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1. 发明授权

US09512156B2 Carbon monoxide releasing rhenium compounds for medical use 有权
标题翻译：一氧化碳释放用于医疗用途的铼化合物
公开(公告)号：US09512156B2
公开(公告)日：2016-12-06
申请号：US13583390
申请日：2011-03-04
申请人： Fabio Zobi , Roger Alberto , Lukas Kromer
发明人： Fabio Zobi , Roger Alberto , Lukas Kromer
IPC分类号： A61K31/55 , A61K31/714 , A61K33/24 , C01G47/00 , C07F13/00 , C07H23/00 , A61P9/00 , A61P9/10 , A61P29/00 , A61P7/02 , A61P35/00 , A61P15/00 , A61P11/00 , A61P9/12 , A61P11/06 , A61P25/00 , A61P13/12 , A61P1/16
CPC分类号： A61K33/24 , A61K31/555 , C07F13/00 , C07F13/005
摘要： The present invention relates to new rhenium compounds of formula (I) with medical utility, corresponding pharmaceutical compositions as well as medical uses thereof.
摘要翻译：具有医疗实用性，相应的药物组合物及其医疗用途。

2. 发明授权

US07188725B2 Kits for preparing transition metal carbonyl complexes 有权
标题翻译：制备过渡金属羰基络合物的试剂盒
公开(公告)号：US07188725B2
公开(公告)日：2007-03-13
申请号：US11237374
申请日：2005-09-28
申请人： Roger Alberto , Roger Schibli
发明人： Roger Alberto , Roger Schibli
IPC分类号： B65D83/10 , B65D85/00
CPC分类号： C07F5/022
摘要： The present invention relates to kits including compounds that may be used as a carbon monoxide source and optionally as a reducing agent in the preparation of transition metal carbonyl complexes.
摘要翻译：本发明涉及试剂盒，其包括可用作一氧化碳源的化合物，并且任选地用作制备过渡金属羰基络合物中的还原剂。

3. 发明授权

US06926883B1 Group (VII) transition-metal complexes with multidentate aminopolycarboxylate ligands and a kit for producing them 失效
标题翻译：具有多齿氨基多羧酸盐配体的（VII）族过渡金属配合物和用于制备它们的试剂盒
公开(公告)号：US06926883B1
公开(公告)日：2005-08-09
申请号：US10030741
申请日：2000-06-28
申请人： Mary M. Dyszlewski , Roger Alberto , Joseph E. Bugaj
发明人： Mary M. Dyszlewski , Roger Alberto , Joseph E. Bugaj
IPC分类号： A61K49/00 , A61K51/04 , C07F5/00 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0497
摘要： The invention relates to novel aminocarboxylate ligands that are suitable for complexing with a radionuclide, and are useful as imaging agents for diagnostic purposes. In accordance with the present invention, a method of preparing a compound of formula (I): fac-[M(CO)3(OH2)3]+, wherein M is Mn, 99mTc, 186Re or 188Re, involves reacting a metal in permetallate form with carbon monoxide and a reducing agent, wherein a mixture of a basic borate buffer and a reducing agent soluble in water but not substantially decomposed by water is solved in a water containing solvent system containing a solution of the metal in permanganate, pertechnetate or perrhenate form in the presence of carbon monoxide. The compound of formula (I) can be reacted with a ligand Lx to form a compound of formula (II): fac-[M(CO)3(X)2L1]n, wherein M is as defined above Lx is a multidentate ligand, and n is a charge of the ligand Lx increased with one + charge. The invention also is directed to novel compounds, and kits for carrying out the disclosed methods.
摘要翻译：本发明涉及适用于与放射性核素络合的新型氨基羧酸酯配体，并且可用作诊断目的的成像剂。根据本发明，制备式（I）化合物的方法：fac- [M（CO）3'（OH 2）3）其中M是Mn，99m Tc，186 Re或188 Re，包括使具有一氧化碳和还原剂的多金属盐形式的金属，其中碱性硼酸盐缓冲剂和可溶于水但基本上不被水分解的还原剂的混合物溶解在含有金属溶液在高锰酸盐溶液中的含水溶剂体系中，高铁酸盐或高铼酸盐形式存在一氧化碳。式（I）化合物可以与配体L x x化合物反应以形成式（II）化合物：fac- [M（CO）3（X）其中M如上所定义，L x X是多齿配体，n是配体L x x的电荷随着+电荷而增加。本发明还涉及用于实施所公开的方法的新化合物和试剂盒。

