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1. 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。

2. 发明授权

US07408046B2 Treatment of bone-associated cancers 失效
标题翻译：骨相关癌症的治疗
公开(公告)号：US07408046B2
公开(公告)日：2008-08-05
申请号：US10882054
申请日：2004-06-30
申请人： Alan R. Fritzberg , Paul G. Abrams , Lauren Marie Tatalick , Kent R. Thoelke , James Kyle Bryan , Mark D. Hylarides , Elizabeth K. John
发明人： Alan R. Fritzberg , Paul G. Abrams , Lauren Marie Tatalick , Kent R. Thoelke , James Kyle Bryan , Mark D. Hylarides , Elizabeth K. John
IPC分类号： C07F5/00
CPC分类号： A61K51/0482 , A61K51/0478 , A61K51/0489 , Y10S514/836
摘要： The present invention relates to a method of suppressing bone marrow (BM) and treating conditions that arise in or near bone such as cancer, myeloproliferative diseases, autoimmune diseases, infectious diseases, metabolic diseases or genetic diseases, with compositions having as their active ingredient a radionuclide complexed with a chelating agent such as macrocyclic aminophosphonic acid.
摘要翻译：本发明涉及一种抑制骨髓（BM）的治疗方法，并且治疗在诸如癌症，骨髓增生性疾病，自身免疫性疾病，传染病，代谢疾病或遗传疾病之类的骨附近或附近产生的病症，组合物具有作为其活性成分的组合物与螯合剂如大环氨基膦酸络合的放射性核素。

3. 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。

4. 发明授权

US5202451A Anchimeric radiometal chelating compounds 失效
标题翻译： ANCHIMERIC RADIOMETAL CHELATING化合物
公开(公告)号：US5202451A
公开(公告)日：1993-04-13
申请号：US157284
申请日：1988-02-17
申请人： Alan R. Fritzberg , Ananthachari Srinivasan
发明人： Alan R. Fritzberg , Ananthachari Srinivasan
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.

5. 发明授权

US5175343A Metal radionuclide labeled proteins for diagnosis and therapy 失效
标题翻译：金属放射性核素标记的蛋白质用于诊断和治疗
公开(公告)号：US5175343A
公开(公告)日：1992-12-29
申请号：US065017
申请日：1987-06-19
申请人： Alan R. Fritzberg , Sudhakar Kasina , Ananthachari Srinivasan , Daniel S. Wilbur
发明人： Alan R. Fritzberg , Sudhakar Kasina , Ananthachari Srinivasan , Daniel S. Wilbur
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
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。

6. 发明授权

US5175256A Protein labeling reagents 失效
标题翻译：蛋白标记试剂
公开(公告)号：US5175256A
公开(公告)日：1992-12-29
申请号：US590180
申请日：1990-09-28
申请人： Sudhakar Kasina , Ananthachari Srinivasan , James Sanderson , Alan R. Fritzberg
发明人： Sudhakar Kasina , Ananthachari Srinivasan , James Sanderson , Alan R. Fritzberg
IPC分类号： A61K51/10 , C07C319/18 , C07C323/52 , C07D307/60 , C07D339/06 , C07D495/04
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).
摘要翻译：新型标记试剂可用于放射性标记蛋白，如具有放射性核素金属如99mTc，186Re和188Re的抗体。试剂为下式：其中：各X独立地选自O，S，NH或NR 2，其中R 2为保护基或吸电子基团; R1表示保护基团，其中每个R 1是单独的保护基团，或者两个R 1符号一起表示单个保护基团; 并且每个T独立地选自氢，1至约6个碳原子的低级烷基，吸电子基团和1至6个碳原子被吸电子基团取代的低级烷基。

7. 发明授权

US5120526A Method of producing metal radionuclide labeled proteins for diagnosis and therapy 失效
标题翻译：生产用于诊断和治疗的金属放射性核素标记蛋白质的方法
公开(公告)号：US5120526A
公开(公告)日：1992-06-09
申请号：US650834
申请日：1991-02-04
申请人： Alan R. Fritzberg , Sudhakar Kasina , Ananthachari Srinivasan , Daniel S. Wilbur
发明人： Alan R. Fritzberg , Sudhakar Kasina , Ananthachari Srinivasan , Daniel S. Wilbur
IPC分类号： A61K51/04 , A61K51/10 , A61K51/12 , C07C227/08 , C07C271/22
CPC分类号： C07C271/22 , A61K51/04 , 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。

