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1. 发明申请

WO2009134405A3 SUBSTRATE BASED PET IMAGING AGENTS 审中-公开
公开(公告)号：WO2009134405A3
公开(公告)日：2009-11-05
申请号：PCT/US2009/002659
申请日：2009-04-30
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , KOLB, Hartmuth, C. , WALSH, Joseph, C. , CHEN, Kai , GANGADHARMATH, Umesh, B. , CHEN, Gang , MOCHARLA, Vani, P. , KASI, Dhanalakshmi , SCOTT, Peter, J.H. , LIANG, Qianwa
发明人： KOLB, Hartmuth, C. , WALSH, Joseph, C. , CHEN, Kai , GANGADHARMATH, Umesh, B. , CHEN, Gang , MOCHARLA, Vani, P. , KASI, Dhanalakshmi , SCOTT, Peter, J.H. , LIANG, Qianwa
IPC分类号： A61K51/08 , A61P1/00
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)

2. 发明申请

WO2008124703A3 DEVELOPMENT OF MOLECULAR IMAGING PROBES FOR CARBONIC ANHYDRASE-IX USING CLICK CHEMISTRY 审中-公开
标题翻译：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：WO2008124703A3
公开(公告)日：2009-02-05
申请号：PCT/US2008059599
申请日：2008-04-07
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH C , WALSH JOSEPH C , KASI DHANALAKSHMI , MOCHARLA VANI , WANG BING , GANGADHARMATH UMESH B , DUCLOS BRIAN A , CHEN KAI , ZHANG WEI , CHEN GANG , PADGETT HENRY CLIFTON , KARIMI FARHAD , SCOTT PETER J H , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , ZHAO TIEMING , XIA CHUNFANG
发明人： KOLB HARTMUTH C , WALSH JOSEPH C , KASI DHANALAKSHMI , MOCHARLA VANI , WANG BING , GANGADHARMATH UMESH B , DUCLOS BRIAN A , CHEN KAI , ZHANG WEI , CHEN GANG , PADGETT HENRY CLIFTON , KARIMI FARHAD , SCOTT PETER J H , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , ZHAO TIEMING , XIA CHUNFANG
IPC分类号： C07D249/04 , A61K31/4192 , A61P35/00 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D417/14 , G01N33/532
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。

3. 发明申请

WO2004087061B1 TUBULIN BINDING AGENTS AND CORRESPONDING PRODRUG CONSTRUCTS 审中-公开
标题翻译：管IN ING ING ING。。。。。。。。。。。。。。
公开(公告)号：WO2004087061B1
公开(公告)日：2005-05-12
申请号：PCT/US2004009417
申请日：2004-03-26
申请人： OXIGENE INC , UNIV BAYLOR , PINNEY KEVIN G , MOCHARLA VANI P , CHEN ZHI , GARNER CHARLES M , GHATAK ANJAN , HADIMANI MALLINATH , KESSLER JIMMY , DORSEY JAMES M , EDVARDSON KLAUS , CHAPLIN DAVID J , PREZIOSO JOSEPH , JELINEK CHRISTOPHER
发明人： PINNEY KEVIN G , MOCHARLA VANI P , CHEN ZHI , GARNER CHARLES M , GHATAK ANJAN , HADIMANI MALLINATH , KESSLER JIMMY , DORSEY JAMES M , EDVARDSON KLAUS , CHAPLIN DAVID J , PREZIOSO JOSEPH , JELINEK CHRISTOPHER
IPC分类号： A61K20060101 , A61K31/075 , C07C41/00 , C07C43/215 , C07C43/23 , C07C45/51 , C07C45/64 , C07C49/84 , C07C205/45 , C07C217/84 , C07C217/94 , C07C225/22 , C07D233/54 , C07D307/80 , C07D307/81 , C07D333/56 , C07D333/64 , C07F9/12 , C07F9/18 , C07F9/24 , C07F9/655 , C07F9/6553
CPC分类号： C07C43/23 , A61K31/075 , A61K31/66 , C07C43/215 , C07C45/512 , C07C45/64 , C07C45/673 , C07C49/755 , C07C49/84 , C07C205/37 , C07C205/45 , C07C217/84 , C07C217/94 , C07C223/06 , C07C225/22 , C07C237/08 , C07C2602/08 , C07C2602/10 , C07D307/80 , C07D307/81 , C07D333/56 , C07D333/64 , C07F9/12 , C07F9/18 , C07F9/247 , C07F9/65517 , C07F9/655354
摘要： A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.
摘要翻译：已经发现了各种各样的微管蛋白结合剂，其结构特征在于一般意义上是能够维持适于分子识别微管蛋白的芳基 - 芳基，伪π层叠距离的半刚性分子框架。在酚类或氨基形式中，这些配体可进一步官能化以制备能够显示肿瘤细胞脉管系统的选择性靶向和破坏的磷酸酯，磷酸盐，氨基磷酸酯和其它前体药物。

