reno , Louis J Theodore
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07K7/06 , A61K47/54 , A61K47/547 , A61K47/549 , A61K51/087 , A61K51/088 , A61K2123/00 , C07K1/13 , C07K14/4721
摘要： Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.

37. 发明申请

US20050276754A1 Bridged aromatic substituted amine ligands with donor atoms 失效
公开(公告)号：US20050276754A1
公开(公告)日：2005-12-15
申请号：US11061110
申请日：2005-02-18
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： A61K51/00 , A61K51/04 , A61K51/08 , A61P35/00 , C07C229/16 , C07C229/18 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F5/00 , C07F9/22 , C07F9/38 , C07F9/6524 , C07F9/6553 , C07F9/6561 , C07F13/00
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

38. 发明授权

US06528627B1 Bridged aromatic substituted amine ligands with donor atoms 失效
公开(公告)号：US06528627B1
公开(公告)日：2003-03-04
申请号：US09724834
申请日：2000-11-28
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： C07F938
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

39. 发明授权

US6024937A Aromatic amine substituted bridged nitrogen and sulfur donor atom ligands for imaging 失效
标题翻译：用于成像的芳族胺取代的桥连氮和硫供体原子配体
公开(公告)号：US6024937A
公开(公告)日：2000-02-15
申请号：US463232
申请日：1995-06-05
申请人： Sudhakar Kasina , Eric Yau , John M. Reno
发明人： Sudhakar Kasina , Eric Yau , John M. Reno
IPC分类号： C07D239/42 , A61K51/00 , A61K51/04 , C07B59/00 , C07C211/50 , C07C211/53 , C07C229/56 , C07C229/60 , C07C229/64 , C07C229/76 , C07C233/43 , C07C239/16 , C07C239/18 , C07C255/24 , C07C271/20 , C07C319/00 , C07C323/34 , C07C323/63 , C07D213/00 , C07D257/10 , C07D285/00 , C07D513/04 , C07F1/08 , C07F1/12 , C07F7/24 , C07F9/94 , C07F13/00 , C07F15/00 , C07D39/02
CPC分类号： C07C211/50 , A61K51/0478 , C07C229/60 , C07C229/64 , C07C233/43 , C07C239/16 , C07C239/18 , C07C323/34 , C07C323/63 , C07D257/10 , C07D285/00 , C07D513/04 , A61K2121/00 , A61K2123/00
摘要： The present invention provides aromatic amine substituted metal chelating compounds, chelates and chelate-targeting moiety conjugates formed from the chelating compounds, and methods for making and using these compounds. Metals capable of being chelated by the chelating compounds include radionuclides, such as .sup.99m Tc and .sup.186188 Re.
摘要翻译：本发明提供由螯合化合物形成的芳族胺取代的金属螯合化合物，螯合物和螯合靶向部分缀合物，以及制备和使用这些化合物的方法。能够被螯合化合物螯合的金属包括放射性核素，例如99mTc和186188Re。

40. 发明授权

US5968477A Radiolabeled annexin conjugates with hexose and a chelator 失效
标题翻译：放射性标记的膜联蛋白与己糖和螯合剂
公开(公告)号：US5968477A
公开(公告)日：1999-10-19
申请号：US690184
申请日：1996-07-26
申请人： Sudhakar Kasina , John M. Reno , Alan R. Fritzberg , Jonathan Tait
发明人： Sudhakar Kasina , John M. Reno , Alan R. Fritzberg , Jonathan Tait
IPC分类号： A61K51/00 , A61K47/48 , A61K51/08 , C07K1/13 , C07K5/04 , C07K7/06 , C07K14/435 , C07K14/47 , A61K35/14 , C07F5/00
CPC分类号： C07K7/06 , A61K47/48023 , A61K47/48076 , A61K47/48092 , A61K51/087 , A61K51/088 , C07K1/13 , C07K14/4721 , A61K2123/00
摘要： Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.
摘要翻译：描述了可用于成像血管血栓的放射性标记的膜联蛋白和修饰的膜联蛋白缀合物。还提供了制备和使用这种放射性标记的膜联蛋白缀合物的方法。

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