公开(公告)号：US20060034758A1

公开(公告)日：2006-02-16

申请号：US11057714

申请日：2005-02-14

Applicant: John Babich ,  Kevin Maresca ,  James Kronauge

Inventor： John Babich ,  Kevin Maresca ,  James Kronauge

IPC: A61K51/00 ,  C07F13/00 ,  C07K14/47

CPC classification number: A61K51/0478 ,  C07F13/005

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08685369B2

公开(公告)日：2014-04-01

申请号：US10589405

申请日：2005-02-14

Applicant: John Babich ,  Kevin Maresca ,  James Kronauge

Inventor： John Babich ,  Kevin Maresca ,  James Kronauge

IPC: A61K49/00

CPC classification number: C07D233/64 ,  A61K51/04 ,  C07D213/38 ,  C07D217/14 ,  C07D235/14 ,  C07D235/20 ,  C07D277/28 ,  C07F13/005

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4735793A

公开(公告)日：1988-04-05

申请号：US771284

申请日：1985-08-30

Applicant: Alun G. Jones ,  Alan Davison ,  James Kronauge ,  Michael J. Abrams

Inventor： Alun G. Jones ,  Alan Davison ,  James Kronauge ,  Michael J. Abrams

IPC: C07B59/00 ,  A61K31/28 ,  A61K31/282 ,  A61K33/24 ,  A61K51/00 ,  A61K51/04 ,  C07B31/00 ,  C07C67/00 ,  C07C325/00 ,  C07C395/00 ,  C07F13/00 ,  C07F15/00 ,  C07F15/06 ,  A61K43/00 ,  A61K49/02 ,  C07C119/02

CPC classification number: C07F13/005 ,  A61K51/0476 ,  C07C251/00 ,  A61K2123/00

Abstract: A coordination complex comprising a radionuclide selected from the class consisting of radioactive isotopes of Tc, Ru, Co, Pt and Re and an isonitrile ligand of the formula:(CNX)R,where X is a lower alkyl group having 1 to 4 carbon atoms, wherein R is selected from the group consisting of COOR.sup.1 and CONR.sup.2 R.sup.3 where R.sup.1 can be H, a pharmaceutically acceptable cation, or a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms, R.sup.2, and R.sup.3 can be H, or a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms, and R.sup.2 and R.sup.3 can be the same or different is disclosed. Kits that can be used to form these complexes are also disclosed.

Abstract translation: 包含选自Tc，Ru，Co，Pt和Re的放射性同位素的放射性核素的配位络合物和式（CNX）R的异腈配体，其中X是具有1至4个碳原子的低级烷基 其中R选自COOR1和CONR2R3，其中R1可以是H，药学上可接受的阳离子或具有1至4个碳原子的取代或未取代的烷基，R 2和R 3可以是H，或者取代或 未取代的具有1至4个碳原子的烷基，R2和R3可以相同或不同。 还可以公开可用于形成这些络合物的试剂盒。

公开(公告)号：US20080025915A1

公开(公告)日：2008-01-31

申请号：US10589405

申请日：2005-02-14

Applicant: John W. Babich ,  Kevin Maresca ,  James Kronauge

Inventor： John W. Babich ,  Kevin Maresca ,  James Kronauge

IPC: A61K51/04 ,  A61K103/10

CPC classification number: C07D233/64 ,  A61K51/04 ,  C07D213/38 ,  C07D217/14 ,  C07D235/14 ,  C07D235/20 ,  C07D277/28 ,  C07F13/005

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4872561A

公开(公告)日：1989-10-10

申请号：US139289

申请日：1987-12-29

Applicant: Alun G. Jones ,  Alan Davison ,  James Kronauge ,  Michael J. Abrams

Inventor： Alun G. Jones ,  Alan Davison ,  James Kronauge ,  Michael J. Abrams

IPC: A61K51/00 ,  A61K51/04 ,  C07F13/00

CPC classification number: C07F13/005 ,  C07C251/00 ,  A61K2123/00

Abstract: A coordination complex comprising a radionuclide selected from the class consisting of radioactive isotopes of Tc, Ru, Co, Pt and Re and an isonitrile ligand of the formula:(CNX)R,where X is a lower alkyl group having 1 to 4 carbon atoms, wherein R is selected from the group consisting of COOR.sup.1 and CONR.sup.2 R.sup.3 where R.sup.1 can be H, a pharmaceutically acceptable cation, or a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms. R.sup.2, and R.sup.3 can be H, or a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms, and R.sup.2 and R.sup.3 can be the same of different is disclosed. Kits that can be used to form these complexes are also disclosed.

Abstract translation: 包含选自Tc，Ru，Co，Pt和Re的放射性同位素的放射性核素的配位络合物和式（CNX）R的异腈配体，其中X是具有1至4个碳原子的低级烷基 其中R选自COOR1和CONR2R3，其中R1可以是H，药学上可接受的阳离子或具有1至4个碳原子的取代或未取代的烷基。 R2和R3可以是H，或者取代或未取代的具有1至4个碳原子的烷基，R2和R3可以是不同的。 还可以公开可用于形成这些络合物的试剂盒。