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1. 发明授权

US5373093A Macrocyclic complexes of yttrium, the lanthanides and the actinides having peripheral coupling functionalities 失效
标题翻译：钇，镧系元素和具有外围偶联官能团的锕系元素的大环络合物
公开(公告)号：US5373093A
公开(公告)日：1994-12-13
申请号：US669833
申请日：1991-03-15
申请人： Lidia M. Vallarino , Robert C. Leif
发明人： Lidia M. Vallarino , Robert C. Leif
IPC分类号： G01N33/533 , A61K31/555 , A61K33/24 , A61K49/00 , A61K49/06 , A61K51/00 , A61P35/00 , A61P37/00 , C07D471/18 , C07D487/18 , C07D491/18 , C07D495/18 , C07D513/18 , C07F5/00 , G01N33/58 , A61K39/395 , C07D221/00
CPC分类号： C07D471/18 , A61K49/06 , C07D491/18 , C07D495/18 , G01N33/582 , G01N2458/40
摘要： Functionalized water soluble macrocyclic complexes of lanthanide, actinide and yttrium ions were obtained by metal templated, Schiff-base, cyclic condensation of: (1) a functionalized 1,2-diaminoethane and a dicarbonyl compound selected from the group consisting of 2,6-dicarbonylpyridine, 2,6-diformylpyridine, 2,5-dicarbonylfuran, 2,5-diformylfuran, 2,5-dicarbonylthiophene and 2,5-diformylthiophene; or (2) 1,2-diaminoethane and a ring-substituted heterocyclic dicarbonyl compound selected from a group consisting of substituted 2,6-dicarbonylpyridine, substituted 2,6-diformylpyridine, substituted 2,5-dicarbonylfuran, substituted 2,5-diformylfuran; substituted 2,5-dicarbonyl thiophene, and substituted 2,5-diformylthiophene. Coordination complexes thus formed are kinetically stable in dilute aqueous solution. They are further reacted, or coupled, through a substituent on the 1,2-diaminoethane or on the pyridine, furan, or thiophene moieties, to one of the following: proteinaceous materials, polysaccharides, other biologically compatible macromolecules or bridging molecules which, can be further reacted or coupled to the above mentioned substrates. These macrocyclic complexes are suitable in the preparation of reporter molecules and for magnetic resonance, radiation imaging and radiation therapy.
摘要翻译：通过金属模板化，席夫碱，环状缩合得到镧系元素，锕系元素和钇离子的官能化水溶性大环络合物：（1）官能化的1,2-二氨基乙烷和选自2,6-二甲基苯基的二羰基化合物，二羰基吡啶，2,6-二甲酰基吡啶，2,5-二羰基呋喃，2,5-二甲基呋喃，2,5-二羰基噻吩和2,5-二甲基噻吩; 或（2）1,2-二氨基乙烷和环取代的杂环二羰基化合物，其选自取代的2,6-二羰基吡啶，取代的2,6-二甲酰基吡啶，取代的2,5-二羰基呋喃，取代的2,5-二甲基呋喃 ; 取代的2,5-二羰基噻吩和取代的2,5-二甲酰基噻吩。如此形成的配位络合物在稀水溶液中动力学稳定。它们进一步通过1,2-二氨基乙烷或吡啶，呋喃或噻吩部分上的取代基反应或偶联到以下之一：蛋白质材料，多糖，其它生物相容性大分子或桥接分子，其可以进一步反应或耦合到上述基底。这些大环配合物适用于报道分子的制备和磁共振，放射成像和放射治疗。

2. 发明授权

US5696240A Macrocyclic complexes of yttrium, the lanthanides and the actinides having peripheral coupling functionalities 失效
标题翻译：钇，镧系元素和具有外围偶联官能团的锕系元素的大环络合物
公开(公告)号：US5696240A
公开(公告)日：1997-12-09
申请号：US351827
申请日：1994-12-08
申请人： Lidia M. Vallarino , Robert C. Leif
发明人： Lidia M. Vallarino , Robert C. Leif
IPC分类号： C07F5/00 , G01N33/58 , A61K49/00 , A61B5/055 , A61K39/395
CPC分类号： C07F5/003 , G01N33/582 , G01N2458/40
摘要： Symmetrically di-functionalized water soluble macrocyclic complexes of lanthanide, actinide and yttrium ions were obtained by metal templated, Schiff-base, cyclic condensation of: (1) a functionalized 1,2-diaminoethane and a dicarbonyl compound selected from the group consisting of 2,6-dicarbonylpyridine, 2,6-diformylpyridine, 2,5-dicarbonylfuran, 2,5-diformylfuran, 2,5-dicarbonyl-thiophene and 2,5-diformylthiophene; or (2) 1,2-diaminoethane and a ring-substituted heterocyclic dicarbonyl compound selected from a group consisting of substituted 2,6-dicarbonylpyridine, substituted 2,6-diformylpyridine, substituted 2,5-dicarbonylfuran, substituted 2,5-diformylfuran; substituted 2,5-dicarbonyl thiophene, and substituted 2,5-diformylthiophene. Asymmetrically functionalized water soluble macrocyclic complexes of the lanthanide, actinide and yttrium ions were obtained by metal templated, Schiff-base, cyclic condensation of appropriately substituted diamine and dicarbonyl precursors, with such precursors contributing two heteroaromatic moieties (pyridine, furan, thiophene, or a combination thereof) to the resulting macrocyclic structure. The coordination complexes thus formed are kinetically stable in dilute aqueous solution. They are further reacted, or coupled, through a substituent on the 1,2-diaminoethane or on the pyridine, furan, or thiophene moieties, to one of the following: proteinaceous materials, polysaccharides, polynucleotides, other biologically compatible macromolecules or bridging molecules which, can be further reacted or coupled to the above mentioned substrates. These macrocyclic complexes are suitable in the preparation of reporter molecules and for magnetic resonance, radiation imaging and radiation therapy.
摘要翻译：通过金属模板化，席夫碱，环状缩合获得镧系元素，锕系元素和钇离子的对称二官能化的水溶性大环络合物：（1）官能化的1,2-二氨基乙烷和二羰基化合物，其选自2 ，6-二羰基吡啶，2,6-二甲酰基吡啶，2,5-二羰基呋喃，2,5-二甲基呋喃，2,5-二羰基噻吩和2,5-二甲基噻吩; 或（2）1,2-二氨基乙烷和环取代的杂环二羰基化合物，其选自取代的2,6-二羰基吡啶，取代的2,6-二甲酰基吡啶，取代的2,5-二羰基呋喃，取代的2,5-二甲基呋喃 ; 取代的2,5-二羰基噻吩和取代的2,5-二甲酰基噻吩。通过金属模板化，席夫碱，适当取代的二胺和二羰基前体的环缩合获得镧系元素，锕系元素和钇离子的不对称官能化的水溶性大环络合物，其中这些前体贡献两个杂芳族部分（吡啶，呋喃，噻吩或其组合）与所得的大环结构。如此形成的配位络合物在稀水溶液中动力学稳定。它们进一步通过1,2-二氨基乙烷或吡啶，呋喃或噻吩部分上的取代基反应或偶联到以下之一：蛋白质材料，多糖，多核苷酸，其它生物相容性大分子或桥接分子，其中，可进一步反应或与上述底物偶联。这些大环配合物适用于报道分子的制备和磁共振，放射成像和放射治疗。

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