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1. 发明专利

CA136570A BASEBALL MASK 未知
公开(公告)号：CA136570A
公开(公告)日：1911-10-31
申请号：CA136570D
申请日：1911-10-05
申请人： O'SHEA DENNIS C
发明人： O'SHEA DENNIS C

2. 发明申请

WO2012131037A1 RADIOLABELLED FLUMAZENIL DERIVATIVES 审中-公开
标题翻译：无辐射氟虫腈衍生物
公开(公告)号：WO2012131037A1
公开(公告)日：2012-10-04
申请号：PCT/EP2012/055789
申请日：2012-03-30
申请人： GE HEALTHCARE LIMITED , SOLBAKKEN, Magne , GAETA, Alessandra , O'SHEA, Dennis , JACKSON, Alexander , TRIGG, William, John
发明人： SOLBAKKEN, Magne , GAETA, Alessandra , O'SHEA, Dennis , JACKSON, Alexander , TRIGG, William, John
IPC分类号： C07B59/00 , A61K51/04 , A61K101/02 , C07D487/14
CPC分类号： C07D471/14 , A61K51/0468 , C07B59/002
摘要： A novel 18F- labelled compound suitable for use as a PET tracer for imaging GABA receptors is provided as well as a precursor compound for use in its synthesis and methods for its preparation. Also disclosed herein is an in vivo imaging method comprising administration of said 18F- labelled compound, which finds use in the diagnosis of conditions in which expression of the GABAA receptor is abnormal, or in the monitoring of such conditions.
摘要翻译：提供了适用于成像GABA受体的PET示踪剂的新颖的18F标记的化合物以及用于其合成的前体化合物及其制备方法。本文还公开了一种体内成像方法，其包括施用所述18F-标记的化合物，其用于诊断其中GABA A受体的表达异常的病症或用于监测这些病症。

3. 发明申请

WO2009021947A1 CHELATORS, PARAMAGNETIC CHELATES THEREOF AND THEIR USE AS CONTRAST AGENTS IN MAGNETIC RESONANCE IMAGING (MRI) 审中-公开
标题翻译：螯合剂，顺磁性螯合物及其作为造影剂用于磁共振成像（MRI）
公开(公告)号：WO2009021947A1
公开(公告)日：2009-02-19
申请号：PCT/EP2008/060570
申请日：2008-08-12
申请人： GE HEALTHCARE AS , AXELSSON, Oskar , WADSWORTH, Harry, John , NEWINGTON, Ian, Martin , O'SHEA, Dennis
发明人： AXELSSON, Oskar , WADSWORTH, Harry, John , NEWINGTON, Ian, Martin , O'SHEA, Dennis
IPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07F5/00 , A61K49/10
CPC分类号： C07D401/14 , C07D213/81 , C07D309/40 , C07D407/14
摘要： The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).
摘要翻译：本发明涉及螯合剂，具体涉及能够与顺磁性金属离子形成配合物即顺磁性螯合物的螯合剂。本发明还涉及所述顺磁性螯合物，所述顺磁性螯合物与其他分子连接以及它们在磁共振成像（MRI）中用作造影剂。

4. 发明申请

WO2011117421A1 TRICYCLIC INDOLE DERIVATIVES AS PBR LIGANDS 审中-公开
标题翻译：作为PBR配比的三聚吲哚类衍生物
公开(公告)号：WO2011117421A1
公开(公告)日：2011-09-29
申请号：PCT/EP2011/054744
申请日：2011-03-28
申请人： GE HEALTHCARE LIMITED , ACHANATH, Radha , BALAJI, Srinath , FAIRWAY, Steven, Michael , MANTZILAS, Dimitrios , MOKKAPATI, Umamaheshwar , O'SHEA, Dennis , PASSMORE, Joanna, Marie , SHAN, Bo , TRIGG, William, John , WADSWORTH, Harry, John , KADAVILPPARAMPU MOHAMED, Afsal, Mohammed
发明人： ACHANATH, Radha , BALAJI, Srinath , FAIRWAY, Steven, Michael , MANTZILAS, Dimitrios , MOKKAPATI, Umamaheshwar , O'SHEA, Dennis , PASSMORE, Joanna, Marie , SHAN, Bo , TRIGG, William, John , WADSWORTH, Harry, John , KADAVILPPARAMPU MOHAMED, Afsal, Mohammed
IPC分类号： C07D209/80 , C07D495/04 , A61K51/04
CPC分类号： C07D209/88 , A61K51/0446
摘要： The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation of the PET tracer of the invention and methods for the preparation of said precursor compound and said PET tracer. Also provided by the present invention is a radiopharmaceutical composition comprising the PET tracer of the invention. Methods for using the PET tracer and the radiopharmaceutical composition are also provided.
摘要翻译：本发明提供了与已知的这种PET示踪剂相比具有改进的外周苯并二氮杂受体（PBR）成像的特性的PET示踪剂。本发明还提供了可用于制备本发明的PET示踪剂的前体化合物和用于制备所述前体化合物和所述PET示踪剂的方法。本发明还提供了包含本发明的PET示踪剂的放射性药物组合物。还提供了使用PET示踪剂和放射性药物组合物的方法。

