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1. 发明申请

US20080025915A1 Technetium-And Rhenium-Bis (Heteroaryl) Complexes, And Methods Of Use Thereof 有权
标题翻译：锝和铼 - 双（杂芳基）络合物及其使用方法
公开(公告)号：US20080025915A1
公开(公告)日：2008-01-31
申请号：US10589405
申请日：2005-02-14
申请人： John W. Babich , Kevin Maresca , James Kronauge
发明人： John W. Babich , Kevin Maresca , James Kronauge
IPC分类号： A61K51/04 , A61K103/10
CPC分类号： C07D233/64 , A61K51/04 , C07D213/38 , C07D217/14 , C07D235/14 , C07D235/20 , C07D277/28 , C07F13/005
摘要： One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
摘要翻译：本发明的一个方面涉及放射性核素与各种杂芳基配体的复合物，例如咪唑基和吡啶基配体，以及它们在放射性药物中用于多种临床诊断和治疗应用的复合物。本发明的另一方面涉及形成上述配合物的一部分的咪唑基和吡啶基配体。还描述了制备放射性核素复合物的方法。本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸，丙氨酸和双氨基酸的咪唑基和吡啶基配体。另外，本发明涉及使用本发明复合物成像哺乳动物区域的方法。

2. 发明授权

US06437103B1 Fatty acid analogs for diagnosis of coronary artery disease 失效
标题翻译：脂肪酸类似物用于诊断冠状动脉疾病
公开(公告)号：US06437103B1
公开(公告)日：2002-08-20
申请号：US09549732
申请日：2000-04-14
申请人： John W. Babich , Kevin Maresca , Timothy Shoup , David R. Elmaleh
发明人： John W. Babich , Kevin Maresca , Timothy Shoup , David R. Elmaleh
IPC分类号： C07F1300
CPC分类号： A61K51/0497 , A61K51/0478
摘要： Radioimaging agents, which exhibit high uptake and retention in the myocardium are disclosed.
摘要翻译：公开了在心肌中表现出高吸收和保留的放射成像剂

3. 发明授权

US08562945B2 Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof 有权
标题翻译：锝和铼 - 双（杂芳基）络合物及其使用方法
公开(公告)号：US08562945B2
公开(公告)日：2013-10-22
申请号：US12631312
申请日：2009-12-04
申请人： John W. Babich , Craig Zimmerman , John Joyal , Kevin P. Maresca , John Marquis , Genliang Lu , Jian-cheng Wang , Shawn Hillier
发明人： John W. Babich , Craig Zimmerman , John Joyal , Kevin P. Maresca , John Marquis , Genliang Lu , Jian-cheng Wang , Shawn Hillier
IPC分类号： A61K31/18 , A61K31/4192 , A61K31/444 , A61K31/555 , A61K51/04 , C07D213/38 , C07D403/12 , C07F13/00 , A61P1/00
CPC分类号： A61K31/18 , A61K31/4192 , A61K31/444 , A61K31/555 , A61K47/22 , A61K49/00 , A61K51/04 , A61K51/0406 , A61K51/041 , A61K51/0446 , A61K51/0474 , A61K51/0478 , C07C275/16 , C07C311/16 , C07D213/38 , C07D403/06 , C07D403/12 , C07F13/005
摘要： Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.
摘要翻译：基于具有取代的吡啶基和咪唑基的配体制备杂环放射性核素的配合物。配体是双功能的，具有可以作为生物活性分子的连接体的氨基酸残基，以及可能使该放射性核素复合的三齿螯合剂。生物活性分子可以是肽或生长抑素。