4. 发明申请

WO2012021882A2 FORMULATION, APPARATUS AND METHOD FOR STABILIZING RADIOPHARMACEUTICALS 审中-公开
标题翻译：用于稳定放射性药物的配方，装置和方法
公开(公告)号：WO2012021882A2
公开(公告)日：2012-02-16
申请号：PCT/US2011/047717
申请日：2011-08-15
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , WALSH, Joseph C. , KOLB, Hartmuth C. , MOCHARLA, Vani P. , MU, Fanrong , GANGADHARMATH, Umesh B.
发明人： WALSH, Joseph C. , KOLB, Hartmuth C. , MOCHARLA, Vani P. , MU, Fanrong , GANGADHARMATH, Umesh B.
IPC分类号： A61K51/12 , A61K47/00
CPC分类号： A61K51/121 , A61J1/065 , A61K9/0019 , A61K47/02 , A61K47/12 , A61K51/0402 , A61K51/0453 , A61K51/0455 , A61K51/0459 , A61K51/0491 , A61K51/1282 , B65D81/2069
摘要： A formulation for stabilizing a radiopharmaceutical. The formulation includes a radiopharmaceutical (or a pharmaceutically acceptable salt thereof), a gas which has oxygen, a stabilizer, and a solvent.
摘要翻译：用于稳定放射性药物的配方。该制剂包括放射性药物（或其药学上可接受的盐），具有氧气的气体，稳定剂和溶剂。

5. 发明申请

WO2009148554A1 ACHIEVEMENT OF HIGH THERAPEUTIC INDEX THROUGH MOLECULAR IMAGING GUIDED TARGETED DRUG TREATMENT 审中-公开
标题翻译：通过分子成像指导的药物治疗实现高效治疗指标
公开(公告)号：WO2009148554A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/003309
申请日：2009-06-01
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , KOLB, Hartmuth, C. , WALSH, Joseph, C. , CHEN, Kai , KASI, Dhanalakshmi , GANGADHARMATH, Umesh, B. , SCOTT, Peter, J.h. , CHEN, Gang , MOCHARLA, Vani, P.
发明人： KOLB, Hartmuth, C. , WALSH, Joseph, C. , CHEN, Kai , KASI, Dhanalakshmi , GANGADHARMATH, Umesh, B. , SCOTT, Peter, J.h. , CHEN, Gang , MOCHARLA, Vani, P.
IPC分类号： A61K51/08 , 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。

6. 发明申请

WO2006116736A3 A METHOD FOR THE PREPARATION OF IMAGING PROBES USING CLICK CHEMISTRY 审中-公开
标题翻译：使用单一化学制备成像探针的方法
公开(公告)号：WO2006116736A3
公开(公告)日：2007-02-01
申请号：PCT/US2006016428
申请日：2006-04-27
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH C , MOCHARLA VANI P , WALSH JOSEPH C
发明人： KOLB HARTMUTH C , MOCHARLA VANI P , WALSH JOSEPH C
IPC分类号： G01N33/534 , G01N33/532
CPC分类号： G01N33/532 , A61K51/0453 , A61K51/0455 , G01N33/533 , G01N33/534 , G01N2800/2821
摘要： The invention provides a method for identifying a candidate imaging probe, the method comprising: a) contacting a first library of candidate compounds with a target biomacromolecule, b) identifying a first member from the first library exhibiting affinity for the first binding site; c) contacting the first member identified from the first library affinity for the first binding site with the target biomacromolecule; d) contacting a second library of candidate compounds with the first member and the target biomacromolecule, e) reacting the complementary first functional group with the second functional group via a biomacromolecule induced click chemistry reaction to form the candidate imaging probe; f) isolating and identifying the candidate imaging probe; g) preparing the candidate imaging probe by chemical synthesis; and h) for imaging applications, converting the candidate imaging probe into an imaging probe.
摘要翻译：本发明提供了一种用于鉴定候选成像探针的方法，所述方法包括：a）使候选化合物的第一文库与靶生物大分子接触，b）鉴定第一个文库对第一结合位点表现出亲和性; c）将从第一文库鉴定的第一结合位点与第一结合位点接触的目标生物大分子; d）使候选化合物的第二文库与第一成员和靶生物大分子接触，e）通过生物大分子诱导的点击化学反应使互补的第一官能团与第二官能团反应以形成候选成像探针; f）分离和识别候选成像探针; g）通过化学合成制备候选成像探针; 和h）用于成像应用，将候选成像探针转换成成像探针。