5. 发明申请

WO2008085064A3 HYDROXYPYRIDINONE CHELATING AGENTS, THEIR METAL COMPLEXES AND THEIR USE AS MRI CONTRAST AGENTS 审中-公开
公开(公告)号：WO2008085064A3
公开(公告)日：2008-07-17
申请号：PCT/NO2008/000012
申请日：2008-01-11
申请人： GE HEALTHCARE AS , WADSWORTH, Harry, John , NEWINGTON, Ian, Martin , JONES, Clare, L. , EWAN, Amanda , O'SHEA, Dennis
发明人： WADSWORTH, Harry, John , NEWINGTON, Ian, Martin , JONES, Clare, L. , EWAN, Amanda , O'SHEA, Dennis
IPC分类号： C07D213/81 , A61K49/10
摘要： The present invention relates to chelating agents, in particular to chelating agents which are capable of forming complexes with paramagnetic metal ions such as iron (III) and gadolinium (III). The invention also relates to the complexes formed and their use as MRI contrast agents.

6. 发明申请

WO1995033747A1 NOVEL 1,1-BIS(HETEROAZOLYL)ALKANE DERIVATIVES AND THEIR USE AS NEUROPROTECTIVE AGENTS 审中-公开
标题翻译：新型1,1-BIS（HETEROAZOLYL）ALKANE衍生物及其作为神经保护剂
公开(公告)号：WO1995033747A1
公开(公告)日：1995-12-14
申请号：PCT/SE1995000604
申请日：1995-05-29
申请人： ASTRA AKTIEBOLAG , BOAR, Bernard, Robin , GRAY, Duncan, Alastair , O'SHEA, Dennis, Mark
发明人： ASTRA AKTIEBOLAG
IPC分类号： C07D417/06
CPC分类号： C07D263/32 , A61K31/427 , C07D277/24 , C07D277/28
摘要： The present invention relates to novel heterocyclic compounds having general formula (1), wherein: X1 and X2 are independently O, S or Se; Y1 and Y2 are independently C or N with the proviso that at least one of Y1 and Y2 is N; Y3 and Y4 are independently C or N with the proviso that at least one of Y3 and Y4 is N; R1 and R2 each represent one or more groups independently selected from H, lower alkyl, lower alkoxy-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl or CF3; and A is (a) or (b) geometrical and optical isomers and racemates thereof where such isomers exist, as well as pharmaceutically acceptable acid addition salts thereof and solvates thereof; having therapeutic activity, processes and intermediates for their preparation, pharmaceutical formulations containing said compounds and the medicinal use of said compounds.
摘要翻译：本发明涉及具有通式（1）的新型杂环化合物，其中：X 1和X 2独立地为O，S或Se; Y1和Y2独立地为C或N，条件是Y1和Y2中的至少一个为N; Y 3和Y 4独立地为C或N，条件是Y 3和Y 4中的至少一个为N; R 1和R 2各自表示一个或多个独立地选自H，低级烷基，低级烷氧基 - 低级烷基，羟基 - 低级烷基，低级酰氧基 - 低级烷基或CF 3的基团; 和A是（a）或（b）其中存在这些异构体的几何和光学异构体及其外消旋体，以及其药学上可接受的酸加成盐和溶剂合物; 具有治疗活性，其制备方法和中间体，含有所述化合物的药物制剂和所述化合物的医药用途。

7. 发明申请

WO1994029272A1 1-SUBSTITUTED ISATIN AND OXINDOLE DERIVATIVES AS INHIBITORS OF ACETYLCHOLINESTERASE 审中-公开
标题翻译：作为乙酰胆碱酯酶抑制剂的1-取代的ISATIN和氧化衍生物
公开(公告)号：WO1994029272A1
公开(公告)日：1994-12-22
申请号：PCT/SE1994000448
申请日：1994-05-13
申请人： ASTRA AKTIEBOLAG , BOAR, Bernard, Robin , O'SHEA, Dennis, Mark , TOMLINSON, Ian, David
发明人： ASTRA AKTIEBOLAG
IPC分类号： C07D209/34
CPC分类号： C07D491/10 , C07D209/34 , C07D209/38
摘要： The present invention relates to novel compounds having general formula (1) wherein n is 3, 4, 5, 6 or 7; X represents one or more substituents independently selected from hydrogen, lower alkyl, aryl, lower alkoxy, halogen, trifluoromethyl, nitro, -NHCOR where R is lower alkyl or aryl, -NR1R2 where R1 and R2 are independently hydrogen or lower alkyl or together form a ring, or cycloalkyl, cycloalkenyl or bicycloalkyl either optionally further substituted by lower alkyl; Y is (a) or (b) where R3 and R4 are independently hydrogen, lower alkyl, lower alkoxy or together form a cyclic acetal; Z is lower alkyl; and W represents one or more substituents independently selected from hydrogen, lower alkyl, lower alkoxy or halogen; stereo and optical isomers and racemates thereof where such isomers exist, as well as pharmaceutically acceptable acid addition salts thereof and solvates thereof having therapeutic activity, intermediates for their preparation, processes for their preparation, pharmaceutical formulations containing said compounds and medicinal use of said compounds.
摘要翻译：本发明涉及具有通式（1）的新化合物，其中n为3,4,5,6或7; X表示一个或多个独立地选自氢，低级烷基，芳基，低级烷氧基，卤素，三氟甲基，硝基，-NHCOR的取代基，其中R是低级烷基或芳基，-NR1R2，其中R1和R2独立地是氢或低级烷基或一起形成环或环烷基，任选进一步被低级烷基取代的环烯基或二环烷基; Y是（a）或（b），其中R 3和R 4独立地是氢，低级烷基，低级烷氧基或一起形成环缩醛; Z是低级烷基; W表示一个或多个独立地选自氢，低级烷基，低级烷氧基或卤素的取代基; 其中存在这些异构体的立体和旋光异构体及其外消旋体，以及其药学上可接受的酸加成盐和具有治疗活性的溶剂合物，其制备中间体，其制备方法，含有所述化合物的药物制剂和所述化合物的药用。

