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公开(公告)号：US08486372B2
公开(公告)日：2013-07-16
申请号：US13113580
申请日：2011-05-23
申请人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
发明人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
IPC分类号： A61B5/055
摘要： The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
摘要翻译： 本申请涉及放射性标记的环状多氮杂肽，包含放射性标记的环状多氮杂肽的药物组合物，以及使用放射性标记的环状多氮杂肽的方法。 这种多分子肽可用于成像研究，如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。
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公开(公告)号：US08043601B2
公开(公告)日：2011-10-25
申请号：US12180444
申请日：2008-07-25
申请人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
发明人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
摘要： The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
摘要翻译： 本申请涉及放射性标记的环状多氮杂肽，包含放射性标记的环状多氮杂肽的药物组合物，以及使用放射性标记的环状多氮杂肽的方法。 这种多分子肽可用于成像研究，如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。
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公开(公告)号：US08420052B2
公开(公告)日：2013-04-16
申请号：US12509259
申请日：2009-07-24
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Wei Zhang , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Kai Chen , Anjana Sinha , Eric Wang , Gang Chen , Peter J. H. Scott , Henry Clifton Padgett , Qianwa Liang , Zhiyong Gao , Tieming Zhao , Chunfang Xia , Vani P. Mocharla
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Wei Zhang , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Kai Chen , Anjana Sinha , Eric Wang , Gang Chen , Peter J. H. Scott , Henry Clifton Padgett , Qianwa Liang , Zhiyong Gao , Tieming Zhao , Chunfang Xia , Vani P. Mocharla
CPC分类号： C07D417/14 , A61K51/0406 , A61K51/0453 , A61K51/0455 , A61K51/0459 , C07D277/64 , C07D277/68 , C07D417/04 , C07D471/04 , C07D498/14 , C07D513/04 , C07D513/14
摘要： Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.
摘要翻译： 本文提供了包含本文公开的式的化合物和组合物，其中所述化合物是淀粉样蛋白结合化合物。 根据本发明的淀粉样蛋白结合化合物可以以适于淀粉样蛋白沉积物的体内成像的量施用于患者，并且可以区分具有淀粉样沉积物的神经组织和正常神经组织。 本发明的淀粉样蛋白探针可用于检测和定量疾病中的淀粉样蛋白沉积物，包括例如唐氏综合症，家族性阿尔茨海默氏病。 在另一个实施方案中，所述化合物可用于治疗或预防神经变性疾病。 本文还提供了允许化合物分布到脑组织中并对脑组织成像的方法，其中与正常对照结合水平相比，化合物与脑组织的结合增加指示哺乳动物患有或 有发展神经变性疾病的风险。
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4.发明申请DEVELOPMENT OF MOLECULAR IMAGING PROBES FOR CARBONIC ANHYDRASE-IX USING CLICK CHEMISTRY 有权使用单一化学物质开发碳氢化合物IX的分子成像探针公开(公告)号：US20090123372A1
公开(公告)日：2009-05-14
申请号：US12099135
申请日：2008-04-07
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Bing Wang , Umesh B. Gangadharmath , Brian A. Duclos , Kai Chen , Wei Zhang , Gang Chen , Henry Clifton Padgett , Farhad Karimi , Peter J. H. Scott , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Tieming Zhao , Chunfang Xia
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Bing Wang , Umesh B. Gangadharmath , Brian A. Duclos , Kai Chen , Wei Zhang , Gang Chen , Henry Clifton Padgett , Farhad Karimi , Peter J. H. Scott , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Tieming Zhao , Chunfang Xia
IPC分类号： C07D249/04 , C07D413/12 , A61K49/04 , A61K51/04
CPC分类号： C07D417/04 , C07D249/04 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14 , C12Q1/485 , G01N2500/04 , G01N2500/10
摘要： The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
摘要翻译： 本申请公开了使用点击化学法鉴定对碳酸酐酶IX（CA-IX）酶具有高结合亲和力的抑制剂的方法，并将其候选用作正电子发射断层摄影（PET）成像剂。
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公开(公告)号：US20090074664A1
公开(公告)日：2009-03-19
申请号：US12180444
申请日：2008-07-25
申请人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
发明人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
摘要： The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
摘要翻译： 本申请涉及放射性标记的环状多氮杂肽，包含放射性标记的环状多氮杂肽的药物组合物，以及使用放射性标记的环状多氮杂肽的方法。 这种多分子肽可用于成像研究，如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。
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6.发明授权Development of molecular imaging probes for carbonic anhydrase-IX using click chemistry 有权使用点击化学开发碳酸酐酶IX的分子成像探针公开(公告)号：US08354092B2
公开(公告)日：2013-01-15
申请号：US12862955
申请日：2010-08-25
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Bing Wang , Umesh B. Gangadharmath , Brian A. Duclos , Kai Chen , Wei Zhang , Gang Chen , Henry Clifton Padgett , Farhad Karimi , Peter J. H. Scott , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Tieming Zhao , Chunfang Xia
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Bing Wang , Umesh B. Gangadharmath , Brian A. Duclos , Kai Chen , Wei Zhang , Gang Chen , Henry Clifton Padgett , Farhad Karimi , Peter J. H. Scott , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Tieming Zhao , Chunfang Xia
