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41. 发明申请

WO2008023251A3 RADIOLABELED 1-ACETATE PET IMAGING FOR RADIOTHERAPY IN HEAD AND NECK CANCER 审中-公开
公开(公告)号：WO2008023251A3
公开(公告)日：2008-02-28
申请号：PCT/IB2007/002412
申请日：2007-08-22
申请人： GE HEALTHCARE LIMITED , SORENSEN, Jens , LANGSTROM, Bengt , SUN, Aijun , JOHANSSON, Silvia
发明人： SORENSEN, Jens , LANGSTROM, Bengt , SUN, Aijun , JOHANSSON, Silvia
IPC分类号： A61K51/00 , C07B59/00
摘要： The present invention provides methods of using optimal PET tracers for diagnosing head and neck cancer. Methods for in vivo imaging uses of the PET tracers that are suitable for uses in radiation therapy (RT) in head and neck cancer and evaluation of salivary gland function are also provided. A pharmaceutical comprising the PET tracer and a kit for the preparation of the pharmaceutical are provided as well.

42. 发明申请

WO2007036785A2 CARBON-ISOTOPE MONOXIDE LABELING OF DAA1106 AND ITS ANALOGUES TO BE USED AS TRACERS FOR A PERIPHERAL TYPE BENZODIAZEPINE BINDING SITE 审中-公开
标题翻译： DAA1106的碳同位素一氧化碳标记及其作为外部类型苯并咪唑结合位点的追踪剂的模拟物
公开(公告)号：WO2007036785A2
公开(公告)日：2007-04-05
申请号：PCT/IB2006/002669
申请日：2006-09-26
申请人： GE HEALTHCARE LIMITED , LANGSTROM, Bengt , RAHMAN, Obaidur , BERGSTROM, Mats , ESTRADA, Sergio
发明人： LANGSTROM, Bengt , RAHMAN, Obaidur , BERGSTROM, Mats , ESTRADA, Sergio
IPC分类号： C07B59/00
CPC分类号： C07B59/001
摘要： A potent and selective ligand for peripheral benzodiazepine receptor (PBR), N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide or DAA1106 and eight structurally related analogues were labelled with 11 C at carbonyl position of the molecule using a low concentration of [ 11 C]carbon monoxide and micro autoclave techniques. Palladium mediated carbonylation using tetrakis(triphenylphosphine)palladium, methyl iodide or iodobenzene and different amines was employed in the synthesis. The 11 C-labelled products were obtained with 15-45% decay-corrected radiochemical yields. Specific radioactivity was determined for the compound [carbonyl- 11 C]DAA1106 to investigate the possibility to obtain the high specific radioactivity for the compounds prepared using this method. The obtained specific radioactivity was 121 GBq/µmol, 36 min after a bombardment of 10 µAh. Synthetic routes for the preparation of precursors and reference compounds were also developed. The presented approach is a novel method for the synthesis of [carbonyl- 11 C]DAA1106 and analogues. Accordingly, the synthetic routes for the preparation of precursor amines and reference compounds are provided. A kit claim and a method of use claim for a PET study comprising an effective amount of carbon-isotope labeled compound and pharmaceutically acceptable salts and solvates thereof are also provided.
摘要翻译：对于外周苯并二氮杂受体（PBR），N-（2,5-二甲氧基苄基）-N-（5-氟-2-苯氧基苯基）乙酰胺或DAA1106和八个结构相关的类似物的有效和选择性配体用< /低级C，使用低浓度的[11 C]一氧化碳和微量高压釜技术在分子的羰基位置。在合成中使用四（三苯基膦）钯，甲基碘或碘苯和不同胺的钯介导羰基化。获得了具有15-45％衰变校正的放射化学产率的<！ - SIPO - >标记的产物。测定化合物[羰基-d11C] DAA1106的比放射性，以研究获得使用该方法制备的化合物的高比放射性的可能性。获得的特异放射性为121 GBq /μmol，轰击后10分钟36分钟。还开发了制备前体和参考化合物的合成路线。所提出的方法是合成[羰基-d1A] DAA1106和类似物的新方法。因此，提供了用于制备前体胺和参考化合物的合成路线。还提供了包括有效量的碳同位素标记的化合物及其药学上可接受的盐和溶剂合物的PET研究的试剂盒要求和使用方法。

