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1. 发明申请

WO2009102498A1 NOVEL IMAGING AGENTS FOR DETECTING NEUROLOGICAL DYSFUNCTION 审中-公开
标题翻译：用于检测神经功能障碍的新型成像剂
公开(公告)号：WO2009102498A1
公开(公告)日：2009-08-20
申请号：PCT/US2009/000961
申请日：2009-02-17
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , KOLB, Hartmuth C. , WALSH, Joseph C. , LIANG, Qianwa , DUCLOS, Brian A. , ZHANG, Wei , SCOTT, Peter J.h. , CHEN, Kai , GAO, Zhiyong , ZHAO, Tieming , MOCHARLA, Vani P. , KASI, Dhanalakshmi , CHEN, Gang , WANG, Eric , SINHA, Anjana , XIA, Chunfang , PADGETT, Henry Clifton , KARIMI, Farhad
发明人： KOLB, Hartmuth C. , WALSH, Joseph C. , LIANG, Qianwa , DUCLOS, Brian A. , ZHANG, Wei , SCOTT, Peter J.h. , CHEN, Kai , GAO, Zhiyong , ZHAO, Tieming , MOCHARLA, Vani P. , KASI, Dhanalakshmi , CHEN, Gang , WANG, Eric , SINHA, Anjana , XIA, Chunfang , PADGETT, Henry Clifton , KARIMI, Farhad
IPC分类号： C07B59/00
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

2. 发明申请

WO2008033561A3 CLICK CHEMISTRY-DERIVED CYCLOPEPTIDE DERIVATIVES AS IMAGING AGENTS FOR INTEGRINS 审中-公开
标题翻译：点击化学衍生的循环代谢产物作为成像成像剂
公开(公告)号：WO2008033561A3
公开(公告)日：2008-05-08
申请号：PCT/US2007020175
申请日：2007-09-17
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH , CHEN KAI , WALSH JOSEPH C , LIANG QIANWA , PADGETT HENRY , KARIMI FARHAD
发明人： KOLB HARTMUTH , CHEN KAI , WALSH JOSEPH C , LIANG QIANWA , PADGETT HENRY , KARIMI FARHAD
IPC分类号： A61K51/08
CPC分类号： A61K51/088 , A61K51/082
摘要： The present application is directed to radiolabeled cyclic polypeptides, pharmaceutical compositions comprising radiolabeled cyclic polypeptides, and methods of using the radiolabeled cyclic polypeptides. Such polypeptides 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肽，包含放射性标记的环状多肽的药物组合物，以及使用放射性标记的环状多肽的方法。这样的多肽可用于成像研究，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）。

3. 发明申请

WO2007144725A3 SYNTHESIS AND EVALUATION OF 18F-LABELLED ALKYL-1-[(R)-1-PHENYLETHYL]-1H-IMIDAZOLE-5-CARBOXYLATE AS A TRACER FOR THE QUANTIFICATION OF ß-11-HYDROXYLASE ENZYME IN THE ADRENAL GLANDS 审中-公开
标题翻译： 18F标记的烷基-1 - [（R）-1-苯基] -1H-咪唑-5-羧酸甲酯作为追踪剂的合成和评价，用于定量在ADRNAL GLANDS中的β-11-羟基酶酶
公开(公告)号：WO2007144725A3
公开(公告)日：2008-02-21
申请号：PCT/IB2007001528
申请日：2007-06-07
申请人： GE HEALTHCARE LTD , LANGSTROM BENGT , KARIMI FARHAD , BLOM ELISABETH , ERLANDSSON MARIA
发明人： LANGSTROM BENGT , KARIMI FARHAD , BLOM ELISABETH , ERLANDSSON MARIA
IPC分类号： C07D233/66
CPC分类号： C07D233/66 , C07B2200/05
摘要： Radioactively labeled derivatives of (R)-3-(1-phenylethyl)-3H-imidazole-4-carboxylic acid esters and one-step methods for preparing these compounds are provided. The radioactively labelled compounds, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET) for the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Associated kits and method for PET studies are also provided.
摘要翻译：提供了（R）-3-（1-苯基乙基）-3H-咪唑-4-羧酸酯的放射性标记的衍生物和制备这些化合物的一步法。放射性标记的化合物和药学上可接受的盐和溶剂化物可用作放射性药物，特别是用于正电子发射断层扫描（PET）用于诊断肾上腺皮质肿块如附带瘤，腺瘤，原发性和转移性皮层癌的放射性药物。还提供了关于PET研究的试剂盒和方法。

