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1. 发明授权

US07947838B2 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：US07947838B2
公开(公告)日：2011-05-24
申请号：US12643175
申请日：2009-12-21
申请人： Robert Mach , Zhude Tu
发明人： Robert 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。

2. 发明申请

US20100150836A1 RADIOLABELLED BENZAMIDE ANALOGUES, THEIR SYNTHESIS AND USE IN DIAGNOSTIC IMAGING 有权
标题翻译：无定形苯扎酰胺类似物，其合成和用于诊断成像
公开(公告)号：US20100150836A1
公开(公告)日：2010-06-17
申请号：US12643175
申请日：2009-12-21
申请人： Robert Mach , Zhude Tu
发明人： Robert Mach , Zhude Tu
IPC分类号： A61K51/04 , A61P35/00
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。

3. 发明申请

US20100028936A1 DETECTION OF CANCER CELLS IN VITRO USING SIGMA-2 RECEPTOR LIGANDS AS RADIOTRACERS 有权
标题翻译：使用SIGMA-2受体配体作为放射线检测体外检测癌细胞
公开(公告)号：US20100028936A1
公开(公告)日：2010-02-04
申请号：US12550220
申请日：2009-08-28
申请人： Robert Mach , Michael J. Welch , Douglas J. Rowland , Zhude Tu
发明人： Robert Mach , Michael J. Welch , Douglas J. Rowland , Zhude Tu
IPC分类号： C12Q1/02
CPC分类号： C07D295/13 , A61K31/47 , A61K31/495 , A61K51/04 , A61K51/0497 , C07C323/41 , C07D217/04 , C07D257/02
摘要： Methods for detection of cancer cells and for determining the proliferative status of cells in a tissue sample in vitro are disclosed. These methods comprise contacting a tissue sample with a radiolabeled compound or salt thereof of Formula wherein at least one of X, Y, and Z comprises a radioisotope, n is an integer from 2 to about 10; and each of A and A1 is a C1-C4 alkoxyl, a C1-C4 fluoroalkyl or a C1-C4 fluoroalkoxyl. The methods further comprise detecting the distribution of the radioisotope in the tissue sample, whereby a cell having a high density of the radioisotope compared to quiescent cells is diagnostic for a cancer cell.
摘要翻译：公开了用于检测癌细胞并用于测定体外组织样品中细胞增殖状态的方法。这些方法包括使组织样品与其中X，Y和Z中的至少一个包含放射性同位素的放射性标记的化合物或其盐接触，n为2至约10的整数; A和A1各自为C1-C4烷氧基，C1-C4氟烷基或C1-C4氟烷氧基。所述方法还包括检测组织样品中放射性同位素的分布，由此与静止细胞相比具有高密度放射性同位素的细胞是癌细胞的诊断。

4. 发明授权

US07612206B2 Sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors 有权
标题翻译：用于成像实体瘤增殖状态的Sigma-2受体放射性示踪剂
公开(公告)号：US07612206B2
公开(公告)日：2009-11-03
申请号：US12044952
申请日：2008-03-08
申请人： Robert Mach , Michael J. Welch , Douglas J. Rowland , Zhude Tu
发明人： Robert Mach , Michael J. Welch , Douglas J. Rowland , Zhude Tu
IPC分类号： C07D491/00 , A61K51/00 , A61M36/14
CPC分类号： C07D295/13 , A61K31/47 , A61K31/495 , A61K51/04 , A61K51/0497 , C07C323/41 , C07D217/04 , C07D257/02
摘要： Novel benzamide compounds of Formula (I), Formula (II), and Formula (III), salts, water soluble salts, analogs and radiolabeled counterparts thereof as sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors. A method for diagnosing a mammal for the presence of a mammalian tumor therein comprises administering to the mammal a diagnostic imaging detectable effective amount of a benzamide compound having a structure illustrated in Formula (I), Formula (II) and Formula (III) and detecting binding of the compound to a tumor in the mammal. A method for diagnostic imaging of a mammalian tissue having cell surface sigma-2 receptors comprising administering to a mammal a diagnostic imaging amount of a compound having a structure illustrated in Formula (I) Formula (II) and Formula (III) and detecting an image of a tissue having an ample cells with sigma-2 receptors.
摘要翻译：式（I），式（II）和式（III）的新型苯甲酰胺化合物，其盐，水溶性盐，类似物和放射性标记的对应物作为用于成像实体瘤增殖状态的σ-2受体放射性示踪剂。用于诊断哺乳动物存在哺乳动物肿瘤的方法包括给予哺乳动物诊断成像可检测的有效量的具有式（I），式（II）和式（III）所示结构的苯甲酰胺化合物和检测化合物与哺乳动物肿瘤的结合。一种用于具有细胞表面σ-2受体的哺乳动物组织的诊断成像的方法，包括向哺乳动物施用具有式（I）式（II）和式（III）所示结构的化合物的诊断成像量，并检测图像的具有西格玛-2受体的大量细胞的组织。

