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21. 发明授权

US10676467B2 Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof 有权
公开(公告)号：US10676467B2
公开(公告)日：2020-06-09
申请号：US16025324
申请日：2018-07-02
申请人： Zhude Tu , Adam Rosenberg , Hui Liu , Junbin Han
发明人： Zhude Tu , Adam Rosenberg , Hui Liu , Junbin Han
IPC分类号： C07D413/04 , C07D419/04 , C07D413/10 , C07D271/06 , C07B59/00 , C07D413/12
摘要： Among the various aspects of the present disclosure is the provision of a compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof. Provided are imaging agents for imaging S1P1 and S1P1 associated diseases, disorders, and conditions. Also provided are therapeutic compositions and methods for the treatment of S1P1 associated diseases, disorders, and conditions.

22. 发明授权

US08506927B2 Pegylated fluorobenzamide analogues, their synthesis and use in diagnostic imaging 失效
标题翻译：聚乙二醇化的氟代苯甲酰胺类似物，它们的合成和用于诊断成像
公开(公告)号：US08506927B2
公开(公告)日：2013-08-13
申请号：US13344084
申请日：2012-01-05
申请人： Robert H. Mach , Zhude Tu
发明人： Robert H. Mach , Zhude Tu
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/065 , C07D217/04
摘要： Pegylated fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labeled with a positron-emitting radioisotope such as 18F, can be used as radiotracers for medical imaging such as imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labeled with 123I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
摘要翻译：公开了选择性结合Sigma-2受体的聚乙二醇化氟烷基苯甲酰胺化合物。当用正电子发射的放射性同位素如18F标记时，这些化合物可用作医学成像的放射性示踪剂，例如通过正电子发射断层摄影（PET）成像肿瘤。此外，当用123I标记时，这些化合物可以用作通过单光子发射计算机断层摄影（SPECT）成像肿瘤的放射性示踪剂。还公开了这些化合物的合成方法。

23. 发明申请

US20120171119A1 PEGYLATED FLUOROBENZAMIDE ANALOGUES, THEIR SYNTHESIS AND USE IN DIAGNOSTIC IMAGING 失效
标题翻译：聚对苯二甲酸甲酯类似物，其合成和用于诊断成像
公开(公告)号：US20120171119A1
公开(公告)日：2012-07-05
申请号：US13344084
申请日：2012-01-05
申请人： Robert H. Mach , Zhude Tu
发明人： Robert H. Mach , Zhude Tu
IPC分类号： A61K51/04 , A61P35/00 , C07D217/20
CPC分类号： A61K51/065 , C07D217/04
摘要： Pegylated fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labeled with a positron-emitting radioisotope such as 18F, can be used as radiotracers for medical imaging such as imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labeled with 123I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
摘要翻译：公开了选择性结合Sigma-2受体的聚乙二醇化氟烷基苯甲酰胺化合物。当用正电子发射的放射性同位素如18F标记时，这些化合物可用作医学成像的放射性示踪剂，例如通过正电子发射断层摄影（PET）成像肿瘤。此外，当用123I标记时，这些化合物可以用作通过单光子发射计算机断层摄影（SPECT）成像肿瘤的放射性示踪剂。还公开了这些化合物的合成方法。

24. 发明授权

US08193360B2 Radiolabelled fluorobenzamide analogues, their synthesis and use in diagnostic imaging 有权
标题翻译：放射性标记的氟代苯甲酰胺类似物，它们的合成和用于诊断成像
公开(公告)号：US08193360B2
公开(公告)日：2012-06-05
申请号：US13082215
申请日：2011-04-07
申请人： Robert H. Mach , Zhude Tu
发明人： Robert H. Mach , Zhude Tu
IPC分类号： C07D217/10
CPC分类号： A61K31/47 , A61K31/495 , A61K51/04 , A61K51/0497 , C07C323/41 , C07D217/04 , C07D257/02 , C07D295/13
摘要： Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
摘要翻译：公开了选择性结合Sigma-2受体的氟烷氧基苯甲酰胺化合物。当用18F标记时，这些化合物可以用作通过正电子发射断层扫描（PET）成像肿瘤的放射性示踪剂。此外，当用123I标记时，这些化合物可以用作通过单光子发射计算机断层摄影（SPECT）成像肿瘤的放射性示踪剂。还公开了这些化合物的合成方法。

