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1. 发明授权

US07321027B2 Small technetium-99m and rhenium labeled agents and methods for imaging tumors 失效
标题翻译：小锝-99m和铼标记的药剂和肿瘤成像方法
公开(公告)号：US07321027B2
公开(公告)日：2008-01-22
申请号：US10279214
申请日：2002-10-23
申请人： Ashfaq Mahmood , Matthias Friebe , Cristina Bolzati , Alun G. Jones , Alan Davison
发明人： Ashfaq Mahmood , Matthias Friebe , Cristina Bolzati , Alun G. Jones , Alan Davison
IPC分类号： C07F13/00
CPC分类号： C07D295/13 , A61K51/0478 , C07C323/41 , C07F13/005 , C07K5/06026
摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabeled metal complexes. Preferred radiolabeled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumor/nontumor ratios of the technetium complexes of the invention indicate that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods of treatment of tumors using a radiolabeled metal complex as a radiopharmaceutical agent to treat the tumor.
摘要翻译：本发明涉及适用于肿瘤例如癌，黑素瘤和其他肿瘤的成像或治疗性治疗的化合物及其相关的锝和铼络合物。在另一个实施方案中，本发明涉及使用放射性标记的金属络合物成像肿瘤的方法。用于成像肿瘤的优选放射性标记复合物包括锝和铼络合物。本发明的锝络合物的高肿瘤摄取和显着的肿瘤/非肿瘤比率表明，这种基于锝-99m的小分子探针可以作为黑色素瘤及其转移的体内诊断剂开发。在另一个实施方案中，本发明涉及使用放射性标记的金属络合物作为放射性药物治疗肿瘤的方法治疗肿瘤。

2. 发明申请

US20080226550A1 SMALL TECHNETIUM-99M AND RHENIUM LABELED AGENTS AND METHODS FOR IMAGING TUMORS 审中-公开
标题翻译：小技术-99M和氙标签代理和成像肿瘤的方法
公开(公告)号：US20080226550A1
公开(公告)日：2008-09-18
申请号：US12017328
申请日：2008-01-21
申请人： Ashfaq Mahmood , Matthias Friebe , Cristina Bolzati , Alun G. Jones , Alan Davison
发明人： Ashfaq Mahmood , Matthias Friebe , Cristina Bolzati , Alun G. Jones , Alan Davison
IPC分类号： A61K51/04 , C07F5/00 , C07D211/00 , A61P35/00 , C07D295/00
CPC分类号： C07D295/13 , A61K51/0478 , C07C323/41 , C07F13/005 , C07K5/06026
摘要： The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabeled metal complexes. Preferred radiolabeled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumor/nontumor ratios of the technetium complexes of the invention indicate that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods of treatment of tumors using a radiolabeled metal complex as a radiopharmaceutical agent to treat the tumor.
摘要翻译：本发明涉及适用于肿瘤例如癌，黑素瘤和其他肿瘤的成像或治疗性治疗的化合物及其相关的锝和铼络合物。在另一个实施方案中，本发明涉及使用放射性标记的金属络合物成像肿瘤的方法。用于成像肿瘤的优选放射性标记复合物包括锝和铼络合物。本发明的锝络合物的高肿瘤摄取和显着的肿瘤/非肿瘤比率表明，这种基于锝-99m的小分子探针可以作为黑色素瘤及其转移的体内诊断剂开发。在另一个实施方案中，本发明涉及使用放射性标记的金属络合物作为放射性药物治疗肿瘤的方法治疗肿瘤。

3. 发明授权

US08182789B2 Intermediate compound of technetium nitride complex for radiodiagnostic imaging 失效
标题翻译：用于放射诊断成像的氮化钇络合物的中间体化合物
公开(公告)号：US08182789B2
公开(公告)日：2012-05-22
申请号：US12160920
申请日：2006-01-20
申请人： Francesco Tisato , Fiorenzo Refosco , Cristina Bolzati , Stefania Agostini , Marina Porchia , Mario Cavazza-Ceccato , Shinji Tokunaga
发明人： Francesco Tisato , Fiorenzo Refosco , Cristina Bolzati , Stefania Agostini , Marina Porchia , Mario Cavazza-Ceccato , Shinji Tokunaga
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07F9/5004 , A61K51/0489 , C07F9/4009 , C07F13/005
摘要： A bisphosphonoamine compound represented by the following formula (I): wherein R1, R2, R3, R4 and R5 are independently an alkyl group having 1 to 6 carbon atoms, and n is an integer of 1 to 6, is extremely useful as an intermediate for preparing a technetium nitride complex for radiodiagnostic imaging.
摘要翻译：由下式（I）表示的双膦酰胺化合物：其中R1，R2，R3，R4和R5独立地为具有1至6个碳原子的烷基，n为1至6的整数，作为中间体是非常有用的用于制备用于放射诊断成像的锝氮化物络合物。