43. 发明申请

WO2007026217A2 DIAGNOSIS OF WHIPLASH ASSOCIATED DISORDERS (WAD) BY USING PET WITH D-[METHYL-11C]-DEPRENYL (DDE) 审中-公开
标题翻译：通过使用具有D- [甲基-11C] -DEPRENYL（DDE）的PET对WHIPLASH相关疾病（WAD）进行诊断
公开(公告)号：WO2007026217A2
公开(公告)日：2007-03-08
申请号：PCT/IB2006/002358
申请日：2006-08-30
申请人： GE HEALTHCARE LIMITED , ENGLER, Henry , LANGSTROM, Bengt , BERGSTROM, Mats , APPEL, Lieuwe , FREDRIKSON, Mats
发明人： ENGLER, Henry , LANGSTROM, Bengt , BERGSTROM, Mats , APPEL, Lieuwe , FREDRIKSON, Mats
CPC分类号： A61K51/04
摘要： Positron Emission Tomography (PET) tracers such as D-[methyl- 11 C]-Deprenyl (DDE) and [ 11 C]-GR205171 (GLD), methods for and methods of preparing biological mechanisms that identify treatment targets in connection with Whiplash-Associated Disorder (WAD) are provided. Associated kits for the evaluation of the biological mechanisms are also provided.
摘要翻译：正电子发射断层扫描（PET）示踪剂，例如D- [甲基-11 C] - 甲苯基（DDE）和[ - 11C] -GR205171（GLD），其方法和提供了识别与Whiplash相关障碍（WAD）有关的治疗目标的生物学机制的方法。还提供了用于评估生物机制的相关工具包。

44. 发明申请

WO2006134424A2 METHOD FOR THE USE OF [11C] CARBON MONOXIDE IN LABELING SYNTHESIS OF 11C-LABELLED ACIDS BY PHOTO-INDUCED FREE RADICAL CARBONYLATION 审中-公开
标题翻译：使用[11C]一氧化碳通过光诱导自由放射性碳化合物在标记11C标记酸的合成方法
公开(公告)号：WO2006134424A2
公开(公告)日：2006-12-21
申请号：PCT/IB2005/004193
申请日：2005-12-05
申请人： GE HEALTHCARE LIMITED , LANGSTROM, Bengt , ITSENKO, Oleksiy
发明人： LANGSTROM, Bengt , ITSENKO, Oleksiy
IPC分类号： C07B59/00 , C07C51/10 , C07C53/124 , C07C53/126 , C07C53/128 , C07C57/03
CPC分类号： B01J19/0093 , A61K41/00 , A61K51/0402 , B01J2219/00788 , B01J2219/00889 , B01J2219/00936 , B01J2219/00963 , C07B59/001 , C07B2200/05 , C07C51/10 , C07C2603/74 , C07C57/03 , C07C53/124 , C07C61/135 , C07C53/126 , C07C53/128 , C07C59/52 , C07C61/08 , C07C57/30 , C07C55/21
摘要： Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using alkyl/aryl iodides with water pretreated by a base are provided. The resultant carbon-isotope labeled acids are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
摘要翻译：提供了用碳同位素标记的一氧化碳使用烷基/芳基碘化物进行光引发羰基化的方法和试剂，其中预处理水由碱处理。所得的碳同位素标记的酸可用作放射性药物，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。

45. 发明申请

WO2006131803A2 METHOD FOR THE USE OF [11C] CARBON MONOXIDE IN LABELING SYNTHESIS OF 11C-LABELLED ESTERS AND ACIDS BY SENSITIZED PHOTO-INDUCED FREE RADICAL CARBONYLATION 审中-公开
标题翻译：使用[11C]一氧化碳在11C标记的酯和酸的合成中的方法通过敏感的光诱导的自由基碳酸化
公开(公告)号：WO2006131803A2
公开(公告)日：2006-12-14
申请号：PCT/IB2006/001452
申请日：2006-06-05
申请人： GE HEALTHCARE LIMITED , LANGSTROM, Bengt , ITSENKO, Oleksiy
发明人： LANGSTROM, Bengt , ITSENKO, Oleksiy
IPC分类号： C07B59/00 , C07C67/36
CPC分类号： C07B59/001 , C07B2200/05 , C07C51/10 , C07C67/36 , C07C69/612 , C07C69/75 , C07C2601/14 , C07C57/30 , C07C55/21
摘要： Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using alkyl/aryl iodides with alcohols or water treated by photosensitizers are provided. The resultant carbon-isotope labeled esters and acids, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits and method for PET studies are also provided.
摘要翻译：提供了用碳同位素标记的一氧化碳使用烷基/芳基碘化物与醇或通过光敏剂处理的水进行光引发羰基化的方法和试剂。所得的碳同位素标记的酯和酸以及药学上可接受的盐和溶剂合物可用作放射性药物，尤其用于正电子发射断层扫描（PET）。还提供了关于PET研究的试剂盒和方法。