25. 发明授权

US08168650B2 Therapeutic uses of bicyclic ligands of sigma 2 receptor 有权
标题翻译： sigma2受体双环配体的治疗用途
公开(公告)号：US08168650B2
公开(公告)日：2012-05-01
申请号：US12543647
申请日：2009-08-19
申请人： Robert H. Mach , Richard Hotchkiss , William Hawkins , Rebecca Aft , Zhude Tu
发明人： Robert H. Mach , Richard Hotchkiss , William Hawkins , Rebecca Aft , Zhude Tu
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D451/14 , C07D451/02
摘要： A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3α-yl)-N′-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for σ2 versus σ1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the σ2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.
摘要翻译：公开了一系列N-取代的9-氮杂双环[3.3.1]壬烷-3α-基苯基氨基甲酸酯类似物及其制备方法。描述了它们对西格玛（＆sgr。1和＆sgr; 2）受体的亲和力。两种新化合物N-（9-（4-氨基丁基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯和N-（9- 6-氨基己基）-9-氮杂双环[3.3.1]壬烷-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对于＆ 1受体。所公开的化合物中有生物素化和荧光类似物。这些化合物可以作为第二受体的探针。此外，一些公开的化合物可以通过胱天蛋白酶依赖性和半胱天冬酶非依赖性机制诱导凋亡细胞死亡，并且对于治疗肿瘤是有效的。该化合物可用作化学治疗剂或化学敏化剂，用于治疗各种实体瘤。

26. 发明申请

US20110230662A1 RADIOLABELLED FLUOROBENZAMIDE ANALOGUES, THEIR SYNTHESIS AND USE IN DIAGNOSTIC IMAGING 有权
标题翻译：放射性氟化硼酰胺类似物，其合成和用于诊断成像
公开(公告)号：US20110230662A1
公开(公告)日：2011-09-22
申请号：US13082215
申请日：2011-04-07
申请人： Robert H. Mach , Zhude Tu
发明人： Robert H. Mach , Zhude Tu
IPC分类号： C07D215/14
CPC分类号： A61K31/47 , A61K31/495 , A61K51/04 , A61K51/0497 , C07C323/41 , C07D217/04 , C07D257/02 , C07D295/13
摘要： Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
摘要翻译：公开了选择性结合Sigma-2受体的氟烷氧基苯甲酰胺化合物。当用18F标记时，这些化合物可以用作通过正电子发射断层扫描（PET）成像肿瘤的放射性示踪剂。此外，当用123I标记时，这些化合物可以用作通过单光子发射计算机断层摄影（SPECT）成像肿瘤的放射性示踪剂。还公开了这些化合物的合成方法。

27. 发明授权

US07659400B2 Radiolabelled benzamide analogues, their synthesis and use in diagnostic imaging 有权
标题翻译：放射性标记的苯甲酰胺类似物，其合成和用于诊断成像
公开(公告)号：US07659400B2
公开(公告)日：2010-02-09
申请号：US11757246
申请日：2007-06-01
申请人： Robert H. Mach , Zhude Tu
发明人： Robert H. Mach , Zhude Tu
IPC分类号： C07D451/00 , C07D451/14
CPC分类号： A61K31/47 , A61K31/495 , A61K51/04 , A61K51/0497 , C07C323/41 , C07D217/04 , C07D257/02 , C07D295/13
摘要： Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
摘要翻译：公开了选择性结合Sigma-2受体的氟烷氧基苯甲酰胺化合物。当用18F标记时，这些化合物可以用作通过正电子发射断层扫描（PET）成像肿瘤的放射性示踪剂。此外，当用123I标记时，这些化合物可以用作通过单光子发射计算机断层摄影（SPECT）成像肿瘤的放射性示踪剂。还公开了这些化合物的合成方法。

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