4. 发明授权

US06344178B1 Method for the preparation of facial metal tricarbonyl compounds and their use in the labelling of biologically active substrates 有权
标题翻译：制备面部金属三羰基化合物的方法及其在生物活性底物标记中的应用
公开(公告)号：US06344178B1
公开(公告)日：2002-02-05
申请号：US09403704
申请日：1999-10-22
申请人： Roger Alberto , Roger Schibli , André Egli
发明人： Roger Alberto , Roger Schibli , André Egli
IPC分类号： A61K4900
CPC分类号： A61K51/088 , A61K51/085 , C07F13/005
摘要： The invention relates to a method of preparing facial metal tricarbonyl compounds and further coordinated facial metal tricarbonyl compounds in water or an aqueous medium. The invention further relates to the use of said facial metal tricarbonyl compounds in the labelling of biologically active substrates and other ligands, and to a kit for preparing a facial metal tricarbonyl compound or further coordinated facial metal tricarbonyl compounds.
摘要翻译：本发明涉及一种在水或水介质中制备面部金属三羰基化合物和进一步配位的面部金属三羰基化合物的方法。本发明还涉及所述面部金属三羰基化合物在生物活性底物和其它配体的标记中的用途，以及用于制备面部金属三羰基化合物或进一步配位的面部金属三羰基化合物的试剂盒。

5. 发明授权

US08961924B2 Metal complexes 有权
标题翻译：金属配合物
公开(公告)号：US08961924B2
公开(公告)日：2015-02-24
申请号：US12921794
申请日：2009-03-10
申请人： Roger Alberto , Henrik Braband
发明人： Roger Alberto , Henrik Braband
IPC分类号： A61K51/00 , A61M36/14 , A61K51/04 , C07F13/00
CPC分类号： A61K51/0482 , C07F13/005
摘要： A method for synthesizing a complex having the formula: [L3MO3]″ wherein L3 represents a tridentate ligand, M represents a metal selected from Tc an Re, and n is a charge from −2 to +1, the method comprising: a) reaction of pertechnetate or perrhenate with a reducing agent and L3, or b) reaction of pertechnetate or perrhenate with a Lewis acid and L3, wherein the synthesis (a) or (b) is carried out in an aqueous medium.
摘要翻译：一种合成具有下式的络合物的方法：其中L3表示三齿配体，M表示选自Tc-Re的金属，n为-2至+1的电荷，该方法包括：a）反应的高锝酸盐或高铼酸盐与还原剂和L3反应，或b）高锝酸盐或高铼酸盐与路易斯酸和L3的反应，其中合成（a）或（b）在水性介质中进行。

6. 发明授权

US08512675B2 N and/or Nα derivatized, metal and organic protected L-histidine for coupling to biomolecules for highly efficient labeling with [M(OH2)3 (CO)3]+ by fac coordination 失效
标题翻译： N和/或Nalpha衍生的金属和有机保护的L-组氨酸，用于偶联到生物分子，用[M（OH）3（CO）3] +进行高效标记，通过fac协调
公开(公告)号：US08512675B2
公开(公告)日：2013-08-20
申请号：US10554331
申请日：2004-04-29
申请人： Roger Alberto , Jae Kyoung Pak
发明人： Roger Alberto , Jae Kyoung Pak
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： G01N33/6842 , C07D233/64 , C07D487/04 , C07K5/06139 , C07K7/083 , C07K7/086 , C07K14/5421 , C07K14/595 , C07K14/655 , C07K14/685 , G01N33/68
摘要： The present invention relates to novel histidine derivates that can be used for the labeling of biomolecules with radioactive metal tricarbonyls. The new derivatives have a histidine that is derivatized at the Nε and at least protected at the Nα and optionally at the Nδ; or derivatized at the Nα and at least protected at the Nα and optionally at the Nδ; or derivatized at the Nε and Nα and at least protected at the Nα and optionally at the Nδ; or derivatized at the Nε; or derivatized at the Nα; or derivatized at the Nε and Nα; or at least protected at the Nα and optionally at the Nδ.
摘要翻译：本发明涉及可用于用放射性金属三羰基标记生物分子的新型组氨酸衍生物。新衍生物具有在Nepsilon衍生的组氨酸，并且至少在Nalpha和任选地在Ndelta保护; 或在Nalpha衍生并至少在Nalpha和任选地在Ndelta保护; 或在Nepsilon和Nalpha衍生，并至少在Nalpha和任选地在Ndelta保护; 或在Nepsilon衍生化; 或在Nalpha衍生化; 或在Nepsilon和Nalpha衍生化; 或至少保护在Nalpha和任选在Ndelta。

7. 发明申请

US20120328712A1 CARBON MONOXIDE RELEASING RHENIUM COMPOUNDS FOR MEDICAL USE 有权
标题翻译：一氧化碳释放铑化合物用于医疗用途
公开(公告)号：US20120328712A1
公开(公告)日：2012-12-27
申请号：US13583390
申请日：2011-03-04
申请人： Fabio Zobi , Roger Alberto , Lukas Kromer
发明人： Fabio Zobi , Roger Alberto , Lukas Kromer
IPC分类号： A61K31/555 , A61K31/714 , A61K33/24 , C01G47/00 , C07F13/00 , C07H23/00 , A61P9/00 , A61P9/10 , A61P29/00 , A61P7/02 , A61P35/00 , A61P15/00 , A61P11/00 , A61P9/12 , A61P11/06 , A61P25/00 , A61P13/12 , A61P1/16 , C12N5/071 , A61K31/28
CPC分类号： A61K33/24 , A61K31/555 , C07F13/00 , C07F13/005
摘要： The present invention relates to new rhenium compounds of formula (I) with medical utility, corresponding pharmaceutical compositions as well as medical uses thereof.
摘要翻译：本发明涉及具有医疗实用性，相应的药物组合物以及其医疗用途的式（I）的新的铼化合物。

