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公开(公告)号：US20080279765A1
公开(公告)日：2008-11-13
申请号：US12095931
申请日：2006-12-07
IPC分类号： A61K51/00 , C07K14/47 , C07H13/00 , C07K14/00 , C07C403/08 , C07K7/06 , C07K5/08 , C07F13/00 , A61K49/00
CPC分类号： A61K51/08 , A61K51/0402 , A61K51/088
摘要： The present invention provides a novel imaging agent targeting the mannose-6-phosphate (M6P) receptor suitable for the non-invasive visualization of fibrosis. A method for the preparation of the imaging agent is also provided by the invention, as well as a precursor for use in said method. The invention also provides a pharmaceutical composition comprising the imaging agent and a kit for the preparation of the pharmaceutical composition. In a further aspect, use of the imaging agent for in vivo imaging and in the preparation of a medicament for the diagnosis of a condition in which the mannose-6-phosphate receptor is upregulated is provided.
摘要翻译： 本发明提供了靶向适于非侵入性可视化纤维化的甘露糖-6-磷酸（M6P）受体的新型成像剂。 本发明还提供了用于制备显影剂的方法，以及用于所述方法的前体。 本发明还提供一种药物组合物，其包含该成像剂和用于制备药物组合物的试剂盒。 在另一方面，提供了用于体内成像和用于诊断其中甘露糖-6-磷酸受体上调的病症的药物的制备的成像剂的用途。
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公开(公告)号：US20060275215A1
公开(公告)日：2006-12-07
申请号：US10560509
申请日：2004-11-26
申请人： Duncan Hiscock , Ben Newton , Benedicte Guilbert
发明人： Duncan Hiscock , Ben Newton , Benedicte Guilbert
CPC分类号： A61K51/0455 , A61K51/0431 , A61K51/0446 , A61K51/0459 , A61K51/088 , Y02P20/582
摘要： The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic caspase-3 inhibitor labelled with an imaging moiety suitable for diagnostic imaging in vivo. The invention also provides pharmaceutical and radiopharmaceutical compositions comprising the imaging agents, together with kits for the preparation of the radiopharmaceuticals. Also described are chelator conjugates of the caspase-3 inhibitor, which are suitable for the preparation of imaging agents comprising a radioactive or paramagnetic metal ion. The imaging agents are useful for the diagnostic imaging and or therapy monitoring in vivo of various disease states where caspase-3 is involved.
摘要翻译： 本发明涉及用于体内成像的诊断成像剂。 成像剂包括用适于体内诊断成像的成像部分标记的合成半胱天冬酶-3抑制剂。 本发明还提供包含成像剂的药物和放射性药物组合物，以及用于制备放射性药物的试剂盒。 还描述了胱天蛋白酶-3抑制剂的螯合剂缀合物，其适用于制备包含放射性或顺磁性金属离子的成像剂。 成像剂可用于在体内涉及caspase-3的各种疾病状态的诊断成像和/或治疗监测。
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公开(公告)号：US06897209B2
公开(公告)日：2005-05-24
申请号：US10647004
申请日：2003-08-22
申请人： Alan Michael Forster , Peter Knox , Marivi Mendizabal , Timothy Charles Richardson , Anthony Eamon Storey , Ian Andrew Wilson , Susan Champion , Alex Gibson , Benedicte Guilbert
发明人： Alan Michael Forster , Peter Knox , Marivi Mendizabal , Timothy Charles Richardson , Anthony Eamon Storey , Ian Andrew Wilson , Susan Champion , Alex Gibson , Benedicte Guilbert
IPC分类号： A61K49/00 , A61K51/00 , A61K51/04 , A61P9/10 , A61P31/10 , A61P35/00 , C07C311/18 , C07F13/00 , C09K3/00 , A61K31/28 , A61K31/18 , A61K31/33 , A61K31/44 , A61K31/4965
CPC分类号： A61K51/0482 , A61K51/0478 , A61K2123/00
摘要： A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula (Y)m-A-NHR)k can function as a substrate for the fibrin-stabilizing Factor XIIIa. The complex is useful for the diagnosis or therapy of thrombosis, embolism, atherosclerosis, inflammation or cancer.