46. 发明申请

WO2006075226A1 11C-LABELED BENZYL-LACTAM COMPOUNDS AND THEIR USE AS IMAGING AGENTS 审中-公开
标题翻译： 11C标记的苯甲酸酯化合物及其作为成像剂的用途
公开(公告)号：WO2006075226A1
公开(公告)日：2006-07-20
申请号：PCT/IB2006/000028
申请日：2006-01-11
申请人： PFIZER PRODUCTS INC. , HELAL, Christopher, John , ANTONI, Gunnar , LANGSTROM, Bengt , SHENG, Jia, Zhi , JAYNES-SOBOLOVE, Susan, Beth , McCARTHY, Timothy, John
发明人： HELAL, Christopher, John , ANTONI, Gunnar , LANGSTROM, Bengt , SHENG, Jia, Zhi , JAYNES-SOBOLOVE, Susan, Beth , McCARTHY, Timothy, John
IPC分类号： C07D207/26 , C07D401/04 , A61K31/4015 , A61P25/00
CPC分类号： C07D207/26 , C07D207/273 , C07D401/04
摘要： The invention relates to "C-labeled compounds, their preparation, compositions comprising an effective amount of a "C-labeled compound, and the use of a "C-labeled compound as a radiopharmaceutical for positron emission tomography.
摘要翻译：本发明涉及“C标记化合物，其制备方法，包含有效量的”C标记化合物“的组合物，以及”C-标记化合物作为正电子发射断层摄影放射性药物“的用途。

47. 发明申请

WO2004089517A1 METHOD OF OBTAINING GALLIUN-68 AND USE THEREOF AND DEVICE FOR CARRYING OUT SAIF METHOD 审中-公开
标题翻译：获得GALLIUN-68的方法及其使用方法和用于执行SAIF方法的装置
公开(公告)号：WO2004089517A1
公开(公告)日：2004-10-21
申请号：PCT/GB2004/001548
申请日：2004-04-08
申请人： AMERSHAM PLC , VELIKYAN, Irina , LANGSTROM, Bengt , BEYER, Gerd, J.
发明人： VELIKYAN, Irina , LANGSTROM, Bengt , BEYER, Gerd, J.
IPC分类号： B01D59/30
CPC分类号： A61K51/088 , A61K51/083 , A61K51/1282 , C22B3/42 , C22B58/00 , G21H5/02 , Y02P10/234
摘要： The present invention relates to a method of obtaining from a 68 Ge/ 68 Ga generator and a method of producing 68 Ga-radiolabelled complexes using the obtained 68 Ga. The invention further relates to a kit, which could be used to obtain 68 Ga and a kit, which could be used for the production of 68 Ga-radiolabelled complexes.
摘要翻译：本发明涉及从68 Ga / 68 Ga发生器获得的方法以及使用所获得的68 Ga制备68 Ga Ga 2放射性标记复合物的方法。本发明还涉及可用于获得68 Ga和试剂盒的试剂盒，该试剂盒可用于生产68 Ga放射性标记的复合物。

48. 发明申请

WO2004089425A1 MICROWAVE METHOD FOR PREPARING RADIOLABELLED GALLIUM COMPLEXES 审中-公开
标题翻译：用于制备无定形玻璃复合物的微波方法
公开(公告)号：WO2004089425A1
公开(公告)日：2004-10-21
申请号：PCT/GB2004/001550
申请日：2004-04-08
申请人： AMERSHAM PLC , VELIKYAN, Irina , LANGSTROM, Bengt
发明人： VELIKYAN, Irina , LANGSTROM, Bengt
IPC分类号： A61K51/00
CPC分类号： A61K51/088 , A61K51/0497 , A61K51/083
摘要： The present invention relates to a method of producing radiolabelled gallium complexes that could be used as diagnostic agents, e.g. for positron emission tomography (PET) imaging.
摘要翻译：本发明涉及可用作诊断剂的放射性标记的镓配合物的方法，例如，用于正电子发射断层扫描（PET）成像。

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