4. 发明申请

WO2007144725A2 SYNTHESIS AND EVALUATION OF 18F-LABELLED ALKYL-1-[(R)-1-PHENYLETHYL]-1H-IMIDAZOLE-5-CARBOXYLATE AS A TRACER FOR THE QUANTIFICATION OF β-11-HYDROXYLASE ENZYME IN THE ADRENAL GLANDS 审中-公开
标题翻译： 18F标记的烷基-1 - [（R）-1-苯基] -1H-咪唑-5-羧酸甲酯作为追踪剂的合成和评价，用于定量在ADRNAL GLANDS中的β-11-羟基酶酶
公开(公告)号：WO2007144725A2
公开(公告)日：2007-12-21
申请号：PCT/IB2007/001528
申请日：2007-06-07
申请人： GE HEALTHCARE LIMITED , LANGSTROM, Bengt , KARIMI, Farhad , BLOM, Elisabeth , ERLANDSSON, Maria
发明人： LANGSTROM, Bengt , KARIMI, Farhad , BLOM, Elisabeth , ERLANDSSON, Maria
IPC分类号： C07D233/66
CPC分类号： C07D233/66 , C07B2200/05
摘要： Radioactively labeled derivatives of (R)-3-(1-phenylethyl)-3H-imidazole-4-carboxylic acid esters and one-step methods for preparing these compounds are provided. The radioactively labelled compounds, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET) for the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Associated kits and method for PET studies are also provided.
摘要翻译：提供了（R）-3-（1-苯基乙基）-3H-咪唑-4-羧酸酯的放射性标记的衍生物和制备这些化合物的一步法。放射性标记的化合物和药学上可接受的盐和溶剂化物可用作放射性药物，特别是用于正电子发射断层扫描（PET）用于诊断肾上腺皮质肿块如附带瘤，腺瘤，原发性和转移性皮层癌的放射性药物。还提供了关于PET研究的试剂盒和方法。

5. 发明申请

WO2006103509A3 METHODS FOR CARBON ISOTOPE LABELING SYNTHESIS BY TRANSITION METAL-PROMOTED CARBONYLATION VIA KETENE USING DIAZO COMPOUNDS AND CARBON-ISOTOPE MONOXIDE 审中-公开
标题翻译：碳同位素标记方法通过使用DIAZO化合物和碳同位素一氧化碳的KETENE过渡金属促进碳酸化合成
公开(公告)号：WO2006103509A3
公开(公告)日：2007-01-04
申请号：PCT/IB2006000632
申请日：2006-03-22
申请人： GE HEALTHCARE LTD , LANGSTROM BENGT , BARLETTA JULIEN , KARIMI FARHAD , DOI HISASHI
发明人： LANGSTROM BENGT , BARLETTA JULIEN , KARIMI FARHAD , DOI HISASHI
IPC分类号： C07B59/00 , A61K51/00 , C07C67/36 , C07C69/38
CPC分类号： A61K51/0402 , C07B2200/05 , C07C67/36 , C07C69/38
摘要： Methods and reagents for transition metal-promoted carbonylation via diazo compounds using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
摘要翻译：提供了使用碳同位素标记的一氧化碳通过重氮化合物进行过渡金属促进羰基化的方法和试剂。所得碳同位素标记的化合物可用作放射性药物，特别用于正电子发射断层扫描（PET）。还提供了用于PET研究的相关工具包。

6. 发明申请

WO2008124651A2 NITRO-IMIDAZOLE HYPOXIA IMAGING AGENTS 审中-公开
标题翻译： NITRO-IMIDAZOLE HYPOXIA成像剂
公开(公告)号：WO2008124651A2
公开(公告)日：2008-10-16
申请号：PCT/US2008059505
申请日：2008-04-04
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH C , WALSH JOSEPH C , GANGADHARMATH UMESH B , KARIMI FARHAD , PADGETT HENRY CLIFTON , KASI DHANALAKSHMI , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , DUCLOS BRIAN A , ZHAO TIEMING
发明人： KOLB HARTMUTH C , WALSH JOSEPH C , GANGADHARMATH UMESH B , KARIMI FARHAD , PADGETT HENRY CLIFTON , KASI DHANALAKSHMI , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , DUCLOS BRIAN A , ZHAO TIEMING
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）的新型放射性标记生物可还原示踪剂。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。