摘要翻译： 放射性金属或顺磁性金属离子与金属螯合剂如二胺二肟的络合物附着有式（Y）的取代基-N-NHR的取代基。 用作纤维蛋白稳定因子XIIIa的底物。 该复合物可用于血栓形成，栓塞，动脉粥样硬化，炎症或癌症的诊断或治疗。
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公开(公告)号：US20080286201A1
公开(公告)日：2008-11-20
申请号：US11815360
申请日：2006-02-03
申请人： Benedicte Guilbert , Sue Champion , Alexander Mark Gibson , Sally-Anne Ricketts , Michelle Avory , Bente E. Arbo
发明人： Benedicte Guilbert , Sue Champion , Alexander Mark Gibson , Sally-Anne Ricketts , Michelle Avory , Bente E. Arbo
CPC分类号： A61K51/088 , A61K38/07
摘要： The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic caspase-3 substrate peptide labelled with an imaging moiety suitable for diagnostic imaging in vivo. The invention also provides radiopharmaceutical compositions comprising the imaging agents, together with kits for the preparation of the radiopharmaceuticals. Also described are non-radioactive precursors suitable for the preparation of the imaging agents. The imaging agents are useful for the diagnostic imaging and or therapy monitoring in vivo of various disease states where caspase-3 is involved.
摘要翻译： 本发明涉及用于体内成像的诊断成像剂。 成像剂包括用适于体内诊断成像的成像部分标记的合成半胱天冬酶-3底物肽。 本发明还提供包含成像剂的放射性药物组合物，以及用于制备放射性药物的试剂盒。 还描述了适用于制备显像剂的非放射性前体。 成像剂可用于在体内涉及caspase-3的各种疾病状态的诊断成像和/或治疗监测。
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公开(公告)号：US20060120956A1
公开(公告)日：2006-06-08
申请号：US10530836
申请日：2003-10-08
申请人： Klaus Kopka , Hans-Jorg Breyholz , Stefan Wagner , Michael Shafers , Bodo Leykau , Benedicte Guilbert , Duncan Wynn
发明人： Klaus Kopka , Hans-Jorg Breyholz , Stefan Wagner , Michael Shafers , Bodo Leykau , Benedicte Guilbert , Duncan Wynn
IPC分类号： A61K51/00 , C07F5/00 , C07D403/02 , C07K16/46
CPC分类号： A61K51/0497 , A61K49/0438 , A61K51/0459
摘要： The present invention relates to diagnostic imaging agents for in vivo imaging. The imaging agents comprise a synthetic barbituric acid derivative labelled at the 5-position with an imaging moiety suitable for diagnostic imaging in vivo. The invention also provides pharmaceutical and radiopharmaceutical compositions comprising the imaging agents, together with kits of the preparation of the radiopharmaceuticals. Also described are chelator conjugates of the barbituric acid derivative, which are suitable for the preparation of imaging agents comprising a radioactive or paramagnetic metal ion. The imaging agents are useful for the diagnostic imaging in vivo of various disease states, including atherosclerosis.
摘要翻译： 本发明涉及用于体内成像的诊断成像剂。 成像剂包括在5位标记的合成巴比妥酸衍生物，其具有适于体内诊断成像的成像部分。 本发明还提供包含成像剂的药物和放射性药物组合物，以及放射性药物的制备试剂盒。 还描述了适用于制备包含放射性或顺磁金属离子的成像剂的巴比妥酸衍生物的螯合剂缀合物。 成像剂可用于各种疾病状态的体内诊断成像，包括动脉粥样硬化。
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公开(公告)号：US20130064770A1
公开(公告)日：2013-03-14
申请号：US13699155
申请日：2011-05-26
申请人： Ian Martin Newington , Duncan George Wynn , Robert James Domett Nairne , Benedicte Guilbert , Subrata Mandal , Jinto Jose , Sunderaraman Varadarajan , Chitralekha Rangaswamy , Helen Betts , Rebecca Davis
发明人： Ian Martin Newington , Duncan George Wynn , Robert James Domett Nairne , Benedicte Guilbert , Subrata Mandal , Jinto Jose , Sunderaraman Varadarajan , Chitralekha Rangaswamy , Helen Betts , Rebecca Davis
IPC分类号： A61K51/04 , C07D403/06 , C07D327/04 , C07D401/14 , C07D417/14 , B01J19/00 , C07D295/096 , C07D417/04 , C07D403/12 , C07D417/12 , C07D401/04 , C07D403/04
CPC分类号： C07D401/04 , A61K51/0459 , A61K51/0461 , B01J19/00 , C07D209/14 , C07D211/96 , C07D213/74 , C07D213/75 , C07D217/06 , C07D233/88 , C07D239/88 , C07D249/04 , C07D253/075 , C07D263/46 , C07D263/58 , C07D277/36 , C07D277/64 , C07D277/74 , C07D295/096 , C07D295/125 , C07D327/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.