4. 发明申请

US20120269726A1 Heterodimers of Glutamic Acid 有权
标题翻译：谷氨酸的异二聚体
公开(公告)号：US20120269726A1
公开(公告)日：2012-10-25
申请号：US13271549
申请日：2011-10-12
申请人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
发明人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
IPC分类号： A61K51/04 , A61P25/00 , G01N33/573 , A61P25/18 , A61P29/00 , A61P25/04 , A61K39/385 , A61P35/00
CPC分类号： C07C275/16 , A61K39/385 , C07B59/001 , C07C275/24 , C07C275/30 , C07C311/19 , C07D213/38
摘要： Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C1-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
摘要翻译：式（Ia）化合物，其中R是C 6 -C 12取代或未取代的芳基，C 6 -C 12取代或未取代的杂芳基，C 1 -C 6取代或未取代的烷基或-NR'R'，Q是C（O），NR'，S，S（O）2，C（O）2（CH 2）p Y是C（O），O，NR'，S，S（O）2，C（O） Z是H或C1-C4烷基，R'是H，C（O），S（O）2，C（O）2，C6-C12取代或未取代的芳基，C6-C12取代或未取代的杂芳基或 C 1 -C 6取代或未取代的烷基，当被取代时，芳基，杂芳基和烷基被卤素，C 1 -C 12杂芳基，-NR'R'或COOZ取代，其具有诊断和治疗性质，例如前列腺癌的治疗和治疗和其他与NAALADase抑制有关的疾病。放射性标记可以通过各种通过碳或杂原子连接在X氨基酸侧链附着的假基团并入结构中。

5. 发明申请

US20120208988A1 HETERODIMERS OF GLUTAMIC ACID 有权
标题翻译：谷氨酸的交联剂
公开(公告)号：US20120208988A1
公开(公告)日：2012-08-16
申请号：US13294677
申请日：2011-11-11
申请人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
发明人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
IPC分类号： C07F13/00 , C07C311/19 , C07C275/24 , C07D401/12 , C07C275/16
CPC分类号： C07C275/16 , A61K39/385 , C07B59/001 , C07C275/24 , C07C275/30 , C07C311/19 , C07D213/38
摘要： Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
摘要翻译：式（Ia）化合物，其中R是C 6 -C 12取代或未取代的芳基，C 6 -C 12取代或未取代的杂芳基，C 1 -C 6取代或未取代的烷基或-NR'R'，Q是C（O），NR'，S，S（O）2，C（O）2（CH 2）p Y是C（O），O，NR'，S，S（O）2，C（O） Z是H或C1-C4烷基，R'是H，C（O），S（O）2，C（O）2，C6-C12取代或未取代的芳基，C6-C12取代或未取代的杂芳基或 C 1 -C 6取代或未取代的烷基，当被取代时，芳基，杂芳基和烷基被卤素，C 6 -C 12杂芳基，-NR'R'或COOZ取代，其具有诊断和治疗性质，例如前列腺癌的治疗和治疗和其他与NAALADase抑制有关的疾病。放射性标记可以通过各种通过碳或杂原子连接在X氨基酸侧链附着的假基团并入结构中。

6. 发明申请

US20100178246A1 TECHNETIUM- AND RHENIUM-BIS(HETEROARYL) COMPLEXES AND METHODS OF USE THEREOF FOR INHIBITING PSMA 有权
标题翻译：技术和RHENIUM-BIS（HETEROARYL）复合物及其用于抑制PSMA的方法
公开(公告)号：US20100178246A1
公开(公告)日：2010-07-15
申请号：US12631337
申请日：2009-12-04
申请人： John W. Babich , Craig Zimmerman , John Joyal , Kevin P. Maresca , Genliang Lu , Shawn Hillier
发明人： John W. Babich , Craig Zimmerman , John Joyal , Kevin P. Maresca , Genliang Lu , Shawn Hillier
IPC分类号： A61K51/04 , C07D403/12 , C07F13/00 , C07D401/12 , A61K31/555 , A61K49/00 , C07D213/56 , A61P25/18 , A61P29/00 , A61P13/08 , A61P35/00
CPC分类号： C07D213/38 , A61K31/18 , A61K31/4192 , A61K31/444 , A61K31/555 , A61K51/0406 , A61K51/041 , A61K51/0474 , A61K51/0478 , C07C275/16 , C07C311/16 , C07D403/06 , C07D403/12 , C07F13/005
摘要： A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.
摘要翻译：式I的化合物，其药学上可接受的盐或溶剂化物：与金属如铼，锝等复合，以提供用于成像组织或治疗疾病的复合物，特别是在金属是放射性的情况下。这种复合物对PSMA蛋白质是特异性的，因此可用于成像或治疗前列腺癌和表达蛋白质的其他组织的癌症。