4. 发明申请

US20080267869A1 RADIOACTIVE TRANSITION METAL-IMIDO HETERO-DIPHOSPHINE COMPLEXES, THEIR PREPARATION AND RADIOPHARMACEUTICAL COMPOSITIONS THEREOF 失效
标题翻译：放射性转移金属 - 咪唑类异双膦酸酯复合物，其制备及放射性能组合物
公开(公告)号：US20080267869A1
公开(公告)日：2008-10-30
申请号：US12144370
申请日：2008-06-23
申请人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
发明人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
IPC分类号： A61K51/04 , C07F3/00
CPC分类号： C07F13/005 , A61K51/0489 , C07B2200/05 , C07F9/5004
摘要： The present invention provides radioactive metal heterocomplexes of formula (I): [(Me=N—R)L1L2]+Z− (I), wherein Me, R, L1 L2 and Z− have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium- or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert [(Me=N—R)L1] moieties. Such moieties are fixed in an intermediate [(Me=N—R)Y2L1)]+ compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2 to give the final [(Me=N—R)L1L2]+ Z−heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2 framework or the imido R group.
摘要翻译：本发明提供了式（I）的放射性金属异复合物：[（Me = NR）L 1 L 2] + Z - （I ），其中Me，R，L 1，L 2，Z 2和Z 2具有说明书中指出的含义。络合物包括三价放射性金属 - 亚氨基，通常是锝或铼 - 酰亚胺基，其通过存在辅助三齿异二膦配体L 1 1强烈稳定，这允许形成取代 -inert [（Me = NR）L 1]部分。这些部分固定在含有两个不稳定的，定形的Y（Y）的中间体[（Me = NR）Y 2 L 1 L 1 - 配体，其中Y优选为卤化物基团。后者容易被二齿配体L 2替代，得到最终的[（Me = NR）L 1 L 2 L 2 + - 异复合物。本发明的配合物可用于制备放射性药物：事实上，赋予生物寻靶特性的生物活性片段可以在L 2框架或亚氨基R基团上引入。

5. 发明申请

US20100160615A1 INTERMEDIATE COMPOUND OF TECHNETIUM NITRIDE COMPLEX FOR RADIODIAGNOSTIC IMAGING 失效
标题翻译：放射线成像技术硝酸复合物的中间化合物
公开(公告)号：US20100160615A1
公开(公告)日：2010-06-24
申请号：US12160920
申请日：2006-01-20
申请人： Francesco Tisato , Fiorenzo Refosco , Cristina Bolzati , Stefania Agostini , Marina Porchia , Mario Cavazza-Ceccato , Shinji Tokunaga
发明人： Francesco Tisato , Fiorenzo Refosco , Cristina Bolzati , Stefania Agostini , Marina Porchia , Mario Cavazza-Ceccato , Shinji Tokunaga
IPC分类号： C07F13/00 , C07F9/28
CPC分类号： C07F9/5004 , A61K51/0489 , C07F9/4009 , C07F13/005
摘要： A bisphosphonoaminc compound represented by the following formula (I): wherein R1, R2, R3, R4 and R5 are independently an alkyl group having 1 to 6 carbon atoms, and n is an integer of 1 to 6, is extremely useful as an intermediate for preparing a technetium nitride complex for radiodiagnostic imaging.
摘要翻译：由下式（I）表示的双膦酰氨基化合物：其中R1，R2，R3，R4和R5独立地是具有1至6个碳原子的烷基，n是1至6的整数，作为中间体是非常有用的用于制备用于放射诊断成像的锝氮化物络合物。

