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Metal complexes based on tetrathiol ligands and their application in nuclear medicine diagnostics and endoradione nuclide therapy as well as processes for the preparation of metal complexes

机译:基于四硫醇配体的金属配合物及其在核医学诊断和内啡肽核素治疗以及金属配合物制备方法中的应用

摘要

The object of the invention is to propose radiolytic and metabolically stable metal complexes which are suitable for conjugation with biomolecules, and to provide a process for their preparation. DOLLAR A The solution includes metal complexes based on tetrathiol ligands of the formula DOLLAR F1 wherein DOLLAR A (CH-R * 1) represents substituted or unsubstituted methylene bridges and DOLLAR AR * 1 * H, substituted or unsubstituted alkyl groups or substituted or unsubstituted aryl groups, m and n represent the number of methyl groups, the sum of m and n is between 4 and 10, DOLLAR AR · 2 · for H, OR · 1 · or NHR · 1 ·, DOLLAR AY 4 times H , 99m TcO, 186 ReO, 188 ReO, 99m TcN, 186 ReN or 188 ReN, DOLLAR AX for (CH) ¶2¶, the unsubstituted amino group (NH) or substituted Amino group (NZ), the guanidyl unit DOLLAR F2 or the urea group DOLLAR F3, DOLLAR A wherein DOLLAR AZ - (CH-R · 1 ·) -A means, p is the number of methylene groups and is between 2 and 8, DOLLAR AA represents a linkable unit, such as COOH, COR · 3 ·, -NCS and DOLLAR AR · 3 · fü r OH, OR · 1 · or NHR · 1 ·, DOLLAR A and the use of the metal complexes according to claim 1 for nuclear medical diagnostics and endoradione nuclide therapy. DOLLAR A In addition, a process for the preparation of the metal complexes is given.
机译:本发明的目的是提出适用于与生物分子结合的辐射分解和代谢稳定的金属配合物,并提供其制备方法。 DOLLAR A该溶液包括基于分子式DOLLAR F1的四硫醇配体的金属配合物,其中DOLLAR A(CH-R * 1)表示取代或未取代的亚甲基桥,DOLLAR AR * 1 * H,取代或未取代的烷基或取代或未取代的芳基基团,m和n代表甲基的数目,m和n的总和在4到10之间,DOLLAR AR·2·对于H,OR·1·或NHR·1·,DOLLAR AY 4倍H,99m TcO ,186 ReO,188 ReO,99m TcN,186 ReN或188 ReN,(CH)¶2¶的DOLLAR AX,未取代的氨基(NH)或取代的氨基(NZ),胍基单元DOLLAR F2或脲基DOLLAR F3,DOLLAR A,其中DOLLAR AZ-(CH-R·1·)-A表示,p是亚甲基的数目,在2至8之间,DOLLAR AA表示可连接的单元,例如COOH,COR·3· ,-NCS和DOLLAR AR·3·OH或OR·1·或NHR·1·DOLLAR A以及根据权利要求1的金属配合物在核医学诊断和内radi酮中的用途核素治疗。美元A此外,给出了制备金属络合物的方法。

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