8. 发明申请

WO2011073304A1 ARYLOXYANILIDE IMAGING AGENTS 审中-公开
标题翻译： ARYLOXYANILIDE成像剂
公开(公告)号：WO2011073304A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069866
申请日：2010-12-16
申请人： GE HEALTHCARE LIMITED , WADSWORTH, Harry John , O'SHEA, Dennis
发明人： WADSWORTH, Harry John , O'SHEA, Dennis
IPC分类号： A61K51/04 , A61K101/00
CPC分类号： A61K51/0423 , A61K51/0419 , A61K51/0425 , B01L3/52 , C07D307/79 , C07D307/81 , C07D317/46 , C07D317/58 , C07D319/18 , C07D321/10
摘要： The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
摘要翻译：本发明提供适用于体内成像的新型放射性标记的芳氧基亚胺衍生物。与已知的芳氧基亚胺衍生物体内显像剂相比，本发明的体内显像剂具有更好的体内成像性能。本发明的体内显像剂与外用苯并二氮杂受体（PBR）具有良好的选择性结合，结合良好的脑摄取和给予受试者后的体内动力学。

9. 发明申请

WO2010037851A2 IMAGING NEUROINFLAMMATION 审中-公开
标题翻译：成像神经炎症
公开(公告)号：WO2010037851A2
公开(公告)日：2010-04-08
申请号：PCT/EP2009/062827
申请日：2009-10-02
申请人： GE HEALTHCARE LIMITED , WADSWORTH, Harry, John , SHAN, Bo , O'SHEA, Dennis , PASSMORE, Joanne, Marie , TRIGG, William, John
发明人： WADSWORTH, Harry, John , SHAN, Bo , O'SHEA, Dennis , PASSMORE, Joanne, Marie , TRIGG, William, John
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , A61K51/0446
摘要： The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
摘要翻译：本发明涉及体内成像，特别是周边苯二氮卓受体（PBR）的体内成像。提供四环吲哚体内显像剂，其以高亲和力结合PBR，在给药后具有良好的摄入脑中，并优先与表达较高水平PBR的组织结合。本发明还提供了可用于合成本发明的体内显像剂的前体化合物，以及包含使用所述前体化合物的所述体内显像剂的合成方法和用于实施所述方法的试剂盒。还提供了用于体内成像剂的自动合成的盒。此外，本发明提供了包含本发明的体内显像剂的放射性药物组合物，以及使用所述体内成像剂的方法。

10. 发明申请

WO2009021948A1 CHELATORS, PARAMAGNETIC CHELATES THEREOF AND THEIR USE AS CONTRAST AGENTS IN MAGNETIC RESONANCE IMAGING (MRI) 审中-公开
标题翻译：引证文献，参考文献及其作为磁共振成像（MRI）的对比剂使用
公开(公告)号：WO2009021948A1
公开(公告)日：2009-02-19
申请号：PCT/EP2008/060572
申请日：2008-08-12
申请人： GE HEALTHCARE AS , WADSWORTH, Harry, John , NEWINGTON, Ian, Martin , O'SHEA, Dennis
发明人： WADSWORTH, Harry, John , NEWINGTON, Ian, Martin , O'SHEA, Dennis
IPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07F5/00 , A61K49/10
CPC分类号： C07D213/69 , C07D309/40 , C07D401/14 , C07D405/14
摘要： The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).
摘要翻译：本发明涉及螯合剂，特别涉及能够与顺磁性金属离子形成络合物即顺磁性螯合物的螯合剂。本发明还涉及所述顺磁性螯合物，所述顺磁性螯合物与其它分子连接，以及它们在磁共振成像（MRI）中作为造影剂的用途。

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