7. 发明申请

WO2006116736A2 IN SITU CLICK CHEMISTRY METHOD FOR SCREENING HIGH AFFINITY MOLECULAR IMAGING PROBES 审中-公开
标题翻译：用于筛选高亲和力分子成像探针的现场点击化学方法
公开(公告)号：WO2006116736A2
公开(公告)日：2006-11-02
申请号：PCT/US2006/016428
申请日：2006-04-27
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , KOLB, Hartmuth, C. , MOCHARLA, Vani, P. , WALSH, Joseph, C.
发明人： KOLB, Hartmuth, C. , MOCHARLA, Vani, P. , WALSH, Joseph, C.
IPC分类号： G01N33/534 , G01N33/532
CPC分类号： G01N33/532 , A61K51/0453 , A61K51/0455 , G01N33/533 , G01N33/534 , G01N2800/2821
摘要： The invention provides a method for identifying a candidate imaging probe, the method comprising: a) contacting a first library of candidate compounds with a target biomacromolecule, b) identifying a first member from the first library exhibiting affinity for the first binding site; c) contacting the first member identified from the first library affinity for the first binding site with the target biomacromolecule; d) contacting a second library of candidate compounds with the first member and the target biomacromolecule, e) reacting the complementary first functional group with the second functional group via a biomacromolecule induced click chemistry reaction to form the candidate imaging probe; f) isolating and identifying the candidate imaging probe; g) preparing the candidate imaging probe by chemical synthesis; and h) for imaging applications, converting the candidate imaging probe into an imaging probe.
摘要翻译：本发明提供了一种用于鉴定候选成像探针的方法，所述方法包括：a）使候选化合物的第一文库与靶生物大分子接触，b）鉴定第一个文库对第一结合位点表现出亲和性; c）将从第一文库鉴定的第一结合位点与第一结合位点接触的目标生物大分子; d）使候选化合物的第二文库与第一成员和靶生物大分子接触，e）通过生物大分子诱导的点击化学反应使互补的第一官能团与第二官能团反应以形成候选成像探针; f）分离和识别候选成像探针; g）通过化学合成制备候选成像探针; 和h）用于成像应用，将候选成像探针转换成成像探针。

8. 发明申请

WO2010111303A2 IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 审中-公开
标题翻译：用于检测神经疾病的成像剂
公开(公告)号：WO2010111303A2
公开(公告)日：2010-09-30
申请号：PCT/US2010028360
申请日：2010-03-23
申请人： SIEMENS MEDICAL SOLUTIONS , GANGADHARMATH UMESH B , KOLB HARTMUTH C , SCOTT PETER J H , WALSH JOSEPH C , ZHANG WEI , SZARDENINGS ANNA KATRIN , SINHA ANJANA , CHEN GANG , WANG ERIC , MOCHARLA VANI P , YU CHUL , LIU CHANGHUI , CASHION DANIEL KURT , KASI DHANALAKSHMI
发明人： GANGADHARMATH UMESH B , KOLB HARTMUTH C , SCOTT PETER J H , WALSH JOSEPH C , ZHANG WEI , SZARDENINGS ANNA KATRIN , SINHA ANJANA , CHEN GANG , WANG ERIC , MOCHARLA VANI P , YU CHUL , LIU CHANGHUI , CASHION DANIEL KURT , KASI DHANALAKSHMI
IPC分类号： A61K51/04 , C07B59/00 , C07D215/00 , C07D235/04 , C07D263/52 , C07D277/62
CPC分类号： A61K51/0455 , A61K51/04 , A61K51/0453 , A61K51/0459 , A61K51/0463 , C07B59/002 , C07D215/06 , C07D235/14 , C07D277/62 , C07D401/04 , C07D403/06 , C07D413/10 , C07D413/14 , C07D487/04
摘要： Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering ti a patient in need compounds of formula (I) capable of binding to tau proteins and ß-amyloid peptides are presented herein. The invention also relates to methods of imaging Aß and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disoders.
摘要翻译：式（I）的成像剂和用于检测神经障碍的方法包括给予需要能够结合tau蛋白和β-淀粉样蛋白肽的式（I）化合物的化合物。本发明还涉及成像Aβ和tau聚集体的方法，包括引入可检测量的包含放射性标记的式（I）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。这些方法和组合使得AD和其他神经系统解剖器的临床前诊断和监测进展。

