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1. 发明授权

US08790619B2 Indole derivatives 有权
标题翻译：吲哚衍生物
公开(公告)号：US08790619B2
公开(公告)日：2014-07-29
申请号：US13258465
申请日：2010-03-26
申请人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
发明人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
IPC分类号： A61K51/00 , A61K36/14
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
摘要： An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes 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. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.
摘要翻译：通过本发明提供的以吲哚为基础的体内显像剂以高亲和力结合PBR，在给药后具有良好的摄入脑中，并具有良好的选择性结合PBR。本发明还包括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。本发明的其它方面包括包含本发明的体内显像剂的放射性药物组合物和使用所述体内显像剂的方法。

2. 发明申请

US20120020884A1 INDOLE DERIVATIVES 有权
标题翻译： INDOLE DORIVATIVES
公开(公告)号：US20120020884A1
公开(公告)日：2012-01-26
申请号：US13258465
申请日：2010-03-26
申请人： Harry John Wadsworth , Bo Shan , Dennis O'shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
发明人： Harry John Wadsworth , Bo Shan , Dennis O'shea , Joanna Marie Passmore , William John Trigg , Amanda Ewan
IPC分类号： A61K51/04 , B01J19/00 , C07D401/08 , C07D495/04 , C07D209/94 , C07D209/80
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
摘要： An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes 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. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.
摘要翻译：通过本发明提供的以吲哚为基础的体内显像剂以高亲和力结合PBR，在给药后具有良好的摄入脑中，并具有良好的选择性结合PBR。本发明还包括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。本发明的其它方面包括包含本发明的体内显像剂的放射性药物组合物和使用所述体内显像剂的方法。

3. 发明授权

US09481685B2 Imaging neuroinflammation 有权
标题翻译：成像神经炎症
公开(公告)号：US09481685B2
公开(公告)日：2016-11-01
申请号：US13119450
申请日：2009-10-02
申请人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg
发明人： Harry John Wadsworth , Bo Shan , Dennis O'Shea , Joanna Marie Passmore , William John Trigg
IPC分类号： A61K51/00 , A61M36/14 , C07D495/04 , A61K51/04
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，其以高亲和力与PBR结合，在给药后具有良好的摄入脑中，并优先结合表达较高水平的PBR的组织。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，以及使用所述体内显像剂的方法。

4. 发明授权

US08501153B2 Active enantiomer 有权
标题翻译：活性对映异构体
公开(公告)号：US08501153B2
公开(公告)日：2013-08-06
申请号：US12880218
申请日：2010-09-13
申请人： Radha Achanath , Srinath Balaji , Afsal M. Kadavilpparampu Mohamed , Umamaheshwar Mokkapati , Steven Fairway , Dimitrios Mantzilas , Dennis O'Shea , William John Trigg , Harry John Wadsworth , Joanna Marie Passmore , Bo Shan
发明人： Radha Achanath , Srinath Balaji , Afsal M. Kadavilpparampu Mohamed , Umamaheshwar Mokkapati , Steven Fairway , Dimitrios Mantzilas , Dennis O'Shea , William John Trigg , Harry John Wadsworth , Joanna Marie Passmore , Bo Shan
IPC分类号： A61K51/00 , A61K36/14
CPC分类号： C07D209/94 , A61K51/0446 , A61K51/0455 , A61K51/0468 , C07B59/002 , C07B2200/05 , C07D209/88 , C07D295/192 , C07D401/06 , C07D495/04
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

US20110190618A1 IMAGING NEUROINFLAMMATION 有权
标题翻译：成像神经炎症
公开(公告)号：US20110190618A1
公开(公告)日：2011-08-04
申请号：US13119450
申请日：2009-10-02
申请人： Harry John Wadsworth , Bo Shan , Dennis O' Shea , Joanna Marie Passmore , William John Trigg
发明人： Harry John Wadsworth , Bo Shan , Dennis O' Shea , Joanna Marie Passmore , William John Trigg
IPC分类号： A61B6/00 , C07D495/04 , A61K51/00 , A61B19/00
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，其以高亲和力与PBR结合，在给药后具有良好的摄入脑中，并优先结合表达较高水平的PBR的组织。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，以及使用所述体内显像剂的方法。