7. 发明授权

US07381399B2 Technetium-dipyridine complexes, and methods of use thereof 有权
标题翻译：锝 - 二吡啶络合物及其使用方法
公开(公告)号：US07381399B2
公开(公告)日：2008-06-03
申请号：US10386403
申请日：2003-03-11
申请人： John W. Babich , Kevin P. Maresca
发明人： John W. Babich , Kevin P. Maresca
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07D213/38 , C07F13/005
摘要： One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
摘要翻译：本发明的一个方面涉及锝（Tc）与各种杂芳族配体如吡啶基和咪唑基配体的新型复合物，以及它们在放射性药物中用于各种临床诊断和治疗应用的用途。本发明的另一方面涉及形成上述配合物的一部分的新型吡啶基配体。还描述了制备锝络合物的方法。本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸，丙氨酸和双氨基酸的新型吡啶基配体。另外，本发明涉及使用本发明复合物成像哺乳动物区域的方法。

8. 发明授权

US08058449B2 Heterodimers of glutamic acid 有权
公开(公告)号：US08058449B2
公开(公告)日：2011-11-15
申请号：US11936659
申请日：2007-11-07
申请人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
发明人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
IPC分类号： C07C275/38
摘要： Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

9. 发明申请

US20100303725A1 Technetium- and Rhenium-Bis(heteroaryl) Complexes, and Methods of Use Thereof 审中-公开
标题翻译：锝和铼 - 双（杂芳基）络合物及其使用方法
公开(公告)号：US20100303725A1
公开(公告)日：2010-12-02
申请号：US12750533
申请日：2010-03-30
申请人： John W. Babich , Kevin B. Maresca , James F. Kronauge, JR.
发明人： John W. Babich , Kevin B. Maresca , James F. Kronauge, JR.
IPC分类号： A61K49/00 , C07D233/61 , C07F15/00 , A61K31/555 , C07K1/00
CPC分类号： C07F13/005 , C07D213/38
摘要： One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
摘要翻译：本发明的一个方面涉及放射性核素与各种杂芳基配体的复合物，例如咪唑基和吡啶基配体，以及它们在放射性药物中用于多种临床诊断和治疗应用的复合物。本发明的另一方面涉及形成上述配合物的一部分的咪唑基和吡啶基配体。还描述了制备放射性核素复合物的方法。本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸，丙氨酸和双氨基酸的咪唑基和吡啶基配体。另外，本发明涉及使用本发明复合物成像哺乳动物区域的方法。

10. 发明授权

US07824661B2 Technetium- and rhenium-bis(heteroaryl) complexes, and methods of use thereof 失效
标题翻译：锝和铼 - 双（杂芳基）络合物及其使用方法
公开(公告)号：US07824661B2
公开(公告)日：2010-11-02
申请号：US11057714
申请日：2005-02-14
申请人： John W. Babich , Kevin B. Maresca , James F. Kronauge, Jr.
发明人： John W. Babich , Kevin B. Maresca , James F. Kronauge, Jr.
IPC分类号： A61K49/00
CPC分类号： A61K51/0478 , C07F13/005
摘要： One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
摘要翻译：本发明的一个方面涉及放射性核素与各种杂芳基配体的复合物，例如咪唑基和吡啶基配体，以及它们在放射性药物中用于多种临床诊断和治疗应用的复合物。本发明的另一方面涉及形成上述配合物的一部分的咪唑基和吡啶基配体。还描述了制备放射性核素复合物的方法。本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸，丙氨酸和双氨基酸的咪唑基和吡啶基配体。另外，本发明涉及使用本发明复合物成像哺乳动物区域的方法。

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