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2,11-diaza-3.3(2,6)pyridinophane compounds and their application as ligands of essential metal ion based MRI contrast agents and 52MN based PET contrast agents

机译:2,11- diaza-[3.3](2,6)吡啶酚化合物及其作为基于必需金属离子的MRI造影剂和52mN的PET造影剂的配体的应用

摘要

The one subject of the invention is the compounds of general formula (I), their isomers, their physiologically acceptable salts and/or Mn(II), Fe(II), Fe(III), Co(II) and Ni(II) complexes. The other subject of the invention is the application of the above compounds. The compounds of general formula (I): wherein —NRR1 group may refer to: a) —NRR1 with N atom in the ring means a ring of 4 to 7, that in certain cases may contain another heteroatom, and in specific cases the ring may be replaced with an aryl group (of 5 to 7 carbon atoms) substituted with —COOH, —OH, —OCH3, —NO2, —NH2, —NCS, —NHS-activated ester, aryl (of 5 to 7 carbon atoms), or nitro-, amino- or isothiocyanate group, or b) in the —NRR1 group R means a H atom, alkyl, aryl, nitroaryl, aminoaryl or isothiocyanate-aryl group (of 1 to 6 carbon atoms) and R4 is a H atom, alkyl (of 1 to 6 carbon atoms) or —(CH2)n—COOH group, whereas n=1 to 10 integer, or c) —NRR1 group is one of the following groups: (formula II) whereas R2 is a H atom, carboxyl- or alkyl-carbonyl group (of 1 to 4 carbon atoms); (formula III) and R2 is a H atom or alkyl or aryl group (of 1 to 6 carbon atoms), and X means independently from one another H atom, —CH3, —COOH, —OH, —OCH3, alkoxy- (of 2 to 6 carbon atoms), —NO2, —NH2, —NCS, —NHS-activated ester, alkyl (of 2 to 12 carbon atoms) or aryl (of 5 to 7 carbon atoms) group, in certain cases the latter may be substituted with hydroxyl, hydroxyalkyl (of 1 to 6 carbon atoms), nitro, amino or isothiocyanate group.; embedded image
机译:本发明的一个主题是通式(I)的化合物,其异构体,其生理学上可接受的盐和/或Mn(II),Fe(II),Fe(III),CO(II)和Ni(II)复合物。本发明的另一个主题是应用上述化合物。通式(I)的化合物:其中-NRR 1 组可以参考:a) - 在环中的n原子中的-nrr 1 表示4到7的环在某些情况下,在某些情况下可含有另一种杂原子,并且在特定情况下,环可以用被-COOH,-OH,-OCH 3 2 ,-nh 2 ,-ncs,-nhs-活性酯,芳基(5至7个碳原子),或硝基,氨基或异硫氰酸酯基团或b)在-NRR 1 Group r表示H原子,烷基,芳基,硝基芳基,氨基芳基或异硫氰酸酯 - 芳基(1至6个碳原子)和R 4 < /亚>是H原子,烷基(1至6个碳原子)或 - (ch 2 n -COOH基团,而n = 1至10个整数,或c)-NRR 1 组是以下基团之一:(公式II),而R 2 是H原子,羧基或烷基 - 羰基(1到4个碳原子); (式III)和R 2 是H原子或烷基或芳基(芳基(碳原子),X装置独立于另一个H原子,-CH 3 ,-COOH,-OH,-OCH 3 ,烷氧基 - (2至6个碳原子), - NO 2 ,-nh 2 ,-NC,-NHS活化酯,烷基(2至12个碳原子)或芳基(5至7个碳原子)组中,后者可以被羟基,羟烷基(1至6个)取代碳原子),硝基,氨基或异硫氰酸酯基团; <化学ID =“Chem-US-00001”> “嵌入式图像”文件=“US10968224-20210406-C00001.gif”他=“250.53mm”ImgContent

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