8. 发明申请

US20110065680A1 Metal Complexes 有权
标题翻译：金属配合物
公开(公告)号：US20110065680A1
公开(公告)日：2011-03-17
申请号：US12921794
申请日：2009-03-10
申请人： Roger Alberto , Henrik Braband
发明人： Roger Alberto , Henrik Braband
IPC分类号： A61K31/555 , C07F13/00 , A61K31/28
CPC分类号： A61K51/0482 , C07F13/005
摘要： A method for synthesizing a complex having the formula: [L3MO3]″ wherein L3 represents a tridentate ligand, M represents a metal selected from Tc an Re, and n is a charge from −2 to +1, the method comprising: a) reaction of pertechnetate or perrhenate with a reducing agent and L3, or b) reaction of pertechnetate or perrhenate with a Lewis acid and L3, wherein the synthesis (a) or (b) is carried out in an aqueous medium.
摘要翻译：一种合成具有下式的络合物的方法：其中L3表示三齿配体，M表示选自Tc-Re的金属，n为-2至+1的电荷，该方法包括：a）反应的高锝酸盐或高铼酸盐与还原剂和L3反应，或b）高锝酸盐或高铼酸盐与路易斯酸和L3的反应，其中合成（a）或（b）在水性介质中进行。

9. 发明授权

US07585852B2 Cobalamine derivatives useful for diagnosis and treatment of abnormal cellular proliferation 失效
标题翻译：用于诊断和治疗异常细胞增殖的钴胺衍生物
公开(公告)号：US07585852B2
公开(公告)日：2009-09-08
申请号：US10583760
申请日：2004-12-21
申请人： Hans-Jörg Treichler , Roger Alberto , Robert Waibel , Martin T. Küenzi , Jakob Nüesch , Stefan Mundwiler , Dave R. van Staveren
发明人： Hans-Jörg Treichler , Roger Alberto , Robert Waibel , Martin T. Küenzi , Jakob Nüesch , Stefan Mundwiler , Dave R. van Staveren
IPC分类号： A61K31/714 , C07H23/00
CPC分类号： C07H23/00 , A61K51/041 , A61K51/0482 , A61K51/0497
摘要： The invention relates to cobalamin derivatives having no or low binding affinity to the transport protein transcobalamin II (TCII) and retaining activity as a vitamin B12 substitute, optionally carrying a therapeutic and/or diagnostic agent, such as a radioactive metal. These compounds have a much reduced accumulation rate in blood and benign organs, such as kidney and liver, compared to the accumulation rate in neoplastic tissues, and are more rapidly eliminated from blood. The invention further relates to a method of diagnosis and a method of treatment of a neoplastic disease or an infection by microorganisms in a mammal by exposing the mammal to a period of a vitamin B12 free diet, and subsequently applying a cobalamin derivative of the invention carrying a diagnostic and/or therapeutic agent. By selecting cobalamin derivatives acting as vitamin B12 substitutes, the risk of the formation of resistant off-spring in neoplastic tissue is much reduced.
摘要翻译：本发明涉及对运输蛋白质转氨酶II（TCII）没有或低结合亲和力的维生素B12替代物，可选地携带治疗和/或诊断剂例如放射性金属的保留活性的钴胺素衍生物。与肿瘤组织中的积累率相比，这些化合物在血液和良性器官如肾脏和肝脏中的积聚速率大大降低，并且从血液中更快速地消除。本发明还涉及一种诊断方法以及通过将哺乳动物暴露于维生素B12游离饮食期间，治疗哺乳动物的肿瘤性疾病或微生物感染的方法，随后将本发明的钴胺素衍生物携带诊断和/或治疗剂。通过选择作为维生素B12替代物的钴胺素衍生物，在肿瘤组织中形成抵抗弹簧的风险大大降低。

10. 发明申请

US20070065485A1 Therapeutic delivery of carbon monoxide 审中-公开
标题翻译：治疗性输送一氧化碳
公开(公告)号：US20070065485A1
公开(公告)日：2007-03-22
申请号：US10567157
申请日：2004-08-04
申请人： Roberto Motterlini , Roger Alberto
发明人： Roberto Motterlini , Roger Alberto
IPC分类号： A61F13/00
CPC分类号： A61K31/69 , A01N1/0226 , A61K31/416 , A61K45/06 , A61K2300/00
摘要： Boranocarbonates are described for administration to a human or other mammal for delivery of carbon monoxide. The boranocarbonate is a compound or ion adapted to make CO available for physiological effect, and may be administered with a guanylate cyclase stimulant or stabilizer. The physiological effect may be stimulation of neurotransmission, vasodilation or smooth muscle relaxation.
摘要翻译：描述了用于向人或其他哺乳动物施用一氧化碳的硼烷化碳。硼烷碳酸酯是适于使CO可用于生理效应的化合物或离子，并且可以与鸟苷酸环化酶刺激剂或稳定剂一起施用。生理作用可能是刺激神经传递，血管舒张或平滑肌松弛。

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