7. 发明申请

WO2008033557A2 CLICK CHEMISTRY-DERIVED CYCLIC PEPTIDOMIMETICS AS INTEGRIN MARKERS 审中-公开
标题翻译：单击化学衍生的循环多肽标志物作为整体标志物
公开(公告)号：WO2008033557A2
公开(公告)日：2008-03-20
申请号：PCT/US2007020130
申请日：2007-09-17
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH , CHEN KAI , WALSH JOSEPH C , GANGADHARMATH UMESH , KASI DHANALAKSHMI , WANG BING , DUCLOS BRIAN , LIANG QIANWA , PADGETT HENRY CLIFTON , KARIMI FARHAD
发明人： KOLB HARTMUTH , CHEN KAI , WALSH JOSEPH C , GANGADHARMATH UMESH , KASI DHANALAKSHMI , WANG BING , DUCLOS BRIAN , LIANG QIANWA , PADGETT HENRY CLIFTON , KARIMI FARHAD
IPC分类号： C07K5/12 , A61K38/12 , A61P35/00
CPC分类号： C07K7/56
摘要： The present application is directed to radiolabeled cyclic peptidomimetics, pharmaceutical compositions comprising radiolabeled cyclic peptidomimetics, and methods of using the radiolabeled cyclic peptidomimetics. Such peptidomimetics 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肽模拟物，包含放射性标记的环状肽模拟物的药物组合物，以及使用放射性标记的环状拟肽的方法。这样的肽模拟物可用于成像研究，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）。

8. 发明申请

WO2007135541A1 11C-LABELED BENZOPHENONE/BENZOXAZOLE ANALOGUES AS AN INFLAMMATION IMAGING AGENT 审中-公开
标题翻译： 11C标记的苯并噻唑/苯并噻唑类似物作为成像成像剂
公开(公告)号：WO2007135541A1
公开(公告)日：2007-11-29
申请号：PCT/IB2007/001311
申请日：2007-05-21
申请人： GE HEALTHCARE LIMITED , KARIMI, Farhad , LANGSTROM, Bengt
发明人： KARIMI, Farhad , LANGSTROM, Bengt
IPC分类号： C07B59/00 , A61K51/04 , C07C49/83 , C07C49/84 , C07C235/20 , C07C235/24 , C07D263/58
CPC分类号： C07C235/20 , A61K51/04 , A61K51/0453 , A61K51/0455 , C07B59/001 , C07B59/002 , C07B2200/05 , C07C45/49 , C07C49/83 , C07C49/84 , C07C235/24 , C07D263/58
摘要： A method of preparing novel [ 11 C]-labeled benzophenone/bezoxazole analogues is provided. The present invention also provides novel [ 11 C]-labeled benzophenone/bezoxazole analogues prepared from the GMP synthesis method. Kit claims for preparing novel [ 11 C]-labeled benzophenone/bezoxazole analogues and a method of use thereof are also provided.
摘要翻译：提供了制备新的[11β]标记的二苯甲酮/异唑唑类似物的方法。本发明还提供了由GMP合成方法制备的新型的[11 C]标记的二苯甲酮/异唑唑类似物。还提供了制备新型标题化合物二苯甲酮/异唑唑类似物的试剂盒说明书及其使用方法。

9. 发明申请

WO2009073273A3 PERFLUORO-ARYLIODONIUM SALTS IN NUCLEOPHILIC AROMATIC 18F-FLUORINATION 审中-公开
标题翻译：全球芳香18F荧光中的全氟阿魏酸钠盐
公开(公告)号：WO2009073273A3
公开(公告)日：2009-09-17
申请号：PCT/US2008078547
申请日：2008-10-02
申请人： GE HEALTHCARE LTD , MEDI PHYSICS INC , LANGSTROM BENGT , KARIMI FARHAD
发明人： LANGSTROM BENGT , KARIMI FARHAD
IPC分类号： A61K51/04
CPC分类号： A61K51/04 , C07B59/001 , C07B63/00
摘要： The present invention describes using fluorous chemistry in n.c.a. nucleophilic aromatic 18F-fluorination reactions by using perfluoro-aryliodonium salts as a precursor for aromatic nucleophilic substitution using a [18F] F- anion to displace a suitable leaving group from an electron deficient benzene ring. The results showed that using perfluoro-aryliodonium salts as a precursor is a suitable leaving group for n. c. a. nucleophilic aromatic 18F-fluorination in synthesis.. The PT-precursor seems to be quite stable. In an attempt to purify the crude 18F-labeled product using fluorous solid phase extraction (F-SPE), the radio labeled impurities decreased significantly. Thus, it is possible to use this PT methodology to simplify and speed up purification methods.
摘要翻译：本发明描述了在n.c.a中使用氟化学。通过使用全氟芳基碘鎓盐作为芳族亲核取代的前体，使用[18 F] F-阴离子将不合适的离去基团从电子缺乏的苯环置换，进行亲核芳香族18F-氟化反应。结果表明，使用全氟芳基碘鎓盐作为前体是n的合适的离去基团。 C。一个。亲核芳香族18F-氟化合成。PT-前体似乎相当稳定。为了使用氟固相萃取（F-SPE）纯化粗制的18F标记产物，放射性标记的杂质显着降低。因此，可以使用这种PT方法来简化和加速净化方法。

10. 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。

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