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1.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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2.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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3.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：US07829063B2
公开(公告)日：2010-11-09
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： A61K51/00 , 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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4.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：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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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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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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公开(公告)号：US20090010846A1
公开(公告)日：2009-01-08
申请号：US12098390
申请日：2008-04-04
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Umesh B. Gangadharmath , Farhad Karimi , Henry Clifton Padgett , Dhanalakshmi Kasi , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Brian A. Duclos , Tieming Zhao
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Umesh B. Gangadharmath , Farhad Karimi , Henry Clifton Padgett , Dhanalakshmi Kasi , Zhiyong Gao , Qianwa Liang , Thomas Lee Collier , Brian A. Duclos , Tieming Zhao
IPC分类号： A61K51/04 , C07D403/12 , A61P35/00
CPC分类号： C07D403/06 , C07B59/002 , C07D403/12
摘要： The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.
摘要翻译： 本发明涉及用于体内检测缺氧性肿瘤或缺血组织的式I的新型放射性标记的生物可降解示踪剂。 在一个实施方案中，示踪剂由2-硝基咪唑部分，三唑，具有药代动力学增强取代基的代谢稳定接头和放射性同位素组成。 优选的体内成像模式是正电子发射断层摄影。
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公开(公告)号：US20110002850A1
公开(公告)日：2011-01-06
申请号：US12836926
申请日：2010-07-15
申请人： Thomas Lee Collier , Brian A. Duclos , Umesh B. Gangadharmath , Zhiyong Gao , Farhad Karimi , Dhanalakshmi Kasi , Hartmuth C. Kolb , Qianwa Liang , Henry Clifton Padgett , Joseph C. Walsh , Tieming Zhao
发明人： Thomas Lee Collier , Brian A. Duclos , Umesh B. Gangadharmath , Zhiyong Gao , Farhad Karimi , Dhanalakshmi Kasi , Hartmuth C. Kolb , Qianwa Liang , Henry Clifton Padgett , Joseph C. Walsh , Tieming Zhao
IPC分类号： A61K51/04 , A61P35/00 , A61K31/4178 , C07D403/06
CPC分类号： C07D403/06 , C07B59/002 , C07D403/12
摘要： The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.
摘要翻译： 本发明涉及用于体内检测缺氧性肿瘤或缺血组织的式I的新型放射性标记的生物可降解示踪剂。 在一个实施方案中，示踪剂由2-硝基咪唑部分，三唑，具有药代动力学增强取代基的代谢稳定接头和放射性同位素组成。 优选的体内成像模式是正电子发射断层摄影。
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公开(公告)号：US07977361B2
公开(公告)日：2011-07-12
申请号：US12836926
申请日：2010-07-15
申请人： Thomas Lee Collier , Brian A. Duclos , Umesh B. Gangadharmath , Zhiyong Gao , Farhad Karimi , Dhanalakshmi Kasi , Hartmuth C. Kolb , Qianwa Liang , Henry Clifton Padgett , Joseph C. Walsh , Tieming Zhao
发明人： Thomas Lee Collier , Brian A. Duclos , Umesh B. Gangadharmath , Zhiyong Gao , Farhad Karimi , Dhanalakshmi Kasi , Hartmuth C. Kolb , Qianwa Liang , Henry Clifton Padgett , Joseph C. Walsh , Tieming Zhao
IPC分类号： C07D249/04 , A61K31/4192
CPC分类号： C07D403/06 , C07B59/002 , C07D403/12
摘要： The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.
摘要翻译： 本发明涉及用于体内检测缺氧性肿瘤或缺血组织的式I的新型放射性标记的生物可降解示踪剂。 在一个实施方案中，示踪剂由2-硝基咪唑部分，三唑，具有药代动力学增强取代基的代谢稳定接头和放射性同位素组成。 优选的体内成像模式是正电子发射断层摄影。
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