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公开(公告)号：US08771641B2
公开(公告)日：2014-07-08
申请号：US13510041
申请日：2010-12-16
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。
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公开(公告)号：US09186424B2
公开(公告)日：2015-11-17
申请号：US14295762
申请日：2014-06-04
IPC分类号： A61K51/04 , A61K31/44 , C07D307/79 , C07D307/81 , C07D317/46 , C07D317/58 , C07D319/18 , C07D321/10 , B01L3/00
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 radiolabelled 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： 本发明提供了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。
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3.发明授权Radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy 有权放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用公开(公告)号：US07850948B2
公开(公告)日：2010-12-14
申请号：US12207774
申请日：2008-09-10
申请人： Matthias Friebe , Peter Muschick , Andreas Huth
发明人： Matthias Friebe , Peter Muschick , Andreas Huth
CPC分类号： A61K51/04 , A61K51/0425 , A61K51/0463
摘要： This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.
摘要翻译： 本发明涉及新的放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用。 根据本发明的放射性卤代苯甲酰胺衍生物显示出新的和特别有利的特性，特别是关于肿瘤浓度和延迟，肝脏浓度和血液积聚。 与健康的身体组织相比，在肿瘤中实现的放射治疗剂量对于本发明的化合物是有利的。
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公开(公告)号：US20090180951A1
公开(公告)日：2009-07-16
申请号：US12331747
申请日：2008-12-10
申请人： Craig N. ZIMMERMAN , John W. BABICH
发明人： Craig N. ZIMMERMAN , John W. BABICH
CPC分类号： A61K51/088 , A61K51/0402 , A61K51/0425 , A61K51/0446 , A61K51/0478 , A61K51/0497
摘要： A complex, its stereoisomer or pharmaceutically acceptable salt has the formula I, where: wherein: W is a group that is A, B, or C: R1 is hydrogen, alkyl or alkoxy; R2 is a bond, hydrogen or alkyl R3, R4 and R5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl; X is a bond, C═O, O═C—O, or CH2; Y is a bond, CH2, or O; m is an integer ranging from 1 to 6; n is an integer ranging from 0 to 6; Metal represents a metallic moiety comprising a radionuclide; and Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex.
摘要翻译： 络合物，其立体异构体或药学上可接受的盐具有式I，其中：其中：W是A，B或C的基团：R 1是氢，烷基或烷氧基; R2是键，氢或烷基R3，R4和R5独立地是氢，碘，烷基，烷氧基，羟基，氨基，氨基烷基，二烷基氨基或羧基; X是键，C-O，O-C-O或CH 2; Y是键，CH2或O; m为1〜6的整数; n为0〜6的整数; 金属代表包含放射性核素的金属部分; 螯合物代表与所述放射性核素配位以形成络合物的螯合部分。
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公开(公告)号：US20140288317A1
公开(公告)日：2014-09-25
申请号：US14295762
申请日：2014-06-04
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 radiolabelled 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： 本发明提供了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。
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公开(公告)号：US20120244073A1
公开(公告)日：2012-09-27
申请号：US13510041
申请日：2010-12-16
IPC分类号： A61K51/04 , B01L3/00 , C07D319/18 , C07D307/79 , C07D317/60
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。
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7.发明申请Radiohalogenated Benzamide Derivatives And Their Use In Tumor Diagnosis And Tumor Therapy 有权放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用公开(公告)号：US20090012090A1
公开(公告)日：2009-01-08
申请号：US12207774
申请日：2008-09-10
申请人： Matthias Friebe , Peter Muschick , Andreas Huth
发明人： Matthias Friebe , Peter Muschick , Andreas Huth
IPC分类号： A61K31/5375 , A61K31/165 , A61K31/235 , A61P35/00 , A61K31/36
CPC分类号： A61K51/04 , A61K51/0425 , A61K51/0463
摘要： This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.
摘要翻译： 本发明涉及新的放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用。 根据本发明的放射性卤代苯甲酰胺衍生物显示出新的和特别有利的特性，特别是关于肿瘤浓度和延迟，肝脏浓度和血液积聚。 与健康的身体组织相比，在肿瘤中实现的放射治疗剂量对于本发明的化合物是有利的。
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8.发明授权Radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy 失效放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用公开(公告)号：US07427390B2
公开(公告)日：2008-09-23
申请号：US11076023
申请日：2005-03-10
申请人： Matthias Friebe , Peter Muschick , Andreas Huth
发明人： Matthias Friebe , Peter Muschick , Andreas Huth
CPC分类号： A61K51/04 , A61K51/0425 , A61K51/0463
摘要： This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.
摘要翻译： 本发明涉及新的放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用。 根据本发明的放射性卤代苯甲酰胺衍生物显示出新的和特别有利的特性，特别是关于肿瘤浓度和延迟，肝脏浓度和血液积聚。 与健康的身体组织相比，在肿瘤中实现的放射治疗剂量对于本发明的化合物是有利的。
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9.发明申请Radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy 失效放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用公开(公告)号：US20050207972A1
公开(公告)日：2005-09-22
申请号：US11076023
申请日：2005-03-10
申请人： Matthias Friebe , Peter Muschick , Andreas Huth
发明人： Matthias Friebe , Peter Muschick , Andreas Huth
CPC分类号： A61K51/04 , A61K51/0425 , A61K51/0463
摘要： This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.
摘要翻译： 本发明涉及新的放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用。 根据本发明的放射性卤代苯甲酰胺衍生物显示出新的和特别有利的特性，特别是关于肿瘤浓度和延迟，肝脏浓度和血液积聚。 与健康的身体组织相比，在肿瘤中实现的放射治疗剂量对于本发明的化合物是有利的。
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