摘要翻译： 本发明涉及放射诊断化合物，制备这些化合物的方法及其用作优选用于PET或SPECT，优选PET的HA血清素5-HT1A受体的显像剂。 还公开了包含成像有效量的放射性标记化合物的组合物。 本发明还涉及非放射性标记的化合物，制备这些化合物的方法及其用于治疗各种神经和/或精神疾病的方法。
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公开(公告)号：US20110129419A1
公开(公告)日：2011-06-02
申请号：US12519398
申请日：2007-12-19
IPC分类号： A61K51/04 , C07C235/56 , C07D401/12 , C07D401/04 , C07D211/58 , C07D405/12 , C07D211/48 , C07D471/10
CPC分类号： A61K51/0406 , A61K51/04 , A61K51/0455 , C07B59/002 , C07B2200/05 , C07C235/56 , C07D211/62 , C07D401/04 , C07D401/14 , C07D405/12 , C07D471/10
摘要： The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.
摘要翻译： 本发明涉及医学成像领域，特别涉及与趋化因子受体5（CCR5）的上调相关的疾病状态的成像。 提供了成像剂，前体和方法，其可用于成像这样的疾病状态。
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公开(公告)号：US07049289B1
公开(公告)日：2006-05-23
申请号：US09674616
申请日：1999-05-14
申请人： Anthony Eamon Storey , Marivi Mendizabal , Susan Champion , Alex Gibson , Benedicte Guilbert , Ian Andrew Wilson , Peter Knox
发明人： Anthony Eamon Storey , Marivi Mendizabal , Susan Champion , Alex Gibson , Benedicte Guilbert , Ian Andrew Wilson , Peter Knox
IPC分类号： A61K38/00
CPC分类号： A61K49/14 , A61K51/088
摘要： Synthetic analogues of lysine and glutamine are provided which function as substrates for the fibrin-stabilising enzyme Factor XIIIa even when labelled with a detectable moiety. The use of suitable protecting groups provides compounds which possess reduced susceptibility to in vivo metabolism especially by peptidases, and are hence useful agents for the diagnosis of thrombosis, embolism, atherosclerosis, inflammation or cancer.
摘要翻译： 提供赖氨酸和谷氨酰胺的合成类似物，其用作纤维蛋白稳定酶因子XIIIa的底物，即使用可检测部分标记。 合适的保护基团的使用提供了具有降低的体内代谢易感性，特别是肽酶的化合物，因此可用于诊断血栓形成，栓塞，动脉粥样硬化，炎症或癌症。
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公开(公告)号：US06653299B1
公开(公告)日：2003-11-25
申请号：US09341915
申请日：1999-10-04
申请人： Alan Michael Forster , Peter Knox , Marivi Mendizabal , Timothy Charles Richardson , Anthony Eamon Storey , Ian Andrew Wilson , Susan Champion , Alex Gibson , Benedicte Guilbert
发明人： Alan Michael Forster , Peter Knox , Marivi Mendizabal , Timothy Charles Richardson , Anthony Eamon Storey , Ian Andrew Wilson , Susan Champion , Alex Gibson , Benedicte Guilbert
IPC分类号： A61K3128
CPC分类号： A61K51/0482 , A61K51/0478 , A61K2123/00
摘要： A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula —(Y)m—A—NHR, can function as a substrate for the fibrin-stabilizing Factor XIIIa. The complex is useful for the diagnosis or therapy of thrombosis, embolism, atherosclerosis, inflammation or cancer.
摘要翻译： 放射性金属或顺磁性金属离子与金属螯合剂如二胺肟的络合物与式 - （Y）m-A-NHR的取代基连接，可用作纤维蛋白稳定因子XIIIa的底物。 该复合物可用于血栓形成，栓塞，动脉粥样硬化，炎症或癌症的诊断或治疗。
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公开(公告)号：US20110268660A1
公开(公告)日：2011-11-03
申请号：US13058345
申请日：2009-08-14
IPC分类号： A61K49/00
CPC分类号： A61K49/0032 , A61K49/0056
摘要： The present invention provides a method of imaging useful in the determination of sites of dysplasia in patients suffering from Barrett's oesophagus. The method comprises the use of an optical imaging agent comprising a vector which targets the extracellular domain of EGFR, the vector also being selective for EGFR over Her2. The vector is labelled with an optical reporter suitable for in vivo imaging using light in the green to near-infrared wavelength 500-1200 nm. Also provided are novel optical imaging agents suitable for use in the method.
摘要翻译： 本发明提供了一种用于确定患有巴雷特食管的患者发育不良部位的成像方法。 该方法包括使用包含靶向EGFR细胞外结构域的载体的光学显像剂，所述载体对于Her2也是EGFR选择性的。 使用适用于使用绿色至近红外波长500-1200nm的光的体内成像的光学报告基来标记载体。 还提供了适用于该方法的新型光学成像剂。
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