6. 发明申请

US20100221189A1 CONTRAST AGENTS 失效
标题翻译：对比剂
公开(公告)号：US20100221189A1
公开(公告)日：2010-09-02
申请号：US12682298
申请日：2008-10-10
申请人： Ian Martin Newington , Duncan George Wynn , Veronique Morisson-Iveson , Joanna Marie Passmore
发明人： Ian Martin Newington , Duncan George Wynn , Veronique Morisson-Iveson , Joanna Marie Passmore
IPC分类号： A61K49/04 , C07C233/15 , C07D241/04 , C07D211/56
CPC分类号： A61K49/0438 , C07C237/46 , C07C2601/14 , C07D211/58 , C07D295/108
摘要： The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula (I) and salts or optical active isomers thereof, wherein each R1 independently are the same or different and denotes a hydrogen atom or a C1 to C4 straight or branched alkyl group which is optionally substituted by 1 to 4 —OH groups; each of R2 independently are the same or different and denote a hydrogen atom or a C1 to C4 straight or branched alkyl group; each R3 independently are the same or different and denotes a hydrogen atom or a C1 to C4 straight or branched alkyl group which is optionally substituted by 1 to 4 —OH groups; each R4 independently are the same or different and denote C1 to C6 straight or branched alkyl moieties substituted by up to 6 —OH groups; and each R5 independently are the same or different and denote C1 to C6 straight or branched alkyl moieties substituted by up to 6 —OH groups; and X denotes a straight chain alkylene moiety with 3 to 10 carbon atoms, a 1,4-cyclohexylene group, or X together with the adjacent —NR1 groups forms a 1,4-piperazine group or a 4-aminopiperidine group. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.
摘要翻译：本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。更具体地说，含碘化合物是含有通式（I）的两个连接的碘化苯基和其盐或光学活性异构体的化合物，其中每个R 1独立地相同或不同，表示氢原子或C1至C4直链或任选被1至4个-OH基团取代的支链烷基; R2各自相同或不同，表示氢原子或C1〜C4直链或支链烷基; 每个R 3独立地相同或不同，表示氢原子或任选被1至4个-OH基团取代的C 1至C 4直链或支链烷基; 每个R 4独立地相同或不同，表示被至多6个-OH基团取代的C1至C6直链或支链烷基部分; 并且每个R 5独立地相同或不同，表示被至多6个-OH基团取代的C 1至C 6直链或支链烷基部分; X表示具有3至10个碳原子的直链亚烷基部分，1,4-亚环己基或X与相邻的-NR1基团一起形成1,4-哌嗪基团或4-氨基哌啶基团。本发明还涉及这种诊断组合物作为造影剂在诊断成像中，特别是在X射线成像中的用途，以及含有这些化合物的造影剂。

7. 发明申请

US20080260651A1 CONTRAST AGENTS 审中-公开
标题翻译：对比剂
公开(公告)号：US20080260651A1
公开(公告)日：2008-10-23
申请号：US12103032
申请日：2008-04-15
申请人： Veronique Morisson-Iveson , Joanna Marie Passmore
发明人： Veronique Morisson-Iveson , Joanna Marie Passmore
IPC分类号： A61K49/04 , C07D207/12 , C07D211/40
CPC分类号： C07D211/46 , A61K49/0438 , C07D207/12
摘要： The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic N-heterocyclic central moiety such as pyrrolidine or piperidine heterocycles allowing for the arrangement of three iodinated phenyl groups bound thereto.The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging, in particular in X-ray imaging, and to contrast media containing such compounds.
摘要翻译：本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。更具体地说，含碘化合物是含有脂族N-杂环中心部分如吡咯烷或哌啶杂环的化合物，其允许与其结合的三个碘化苯基的排列。本发明还涉及这样的诊断组合物作为造影剂在诊断成像，特别是X射线成像中的用途，以及含有这些化合物的造影剂。

8. 发明授权

US08202511B2 Contrast agents 失效
标题翻译：对比剂
公开(公告)号：US08202511B2
公开(公告)日：2012-06-19
申请号：US12682298
申请日：2008-10-10
申请人： Ian Martin Newington , Duncan George Wynn , Veronique Morisson-Iveson , Joanna Marie Passmore
发明人： Ian Martin Newington , Duncan George Wynn , Veronique Morisson-Iveson , Joanna Marie Passmore
IPC分类号： A61K49/04
CPC分类号： A61K49/0438 , C07C237/46 , C07C2601/14 , C07D211/58 , C07D295/108
摘要： The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.
摘要翻译：本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。本发明还涉及这种诊断组合物作为造影剂在诊断成像中，特别是在X射线成像中的用途，以及含有这些化合物的造影剂。

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