5. 发明申请

US20130315825A1 TRICYCLIC HETEROAROMATIC COMPOUNDS AS ALPHA-SYNUCLEIN LIGANDS 审中-公开
标题翻译：三聚异氰酸酯化合物作为ALPHA-SYNUCLEIN配体
公开(公告)号：US20130315825A1
公开(公告)日：2013-11-28
申请号：US13887171
申请日：2013-05-03
申请人： Zhude Tu , Robert Mach , Lihai Yu , Paul Kotzbauer
发明人： Zhude Tu , Robert Mach , Lihai Yu , Paul Kotzbauer
IPC分类号： C07D279/20 , A61K51/04 , C07D241/46 , C07D513/04 , C07D265/38
CPC分类号： C07D279/20 , A61K51/0465 , C07D241/46 , C07D265/38 , C07D279/30 , C07D513/04
摘要： Derivatives of phenothiazine, phenoxazine, and phenazine compounds and their use as α-synuclein ligands are described. Also described are methods of using these compounds and their radiolabeled analogs for the detection, monitoring, and treatment of synucleinopathies, including Parkinson's disease.
摘要翻译：吩噻嗪，吩恶嗪和吩嗪化合物的衍生物及其作为α-突触核蛋白配体的用途。还描述了使用这些化合物及其放射性标记的类似物用于检测，监测和治疗突触核蛋白病（包括帕金森病）的方法。

6. 发明申请

US20050107398A1 Sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors 有权
标题翻译：用于成像实体瘤增殖状态的Sigma-2受体放射性示踪剂
公开(公告)号：US20050107398A1
公开(公告)日：2005-05-19
申请号：US10903771
申请日：2004-07-30
申请人： Robert Mach , Michael Welch , Douglas Rowland , Zhude Tu
发明人： Robert Mach , Michael Welch , Douglas Rowland , Zhude Tu
IPC分类号： A61K31/47 , A61K31/495 , A61K51/04 , C07C323/41 , C07D217/04 , C07D257/02 , C07D295/13
CPC分类号： C07D295/13 , A61K31/47 , A61K31/495 , A61K51/04 , A61K51/0497 , C07C323/41 , C07D217/04 , C07D257/02
摘要： Novel benzamide compounds of Formula (I), Formula (II) and Formula (III, salts, water soluble salts, analogs and radiolabeled counterparts thereof as sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors. A method for diagnosing a mammal for the presence of a mammalian tumor therein comprises administering to the mammal a diagnostic imaging detectable effective amount of a benzamide compound having a structure illustrated in Formula (I), Formula (II) and Formula (III) and detecting binding of the compound to a tumor in the mammal. A method for diagnostic imaging of a mammalian tissue having cell surface sigma-2 receptors comprising administering to a mammal a diagnostic imaging amount of a compound having a structure illustrated in Formula (I) Formula (II) and Formula (III) and detecting an image of a tissue having an ample cells with sigma-2 receptors.
摘要翻译：式（I），式（II）和式（III）的新型苯甲酰胺化合物，用于成像实体瘤增殖状态的σ-2受体放射性示踪剂的盐，水溶性盐，类似物和放射性标记的对应物。对于哺乳动物肿瘤的存在，其中包括给予哺乳动物诊断成像可检测的有效量的具有式（I），式（II）和式（III）所示结构的苯甲酰胺化合物，并检测该化合物与一种用于具有细胞表面σ-2受体的哺乳动物组织的诊断成像的方法，包括向哺乳动物施用具有式（I）式（II）和式（III）所示结构的化合物的诊断成像量）并用σ-2受体检测具有充足细胞的组织的图像。