6. 发明授权

US07445765B2 Radiopharmaceutical for diagnostic imaging containing a technetium-99m nitride heterocomplex 失效
标题翻译：用于包含锝-99m氮化物异复合物的诊断成像的放射性药物
公开(公告)号：US07445765B2
公开(公告)日：2008-11-04
申请号：US10332707
申请日：2001-07-25
申请人： Adriano Duatti , Cristina Bolzati , Licia Uccelli , Alessandra Boschi , Fiorenzo Refosco , Francesco Tisato
发明人： Adriano Duatti , Cristina Bolzati , Licia Uccelli , Alessandra Boschi , Fiorenzo Refosco , Francesco Tisato
IPC分类号： A61K49/00
CPC分类号： A61K51/02 , A61K51/0476
摘要： A radiopharmaceutical for diagnostic imaging containing as an active ingredient a technetium-99m nitride heterocomplex comprising technetium-99m nitride and two different ligands coordinated therewith, i.e., a bisphosphinoamine compound as a π electron acceptor and a bidentate ligand as a π electron donor and represented by the following formula (I): [99mTc(N)(PNP)(XY)]+ (I)wherein 99mTc(N) is technetium-99m nitride, PNP is a bisphosphinoamine compound and XY is a bidentate ligand, is markedly accumulated in heart and adrenal glands and hence is useful for radiodiagnostic imaging of heart and adrenal glands.
摘要翻译：用于诊断成像的放射性药物，其包含锝-99m氮化物异复合物作为活性成分，其包含锝-99m氮化物和与其配位的两种不同配体，即作为pi电子受体的双膦胺化合物和作为pi电子供体的二齿配体，以下式（I）：其中99m Tc（N（N））其中99m Tc（N）（PNP）（XY））是锝-99m氮化物，PNP是双膦胺化合物，XY是双齿配体，明显地积聚在心脏和肾上腺中，因此可用于心脏和肾上腺的放射诊断成像。

7. 发明申请

US20060120957A1 Radioactive transition metal-imido hetero-diphosphine complexes, their preparation and radiopharmaceutical compositions thereof 失效
标题翻译：放射性过渡金属 - 亚氨基杂二膦配合物，它们的制备和放射性药物组合物
公开(公告)号：US20060120957A1
公开(公告)日：2006-06-08
申请号：US10533988
申请日：2003-10-31
申请人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
发明人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
IPC分类号： A61K51/00 , C07F5/00
CPC分类号： C07F13/005 , A61K51/0489 , C07B2200/05 , C07F9/5004
摘要： The present invention provides radioactive metal heterocomplexes of formula (I): [(Me═N—R)L1L2]+Z. (I), wherein Me, R, L1 L2 and Z− have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium- or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert [(Me═N—R)L1] moieties. Such moieties are fixed in an intermediate [(Me═N—R)Y2L1)]+ compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2 to give the final [(Me═N—R)L1L2]+Z−heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2 framework or the imido R group.
摘要翻译：本发明提供式（I）的放射性金属异复合物：[（Me-N-R）L 1 L 2 + Z。（I），其中Me，R，L 1，L 2和Z 2具有说明书中指出的含义。络合物包括三价放射性金属 - 亚氨基，通常是锝或铼 - 酰亚胺基，其通过存在辅助三齿异二膦配体L 1 1强烈稳定，这允许形成取代 -inert [（Me-NR）L 1]部分。这些部分被固定在含有两个不稳定的，定形的Y（Y）的中间体[（Me-NR）Y 2 L 1 L 1）+ / 配体，其中Y优选为卤化物基团。后者容易被二齿配体L 2替代，得到最终的[（Me-NR）L 1 L 2 L 2 O 2 + - 异复合物。本发明的配合物可用于制备放射性药物：事实上，赋予生物寻靶特性的生物活性片段可以在L 2框架或亚氨基R基团上引入。

8. 发明授权

US07396523B2 Radioactive transition metal-imido hetero-diphosphine complexes, their preparation and radiopharmaceutical compositions thereof 失效
标题翻译：放射性过渡金属 - 亚氨基杂二膦配合物，它们的制备和放射性药物组合物
公开(公告)号：US07396523B2
公开(公告)日：2008-07-08
申请号：US10533988
申请日：2003-10-31
申请人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
发明人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07F13/005 , A61K51/0489 , C07B2200/05 , C07F9/5004
摘要： The present invention provides radioactive metal heterocomplexes of formula (I): [(Me═N—R)L1L2]+Z (I), wherein Me, R, L1 L2 and Z− have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium- or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert [(Me═N—R)L1] moieties. Such moieties are fixed in an intermediate [(Me═N—R)Y2L1)]+ compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2 to give the final [(Me═N—R)L1L2]+Z− heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2 framework or the imido R group.
摘要翻译：本发明提供式（I）的放射性金属异复合物：[（Me-NR）L 1 L 2 + Z（I），其中Me，R，L ^{1 2＆lt; 2＆gt;和Z - - 具有说明书中指出的含义。络合物包括三价放射性金属 - 亚氨基，通常是锝或铼 - 酰亚胺基，其通过存在辅助三齿异二膦配体L 1 1强烈稳定，这允许形成取代 -inert [（Me-NR）L 1]部分。这些部分被固定在含有两个不稳定的，定形的Y（Y）的中间体[（Me-NR）Y 2 L 1 L 1）+ / 配体，其中Y优选为卤化物基团。后者容易被二齿配体L 2替代，得到最终的[（Me-NR）L 1 L 2 L 2 O 2 + - 异复合物。本发明的配合物可用于制备放射性药物：事实上，赋予生物寻靶特性的生物活性片段可以在L 2框架或亚氨基R基团上引入。}