9. 发明申请

WO2010011964A3 IMAGING AGENTS USEFUL FOR IDENTIFYING AD PATHOLOGY 审中-公开
标题翻译：成像剂有助于鉴别AD病理
公开(公告)号：WO2010011964A3
公开(公告)日：2010-08-26
申请号：PCT/US2009051748
申请日：2009-07-24
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH C , WALSH JOSEPH C , ZHANG WEI , GANGADHARMATH UMESH B , KASI DHANALAKSHMI , CHEN KAI , SINHA ANJANA , WANG ERIC , CHEN GANG , MOCHARLA VANI P , SCOTT PETER J H , PADGETT HENRY CLIFTON , LIANG QIANWA , GAO ZHIYONG , ZHAO TIEMING , XIA CHUNFANG
发明人： KOLB HARTMUTH C , WALSH JOSEPH C , ZHANG WEI , GANGADHARMATH UMESH B , KASI DHANALAKSHMI , CHEN KAI , SINHA ANJANA , WANG ERIC , CHEN GANG , MOCHARLA VANI P , SCOTT PETER J H , PADGETT HENRY CLIFTON , LIANG QIANWA , GAO ZHIYONG , ZHAO TIEMING , XIA CHUNFANG
IPC分类号： A61K51/04 , C07D498/14 , C07D513/04 , C07D513/14
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化学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。根据本发明的结合淀粉样蛋白的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，并区分具有淀粉样蛋白沉积物的神经组织和正常神经组织。本发明的淀粉状蛋白探针可用于检测和定量疾病中的淀粉状蛋白沉积物，所述疾病包括例如唐氏综合征，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。本文还提供了使化合物分布到脑组织中并使脑组织成像的方法，其中所述化合物与与正常对照水平的结合相比，脑组织指示该哺乳动物患有神经退行性疾病或处于发展神经退行性疾病的风险中。

10. 发明申请

WO2010011964A2 IMAGING AGENTS USEFUL FOR IDENTIFYING AD PATHOLOGY 审中-公开
标题翻译：成像代理有助于识别广泛的病理学
公开(公告)号：WO2010011964A2
公开(公告)日：2010-01-28
申请号：PCT/US2009/051748
申请日：2009-07-24
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , KOLB, Hartmuth, C. , WALSH, Joseph, C. , ZHANG, Wei , GANGADHARMATH, Umesh B. , KASI, Dhanalakshmi , CHEN, Kai , SINHA, Anjana , WANG, Eric , CHEN, Gang , MOCHARLA, Vani, P. , SCOTT, Peter J.H. , PADGETT, Henry, Clifton , LIANG, Qianwa , GAO, Zhiyong , ZHAO, Tieming , XIA, Chunfang
发明人： KOLB, Hartmuth, C. , WALSH, Joseph, C. , ZHANG, Wei , GANGADHARMATH, Umesh B. , KASI, Dhanalakshmi , CHEN, Kai , SINHA, Anjana , WANG, Eric , CHEN, Gang , MOCHARLA, Vani, P. , SCOTT, Peter J.H. , PADGETT, Henry, Clifton , LIANG, Qianwa , GAO, Zhiyong , ZHAO, Tieming , XIA, Chunfang
IPC分类号： A61K51/04 , C07D498/14 , C07D513/04 , C07D513/14
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于脑组织和成像脑组织的方法，其中化合物与脑组织与正常对照水平的结合相比表明哺乳动物患有或有发展为神经变性疾病的风险。

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