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1. 发明授权

US11167049B2 Organ protection in PSMA-targeted radionuclide therapy of prostate cancer 有权
公开(公告)号：US11167049B2
公开(公告)日：2021-11-09
申请号：US16860925
申请日：2020-04-28
申请人： Molecular Insight Pharmaceuticals, Inc.
发明人： John W. Babich , Shawn Hillier , John Joyal
IPC分类号： A61K51/04 , A61K31/555 , A61K51/12
摘要： A method of reducing radiation exposure of a non-cancerous tissue of a patient diagnosed with a cancer includes administering to the patient an agent capable of competing for binding sites on a surface of the non-cancerous tissue, provided that the administration is carried out after a waiting period that follows administration of a compound including a radionuclide to the patient, the compound having affinity for both a cancerous tissue and the non-cancerous tissue, and, further provided that the binding sites have an affinity for both the agent and the compound.

2. 发明授权

US10898598B2 Triazine based radiopharmaceuticals and radioimaging agents 有权
公开(公告)号：US10898598B2
公开(公告)日：2021-01-26
申请号：US16231153
申请日：2018-12-21
申请人： Molecular Insight Pharmaceuticals, Inc.
发明人： John W. Babich , Craig Zimmerman , John L. Joyal , Genliang Lu
IPC分类号： A61K51/04 , C07D401/14 , C07D403/14 , C07D413/14 , C07F5/00 , A61B6/00
摘要： Metal complexes including a radionuclide and a compound of Formula I and Formula II are potent inhibitors of PSMA.

3. 发明授权

US10640461B2 Heterodimers of glutamic acid 有权
公开(公告)号：US10640461B2
公开(公告)日：2020-05-05
申请号：US15068841
申请日：2016-03-14
申请人： Molecular Insight Pharmaceuticals, Inc.
发明人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
IPC分类号： A61K51/04 , A61K49/00 , C07C275/16 , C07B59/00 , C07C275/30 , C07C311/19 , C07D213/38 , C07C275/24 , A61K39/385
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.

4. 发明申请

US20190276393A1 Heterodimers of Glutamic Acid 审中-公开
公开(公告)号：US20190276393A1
公开(公告)日：2019-09-12
申请号：US16156289
申请日：2018-10-10
申请人： Molecular Insight Pharmaceuticals, Inc.
发明人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
IPC分类号： C07C275/16 , A61K39/385 , C07D213/38 , C07B59/00 , C07C275/30 , C07C275/24 , C07C311/19
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 therapetitic 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.

5. 发明申请

US20140341805A1 TECHNETIUM- AND RHENIUM-BIS(HETEROARYL) COMPLEXES AND METHODS OF USE THEREOF 有权
标题翻译：技术和铑（复合物）复合物及其使用方法
公开(公告)号：US20140341805A1
公开(公告)日：2014-11-20
申请号：US14446220
申请日：2014-07-29
申请人： Molecular Insight Pharmaceuticals, Inc.
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： A61K51/04
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： A method of imaging a region in a subject includes administering to the subject a complex of a metal chelated to a compound, and obtaining an image of the region in the subject.
摘要翻译：对受试者中的区域成像的方法包括向受试者施用与化合物螯合的金属的复合物，并获得受试者中的区域的图像。

6. 发明授权

US08685369B2 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：US08685369B2
公开(公告)日：2014-04-01
申请号：US10589405
申请日：2005-02-14
申请人： John Babich , Kevin Maresca , James Kronauge
发明人： John Babich , Kevin Maresca , James Kronauge
IPC分类号： A61K49/00
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。

7. 发明申请

US20140030188A1 PROCESS FOR PRODUCTION OF HETERODIMERS OF GLUTAMIC ACID 审中-公开
标题翻译：制备葡萄糖酸酯的方法
公开(公告)号：US20140030188A1
公开(公告)日：2014-01-30
申请号：US13890912
申请日：2013-05-09
申请人： Molecular Insight Pharmaceuticals, Inc.
发明人： John W. BABICH , Craig ZIMMERMAN , Kevin P. MARESCA
IPC分类号： A61K51/04
CPC分类号： A61K51/0497 , C07B59/001 , C07B2200/05 , C07C273/1854 , C07C303/40 , C07F7/2208 , C07C311/19 , C07C275/16 , C07C275/24 , C07C275/30
摘要： A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of readionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; 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; R′ is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.
摘要翻译：用于制备放射性标记的式（I）化合物的制备方法包括在酸性条件下，在氧化剂存在下使式（II）化合物与卤素的准氮化物源反应，其中：* I为123 I，124 I，125 I 或131I; R是低级烷基，任选被一个或多个氟原子取代; Q是C（O），O，NR'，S，S（O）2，C（O）2，（CH 2）p; Y是C（O），O，NR'，S，S（O）2，C（O）2，（CH 2）p; R'是H，C（O），S（O）2，C（O）2; Z是H，C 1 -C 4烷基，苄基，取代的苄基或三烷基甲硅烷基; m为0,1,2,3,4或5; n为0，1，2，3，4，5或6; p为0,1,2,3,4,5或6。

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

US20110124948A1 RADIOLABELED TREATMENT INFUSION SYSTEM, APPARATUS, AND METHODS OF USING THE SAME 审中-公开
标题翻译：放射线治疗输注系统，装置及其使用方法
公开(公告)号：US20110124948A1
公开(公告)日：2011-05-26
申请号：US12936083
申请日：2009-04-03
申请人： Daniel L. Yokell
发明人： Daniel L. Yokell
IPC分类号： A61M36/08
CPC分类号： A61M5/1407 , A61M5/007 , A61M5/1415 , A61M5/1785 , A61M2209/08 , G21F5/015 , G21G1/0005 , G21H5/02
摘要： Described herein are methods and devices for infusion of a radioactive compound, such as yttrium-90 radiolabeled somatostatin peptide or analog. A radiation shield defining a shielded cavity suitable for storing a radioactive substance includes a first aperture providing external access to the shielded cavity and a second aperture suitable for transferring a dosage vial into and out of the shielded cavity. A removable shielded plug and panel are adapted to shield respective apertures of the radiation shield. At least one dose of a radiolabeled compound stored in a vial in the radiation shield is delivered through a fluid communication channel at a rate of about 500 mL/hour. The fluid communication channel is washed after delivery, such that the process substantially reduces radiation exposure during infusion of the radiolabeled compound into a patient.
摘要翻译：本文描述了用于输注放射性化合物的方法和装置，例如钇-90放射性标记的生长抑素肽或类似物。限定适于存储放射性物质的屏蔽空腔的辐射屏蔽包括提供对屏蔽空腔的外部通路的第一孔和适于将剂量小瓶转入和移出屏蔽腔的第二孔。可拆卸屏蔽插头和面板适于屏蔽辐射屏蔽的各个孔。储存在辐射屏蔽中的小瓶中的至少一剂放射性标记化合物以约500mL /小时的速率通过流体连通通道输送。流体连通通道在输送后洗涤，使得该过程在将放射性标记的化合物输注入患者期间显着降低辐射暴露。

10. 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。

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