9. 发明授权

US6127530A Method for the reduction of oxygenated compounds of rhenium or technetium 失效
标题翻译：还原铼或锝氧化化合物的方法
公开(公告)号：US6127530A
公开(公告)日：2000-10-03
申请号：US269898
申请日：1999-06-04
申请人： Adriano Duatti , Cristina Bolzati , Licia Uccelli , Rodolfo Franceschini , Alessandra Boschi
发明人： Adriano Duatti , Cristina Bolzati , Licia Uccelli , Rodolfo Franceschini , Alessandra Boschi
IPC分类号： A61K51/00 , A61K51/04 , A61K47/06 , C07F13/00
CPC分类号： A61K51/0478
摘要： The present invention relates in general to a method for the reduction of oxygenated compounds of rhenium and technetium and in particular to the reduction of perrhenate or pertechnetate ions.More particularly, the invention relates to reactions for the reduction of the said oxygenated compounds which are carried out in the course of the preparation of complexes of the radionuclides .sup.186 Re, .sup.188 Re and .sup.99m Tc; in these reactions, the radionuclide perrhenate or pertechnetate ion is reduced in the presence of a reducing agent and a ligand which can form a complex with the radionuclide in its reduced oxidation state.
摘要翻译： PCT No.PCT / EP97 / 05448 Sec。 371日期1999年6月4日第 102（e）日期1999年6月4日PCT 1997年10月3日PCT PCT。第WO98 / 14219号公报日本公开日1998年4月9日本发明一般涉及还原铼和锝的含氧化合物的方法，特别涉及铼酸盐或高锝酸盐离子的还原。更具体地，本发明涉及在制备放射性核素186Re，188Re和99mTc的络合物的过程中还原所述含氧化合物的反应; 在这些反应中，在还原剂和可以与其还原氧化态的放射性核素形成络合物的还原剂和配体的存在下，将高铼酸根离子或高锝酸根离子还原。

10. 发明授权

US07771704B2 Radioactive transition metal-imido hetero-diphosphine complexes, their preparation and radiopharmaceutical compositions thereof 失效
标题翻译：放射性过渡金属 - 亚氨基杂二膦配合物，它们的制备和放射性药物组合物
公开(公告)号：US07771704B2
公开(公告)日：2010-08-10
申请号：US12144370
申请日：2008-06-23
申请人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
发明人： Francesco Tisato , Cristina Bolzati , Marina Porchia , Fiorenzo Refosco
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07F13/005 , A61K51/0489 , C07B2200/05 , C07F9/5004
摘要： The present invention provides radioactive metal heterocomplexes of formula (I): [(Me=N—R)L1L2]+Z− wherein Me, R, L1L2 and Z− have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium-or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert [(Me=N—R)L1] moieties. Such moieties are fixed in an intermediate [(Me=N—R)Y2L1)]+ compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2 to give the final [(Me=N—R)L1L2]+ Z−heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2 framework or the imido R group.
摘要翻译：本发明提供式（I）的放射性金属异复合物：[（Me = N-R）L1L2] + Z-其中Me，R，L1L2和Z-具有说明书中所示的含义。络合物包括三价放射性金属 - 亚氨基，通常是锝或铼 - 亚胺基，其通过存在辅助三齿异二膦配体L1而稳定，其允许形成取代惰性的[（Me = N- R）L1]部分。这些部分固定在含有两个不稳定的，定位的Y配体的中间体[（Me = N-R）Y2L1）] +化合物中，其中Y优选为卤素基团。后者容易被二齿配体L2替代，得到最终的[（Me = N-R）L1L2] + Z-异构复合物。本发明的复合物可用于制备放射性药物：事实上，赋予生物靶标特性的生物活性片段可以引入到L2骨架或亚胺基R基团上。

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