IPC分类号： A61K51/00 , C07D249/00 , C07D343/00
CPC分类号： C07D417/04 , C07D249/04 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14 , C12Q1/485 , G01N2500/04 , G01N2500/10
摘要： The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
摘要翻译： 本申请公开了使用点击化学法鉴定对碳酸酐酶IX（CA-IX）酶具有高结合亲和力的抑制剂的方法，并将其候选用作正电子发射断层摄影（PET）成像剂。
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公开(公告)号：US20110256057A1
公开(公告)日：2011-10-20
申请号：US13113580
申请日：2011-05-23
申请人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
发明人： Hartmuth C. Kolb , Kai Chen , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Gang Chen , Qianwa Liang , Tieming Zhao
摘要： The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
摘要翻译： 本申请涉及放射性标记的环状多氮杂肽，包含放射性标记的环状多氮杂肽的药物组合物，以及使用放射性标记的环状多氮杂肽的方法。 这种多分子肽可用于成像研究，如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。
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公开(公告)号：US20110046378A1
公开(公告)日：2011-02-24
申请号：US12867502
申请日：2009-02-17
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Qianwa Liang , Brian A. Duclos , Wei Zhang , Peter J.H. Scott , Kai Chen , Zhiyong Gao , Tieming Zhao , Vani P. Mocharla , Dhanalakshmi Kasi , Gang Chen , Eric Wang , Anjana Sinha , Chunfang Xia , Henry Clifton Padgett , Farhad Karimi
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Qianwa Liang , Brian A. Duclos , Wei Zhang , Peter J.H. Scott , Kai Chen , Zhiyong Gao , Tieming Zhao , Vani P. Mocharla , Dhanalakshmi Kasi , Gang Chen , Eric Wang , Anjana Sinha , Chunfang Xia , Henry Clifton Padgett , Farhad Karimi
IPC分类号： C07D471/04 , C07D235/10 , C07D311/30 , C07D209/88 , C07D311/16 , C07D217/24 , C07D261/08 , C07D217/04 , C07D215/38 , C07D405/04 , C07D215/233 , C07D407/04 , C07D249/06 , C07D401/04 , C07D209/80 , C07D405/12
CPC分类号： C07B59/002
摘要： Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease
摘要翻译： 本文公开了在哺乳动物中诊断阿尔茨海默病或其倾向的化合物和方法，所述方法包括向哺乳动物施用诊断有效量的放射性标记的化合物，其中所述化合物选自放射性标记的黄酮，香豆素，咔唑 ，喹啉酮，色烯酮，咪唑和三唑衍生物，使化合物分布到脑组织中，并使脑组织成像，其中与正常对照结合水平相比，化合物与脑组织的结合增加指示哺乳动物 患有或有发生阿尔茨海默病的风险
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9.发明申请Development of Molecular Imaging Probes for Carbonic Anhydrase-IX Using Click Chemistry 有权使用点击化学开发碳酸酐酶IX的分子成像探针公开(公告)号：US20100317842A1
公开(公告)日：2010-12-16
申请号：US12862955
申请日：2010-08-25
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Bing Wang , Umesh B. Gangadharmath , Brian A. Duclos , Kai Chen , Wei Zhang , Gang Chen , Henry Clifton Padgett , Farhad Karimi , Peter J.H. Scott , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Tieming Zhao , Chunfang Xia
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Dhanalakshmi Kasi , Vani P. Mocharla , Bing Wang , Umesh B. Gangadharmath , Brian A. Duclos , Kai Chen , Wei Zhang , Gang Chen , Henry Clifton Padgett , Farhad Karimi , Peter J.H. Scott , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Tieming Zhao , Chunfang Xia
IPC分类号： C07D417/12 , C07D417/14 , C07D249/06 , C07D413/06 , C07D403/06 , C07D405/12 , C07D401/12 , C07D453/02 , C07D453/04 , C07H7/06 , C07H17/02
CPC分类号： C07D417/04 , C07D249/04 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14 , C12Q1/485 , G01N2500/04 , G01N2500/10
摘要： The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
摘要翻译： 本申请公开了使用点击化学法鉴定对碳酸酐酶IX（CA-IX）酶具有高结合亲和力的抑制剂的方法，并将其候选用作正电子发射断层摄影（PET）成像剂。
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公开(公告)号：US20110091382A1
公开(公告)日：2011-04-21
申请号：US12372717
申请日：2009-02-17
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Qianwa Liang , Brian A. Duclos , Wei Zhang , Peter J.H. Scott , Kai Chen , Zhiyong Gao , Tieming Zhao , Vani P. Mocharla , Dhanalakshmi Kasi , Gang Chen , Eric Wang , Anjana Sinha , Chunfang Xia , Henry Clifton Padgett , Farhad Karimi
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Qianwa Liang , Brian A. Duclos , Wei Zhang , Peter J.H. Scott , Kai Chen , Zhiyong Gao , Tieming Zhao , Vani P. Mocharla , Dhanalakshmi Kasi , Gang Chen , Eric Wang , Anjana Sinha , Chunfang Xia , Henry Clifton Padgett , Farhad Karimi
IPC分类号： A61K51/04 , C07D209/82 , C07D311/20 , C07D403/12 , C07D405/12 , C07D471/04 , A61P25/28 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/18
CPC分类号： C07B59/002
摘要： Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.
摘要翻译： 本文公开了在哺乳动物中诊断阿尔茨海默病或其倾向的化合物和方法，所述方法包括向哺乳动物施用诊断有效量的放射性标记的化合物，其中所述化合物选自放射性标记的黄酮，香豆素，咔唑 ，喹啉酮，色烯酮，咪唑和三唑衍生物，使化合物分布到脑组织中，并使脑组织成像，其中与正常对照结合水平相比，化合物与脑组织的结合增加指示哺乳动物 患有或有发生阿尔茨海默病的风险。
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