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公开(公告)号：US09005577B2
公开(公告)日：2015-04-14
申请号：US12433211
申请日：2009-04-30
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Umesh B. Gangadharmath , Gang Chen , Vani P. Mocharla , Dhanalakshmi Kasi , Peter J. H. Scott , Qianwa Liang
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Umesh B. Gangadharmath , Gang Chen , Vani P. Mocharla , Dhanalakshmi Kasi , Peter J. H. Scott , Qianwa Liang
CPC分类号： A61K51/088 , G01N33/60 , G01N2333/96466
摘要： The present application is directed to radiolabeled imaging agents comprising a radiolabel, and a substrate, pharmaceutical compositions comprising radiolabeled imaging agents, and methods of using the radiolabeled imaging agents. The present application is further directed to methods of preparing the radiolabeled imaging agent. Such imaging agents can used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
摘要翻译： 本申请涉及包含放射性标记和底物，包含放射性标记的成像剂的药物组合物的放射性标记的成像剂，以及使用放射性标记的成像剂的方法。 本申请进一步涉及制备放射性标记的成像剂的方法。 这些成像剂可用于成像研究，例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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3.发明授权Achievement of a high therapeutic index through molecular imaging guided targeted drug treatment 有权通过分子成像实现高治疗指标，引导靶向药物治疗公开(公告)号：US08293206B2
公开(公告)日：2012-10-23
申请号：US12455346
申请日：2009-06-01
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Dhanalakshmi Kasi , Umesh B. Gangadharmath , Peter J. H. Scott , Gang Chen , Vani P. Mocharla
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Dhanalakshmi Kasi , Umesh B. Gangadharmath , Peter J. H. Scott , Gang Chen , Vani P. Mocharla
CPC分类号： A61K51/088 , A61K51/082
摘要： The present disclosure provides methods for treating cancer in a patient in need of such treatment, the method includes prequalifying a patient's therapeutic treatment by performing a molecular imaging procedure to the patient using a labeled biomarker specific for a cancer target at the tumor site; and administering a therapeutic effective amount of a compound comprising a targeting agent linked to a chemotherapeutic or a targeting agent linked to an antibody. Embodiments of the present invention also include compounds and compositions for using such methods.
摘要翻译： 本公开提供了在需要这种治疗的患者中治疗癌症的方法，所述方法包括通过使用在肿瘤部位对癌症靶标特异的标记的生物标志物向患者进行分子成像程序来资格评估患者的治疗性治疗; 以及施用治疗有效量的包含连接于与抗体连接的化学治疗剂或靶向剂的靶向剂的化合物。 本发明的实施方案还包括使用这些方法的化合物和组合物。
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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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5.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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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：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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公开(公告)号：US20100074843A1
公开(公告)日：2010-03-25
申请号：US12433211
申请日：2009-04-30
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Umesh B. Gangadharmath , Gang Chen , Vani P. Mocharla , Dhanalakshmi Kasi , Peter J.H. Scott , Qianwa Liang
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Umesh B. Gangadharmath , Gang Chen , Vani P. Mocharla , Dhanalakshmi Kasi , Peter J.H. Scott , Qianwa Liang
CPC分类号： A61K51/088 , G01N33/60 , G01N2333/96466
摘要： The present application is directed to radiolabeled imaging agents comprising a radiolabel, and a substrate, pharmaceutical compositions comprising radiolabeled imaging agents, and methods of using the radiolabeled imaging agents. The present application is further directed to methods of preparing the radiolabeled imaging agent. Such imaging agents can used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
摘要翻译： 本申请涉及包含放射性标记和底物，包含放射性标记的成像剂的药物组合物的放射性标记的成像剂，以及使用放射性标记的成像剂的方法。 本申请进一步涉及制备放射性标记的成像剂的方法。 这些成像剂可用于成像研究，例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：US20120302755A1
公开(公告)日：2012-11-29
申请号：US13477095
申请日：2012-05-22
申请人： Anna Katrin Szardenings , Hartmuth C. Kolb , Joseph C. Walsh , Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Changhui Liu , Anjana Sinha , Eric Wang , Chul Yu , Wei Zhang , Kai Chen , Vani P. Mocharla , Peter J.H. Scott
发明人： Anna Katrin Szardenings , Hartmuth C. Kolb , Joseph C. Walsh , Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Changhui Liu , Anjana Sinha , Eric Wang , Chul Yu , Wei Zhang , Kai Chen , Vani P. Mocharla , Peter J.H. Scott
IPC分类号： C07D471/04 , C07D471/14
CPC分类号： A61K51/0455 , A61K51/0446 , C07B59/002 , C07D471/04 , C07D471/14
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 carbazoles and derivatives thereof 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倾向于其的化合物和方法，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咔唑及其衍生物，以及 三唑衍生物，允许化合物分布到脑组织中并对脑组织进行成像，其中与正常对照水平的结合相比，化合物与脑组织的结合增加表明哺乳动物患有或处于危险中 发展为阿尔茨海默病。
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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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10.发明申请Achievement of a high therapeutic index through molecular imaging guided targeted drug treatment 有权通过分子成像实现高治疗指标，引导靶向药物治疗公开(公告)号：US20100074910A1
公开(公告)日：2010-03-25
申请号：US12455346
申请日：2009-06-01
申请人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Dhanalakshmi Kasi , Umesh B. Gangadharmath , Peter J.H. Scott , Gang Chen , Vani P. Mocharla
发明人： Hartmuth C. Kolb , Joseph C. Walsh , Kai Chen , Dhanalakshmi Kasi , Umesh B. Gangadharmath , Peter J.H. Scott , Gang Chen , Vani P. Mocharla
IPC分类号： A61K39/395 , C07K14/00 , C07K16/00 , A61K38/16 , A61P35/00
CPC分类号： A61K51/088 , A61K51/082
摘要： The present disclosure provides methods for treating cancer in a patient in need of such treatment, the method includes prequalifying a patient's therapeutic treatment by performing a molecular imaging procedure to the patient using a labeled biomarker specific for a cancer target at the tumor site; and administering a therapeutic effective amount of a compound comprising a targeting agent linked to a chemotherapeutic or a targeting agent linked to an antibody. Embodiments of the present invention also include compounds and compositions for using such methods.
摘要翻译： 本公开提供了在需要这种治疗的患者中治疗癌症的方法，所述方法包括通过使用在肿瘤部位对癌症靶标特异的标记的生物标志物向患者进行分子成像程序来资格评估患者的治疗性治疗; 以及施用治疗有效量的包含连接于与抗体连接的化学治疗剂或靶向剂的靶向剂的化合物。 本发明的实施方案还包括使用这些方法的化合物和组合物。
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