8. 发明授权

US4885153A Radiohalogenated for proteins 失效
标题翻译：放射性卤化蛋白质
公开(公告)号：US4885153A
公开(公告)日：1989-12-05
申请号：US338497
申请日：1989-04-13
申请人： Daniel S. Wilbur , Alan R. Fritzberg , David S. Jones
发明人： Daniel S. Wilbur , Alan R. Fritzberg , David S. Jones
IPC分类号： C07F3/12 , C07F7/22
CPC分类号： C07F7/2212 , C07F3/12
摘要： Haloaryl compounds bearing a defined functional group or precursor are metalated with either Sn(n-Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound may be transmetalated in site-specific reaction with one of the following organometallic groups: HgX.sub.2, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.3, wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The stannylated or otherwise metalated compounds are subsequently radiohalogenated via a demetalation reaction. The Stannylated or otherwise metalated compounds are subsequently radiohalogenated via a demetalation reaction. The functional group is suitable for conjugation to protein and can be present or be added subsequent, but most preferably prior, to the radiohalogenation.Also compounds of the formula: R.sub.1 --Ar--R.sub.2, wherein R.sub.1 is either a radiohalogen or any one of the organometallic groups stated above, Ar is aromatic or heteroaromatic ring, and R.sub.2 is a short-chain substituent that does not highly activate the aromatic ring an that bears a functional group suitable for conjugation to protein under conditions that preserve the biological activity of the protein. The radiohalogenated small nolecules are conjugated to proteins such as monoclonal antibodies for use in diagnosis and therapy.
摘要翻译：带有限定官能团或前体的卤代芳基化合物与Sn（n-Bu）3或SnMe 3金属化。所得的芳基锡化合物可以与以下有机金属基团之一的位置特异性反应转金属：HgX2，Hg（OAc）2，BX3或BZ3，其中X为Cl，Br或I，Z为烷基或烷氧基。然后通过脱金属反应使经卤化或其它金属化的化合物放射性卤化。然后通过脱金属反应使经卤化或其它金属化的化合物放射性卤化。该官能团适用于与蛋白质缀合，并且可以存在或随后添加，但最优选之前为放射性卤化。还有下式的化合物：R1-Ar-R2，其中R1是放射性卤素或上述有机金属基团中的任一个，Ar是芳族或杂芳族环，R2是不高度活化芳族的短链取代基在保护蛋白质的生物活性的条件下，具有适合于与蛋白质缀合的官能团。放射性卤化的小分子与蛋白质缀合，例如用于诊断和治疗的单克隆抗体。

9. 发明授权

US07691985B2 Skeletal-targeted radiation to treat bone-associated pathologies 失效
标题翻译：骨骼靶向辐射治疗骨相关病变
公开(公告)号：US07691985B2
公开(公告)日：2010-04-06
申请号：US12043757
申请日：2008-03-06
申请人： Alan R. Fritzberg
发明人： Alan R. Fritzberg
IPC分类号： C07F5/00
CPC分类号： A61K51/0478 , A61K51/0489
摘要： The present invention relates to a method of suppressing bone marrow (BM) and treating conditions that arise in or near bone such as cancer, myeloproliferative diseases, autoimmune diseases, infectious diseases, metabolic diseases or genetic diseases, with compositions having as their active ingredient a radionuclide complexed with a chelating agent such as macrocyclic aminophosphonic acid.
摘要翻译：本发明涉及一种抑制骨髓（BM）的治疗方法，并且治疗在诸如癌症，骨髓增生性疾病，自身免疫性疾病，传染病，代谢疾病或遗传疾病之类的骨附近或附近产生的病症，组合物具有作为其活性成分的组合物与螯合剂如大环氨基膦酸络合的放射性核素。

10. 发明申请

US20080279773A1 SKELETAL-TARGETED RADIATION TO TREAT BONE-ASSOCIATED PATHOLOGIES 失效
标题翻译：骨骼靶向辐射治疗骨相关病理学
公开(公告)号：US20080279773A1
公开(公告)日：2008-11-13
申请号：US12043757
申请日：2008-03-06
申请人： Alan R. Fritzberg
发明人： Alan R. Fritzberg
IPC分类号： A61K51/00 , A61P35/00
CPC分类号： A61K51/0478 , A61K51/0489
摘要： The present invention relates to a method of suppressing bone marrow (BM) and treating conditions that arise in or near bone such as cancer, myeloproliferative diseases, autoimmune diseases, infectious diseases, metabolic diseases or genetic diseases, with compositions having as their active ingredient a radionuclide complexed with a chelating agent such as macrocyclic aminophosphonic acid.
摘要翻译：本发明涉及一种抑制骨髓（BM）的治疗方法，并且治疗在诸如癌症，骨髓增生性疾病，自身免疫性疾病，传染病，代谢疾病或遗传疾病之类的骨附近或附近产生的病症，组合物具有作为其活性成分的组合物与螯合剂如大环氨基膦酸络合的放射性核素。

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