7. 发明申请

US20080107599A1 RADIOLABELLED BENZAMIDE ANALOGUES, THEIR SYNTHESIS AND USE IN DIAGNOSTIC IMAGING 有权
标题翻译：无定形苯扎酰胺类似物，其合成和用于诊断成像
公开(公告)号：US20080107599A1
公开(公告)日：2008-05-08
申请号：US11757246
申请日：2007-06-01
申请人： Robert Mach , Zhude Tu
发明人： Robert Mach , Zhude Tu
IPC分类号： A61K51/00 , A61P35/00 , C07D217/00
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^{18 F标记时，这些化合物可以用作通过正电子发射断层摄影（PET）成像肿瘤的放射性示踪剂。此外，当用<123>标记的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。}

8. 发明申请

US20110311447A1 Compounds comprising 4-benzoylpiperidine as a Sigma-1-selective ligand 有权
标题翻译：包含4-苯甲酰基哌啶作为Sigma-1-选择性配体的化合物
公开(公告)号：US20110311447A1
公开(公告)日：2011-12-22
申请号：US13164840
申请日：2011-06-21
申请人： Zhude Tu , Robert H. Mach , Wei Wang , Stanley M. Parsons
发明人： Zhude Tu , Robert H. Mach , Wei Wang , Stanley M. Parsons
IPC分类号： A61K51/04 , C07D401/14 , A61P25/28 , A61P25/22 , A61P25/00 , C07D401/04 , A61P25/24
CPC分类号： C07D401/04 , A61K51/0455 , C07D401/14
摘要： Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for σ1 receptors. Some compounds are also highly selective for σ1 receptor compared to σ2 receptor. Compounds can comprise radioisotopes, including 18F or 11C. Radiolabeled compounds can be used as probes for imaging distribution of σ1 receptor in a subject such as a human using positron emission tomography (PET) scanning.
摘要翻译：公开了二哌啶基化合物及其盐。这些化合物包括与α受体1的高亲和力配体。一些化合物与＆sgr。2受体相比，对于α受体1受体也是高选择性的。化合物可以包括放射性同位素，包括18F或11C。放射性标记的化合物可用作用于使用正电子发射断层扫描（PET）扫描的受试者例如人的成像分布的探针。

9. 发明授权

US08658131B2 Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand 有权
标题翻译：包含4-苯甲酰基哌啶作为σ-1-选择性配体的化合物
公开(公告)号：US08658131B2
公开(公告)日：2014-02-25
申请号：US13164840
申请日：2011-06-21
申请人： Zhude Tu , Robert H. Mach , Wei Wang , Stanley M. Parsons
发明人： Zhude Tu , Robert H. Mach , Wei Wang , Stanley M. Parsons
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07D401/04 , A61K51/0455 , C07D401/14
摘要： Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for σ1 receptors. Some compounds are also highly selective for σ1 receptor compared to σ2 receptor. Compounds can comprise radioisotopes, including 18F or 11C. Radiolabeled compounds can be used as probes for imaging distribution of σ1 receptor in a subject such as a human using positron emission tomography (PET) scanning.
摘要翻译：公开了二哌啶基化合物及其盐。这些化合物包括用于σ1受体的高亲和力配体。与sigma2受体相比，一些化合物对σ1受体也具有高选择性。化合物可以包括放射性同位素，包括18F或11C。放射性标记的化合物可用作用于使用正电子发射断层摄影（PET）扫描的受试者（例如人）中的sigma1受体成像分布的探针。

10. 发明授权

US07612085B2 Sigma 2 receptor ligands and therapeutic uses therefor 有权
标题翻译： Sigma 2受体配体及其治疗用途
公开(公告)号：US07612085B2
公开(公告)日：2009-11-03
申请号：US11776533
申请日：2007-07-11
申请人： Robert H. Mach , Zhude Tu , Wenhua Chu , Suwanna Vangveravong , Richard Hotchkiss , William Hawkins , Rebecca Aft
发明人： Robert H. Mach , Zhude Tu , Wenhua Chu , Suwanna Vangveravong , Richard Hotchkiss , William Hawkins , Rebecca Aft
IPC分类号： A01N43/42 , A61K31/44 , C07D221/02
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-3-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（sigma1和sigma2）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-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-3α-基）-N' - （2-甲氧基-5-甲基苯基）氨基甲酸酯显示出对sigma2与σ1受体的高亲和力和选择性。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sigma2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。这些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。

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