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公开(公告)号：US20090175775A1
公开(公告)日：2009-07-09
申请号：US10585294
申请日：2005-01-10
IPC分类号： C07F15/00 , C07F13/00 , C07F1/08 , C01B21/092
CPC分类号： C07D487/22 , A61K47/551 , A61K51/0453
摘要： The present invention relates to a metal complex of the general formula M(L)n, wherein each L is independently selected and represents a ligand and at least one L is vitamin B12 (cyanocobalamin) or a derivative thereof bound through the nitrogen atom of its cyanide group to M, which is an element selected from the transition metals, thus, forming a M-NC—[Co] moiety with [Co] representing vitamin B12 without cyanide and wherein n is 1, 2, 3, 4, 5 or 6. The complex can be prepared by mixing a precursor molecule with vitamin B12. The metal complexes can be used for radiodiagnostics, chemotherapy and radionuclide therapy.
摘要翻译： 本发明涉及一种通式M（L）n的金属络合物，其中每个L独立选择并代表一种配体，至少一种L是维生素B12（氰钴胺）或其衍生物，其结合在其的氮原子上 氰化物基团，其是选自过渡金属的元素，因此，形成具有代表不含氰化物的维生素B12的[Co]部分的M-NC- [Co]部分，并且其中n为1,2,3,4,5或 复合物可以通过将前体分子与维生素B12混合来制备。 金属络合物可用于放射诊断，化疗和放射性核素治疗。
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公开(公告)号：US07692002B2
公开(公告)日：2010-04-06
申请号：US10585294
申请日：2005-01-10
IPC分类号： C07D487/22 , C07F15/00 , C07F7/22 , C07H23/00
CPC分类号： C07D487/22 , A61K47/551 , A61K51/0453
摘要： The present invention relates to a metal complex of the general formula M(L)n, wherein each L is independently selected and represents a ligand and at least one L is vitamin B12 (cyanocobalamin) or a derivative thereof bound through the nitrogen atom of its cyanide group to M, which is an element selected from the transition metals, thus, forming a M-NC-[Co] moiety with [Co] representing vitamin B12 without cyanide and wherein n is 1, 2, 3, 4, 5 or 6. The complex can be prepared by mixing a precursor molecule with vitamin B12. The metal complexes can be used for radiodiagnostics, chemotherapy and radionuclide therapy.
摘要翻译： 本发明涉及一种通式M（L）n的金属络合物，其中每个L独立选择并代表一种配体，至少一种L是维生素B12（氰钴胺）或其衍生物，其结合在其的氮原子上 氰化物基团，其是选自过渡金属的元素，因此，形成具有代表不含氰化物的维生素B12的[Co]部分的M-NC- [Co]部分，并且其中n为1,2,3,4,5或 复合物可以通过将前体分子与维生素B12混合来制备。 金属络合物可用于放射诊断，化疗和放射性核素治疗。
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3.发明申请Cobalamine derivatives useful for diagnosis and treatment of abnormal cellular proliferation 失效用于诊断和治疗异常细胞增殖的钴胺衍生物公开(公告)号：US20070155692A1
公开(公告)日：2007-07-05
申请号：US10583760
申请日：2004-12-21
申请人： Hans-Jorg Treichler , Roger Alberto , Robert Waibel , Martin Kuenzi , Jakob Nuesch , Stefan Mundwiler , Dave van Staveren
发明人： Hans-Jorg Treichler , Roger Alberto , Robert Waibel , Martin Kuenzi , Jakob Nuesch , Stefan Mundwiler , Dave 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 (a) having no binding affinity or low binding affinity to the transport protein transcobalamin II TCII) and (b) 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 comprising (a) exposing the mammal to a period of a vitamin B12-free diet, and (b) 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 offspring in neoplastic tissue is much reduced.
摘要翻译： 本发明涉及对运输蛋白转铁蛋白II TCII没有结合亲和力或低结合亲和力的钴胺素衍生物（a））和（b）保留作为维生素B12替代物的活性，任选地携带治疗和/或诊断剂，例如 放射性金属。 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和治疗哺乳动物的微生物的肿瘤疾病或感染的方法，其包括（a）将哺乳动物暴露于不含维生素B12的饮食期间，以及（b）随后应用 携带诊断和/或治疗剂的本发明的钴胺素衍生物。 通过选择作为维生素B12替代物的钴胺素衍生物，在肿瘤组织中形成抗性后代的风险大大降低。
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4.发明授权Cobalamine derivatives useful for diagnosis and treatment of abnormal cellular proliferation 失效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。
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5.发明申请Preparation of m(co)3-complexes by solid phase techniques via metal assisted cleavage from the solid support 审中-公开通过固相技术通过金属辅助裂解从固体支持物制备m（共）3-络合物公开(公告)号：US20060165594A1
公开(公告)日：2006-07-27
申请号：US10525152
申请日：2003-09-02
申请人： Roger Alberto , Stefan Mundwiler
发明人： Roger Alberto , Stefan Mundwiler
CPC分类号： A61K51/025 , C07B2200/11 , C07F13/005
摘要： The present invention relates to a process for generating a water soluble metal complexed agent, comprising contacting a solid phase bound organic conjugate represented by the formula I with [M(H2O)3(CO)3]n+, under suitable conditions to cause the formation of a coordinate bond between [M(H2O)3(CO)3]n+ and the tertiary amine nitrogen atom of the solid phase bound organic conjugate and thereby the release of the metal complexed agent thus formed from the support. The invention further relates to the conjugate of formula (I) and to a kit for performing the process.
摘要翻译： 本发明涉及一种产生水溶性金属络合剂的方法，包括使由式I表示的固相结合的有机共轭与[M（H 2 H 2 O）3 在适合的条件下，使[M（H 2 H 2 O）2 +（CO）3 N] 因此，固相结合有机共轭物的叔胺氮原子，从而释放金属络合剂，因此， 由支持形成。 本发明还涉及式（I）的缀合物和用于进行该方法的试剂盒。
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