首页> 外国专利> NEW 2, 1 L -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

NEW 2, 1 L -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:新型2,1 L -DIAZA- [3.3](2,6)吡啶并烷化合物及其作为基本金属离子MRI造影剂和52MN基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.
机译:本发明的一个主题是通式(I)的化合物,其异构体,其生理上可接受的盐和/或Mn(II),Fe(II),Fe(III),Co(II)和Ni(II)复合体。本发明的另一个主题是上述化合物的应用。通式(I)的化合物:其中-NRR1基团可表示:a)-在环中具有N原子的-NRR1是指4至7的环,在某些情况下可包含另一个杂原子,在特定情况下该环可以被被-COOH,-OH,-OCH3,-NO2,-NH2,-NCS,-NHS-活化的酯,芳基(具有5-7个碳原子)取代的芳基(具有5-7个碳原子)取代-NRR1基团中的,或硝基,氨基或异硫氰酸酯基,或b)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(碳数为1-6),R4为H原子,烷基(具有1至6个碳原子)或-(CH2)n-COOH基团,而n = 1至10的整数或c)-NRR1基团是以下基团之一:(式II),而R2是H原子,羧基或烷基羰基(具有1-4个碳原子);(式III),R 2是H原子或烷基或芳基(具有1-6个碳原子),并且X是彼此独立的。 H原子,-CH3,-COOH,-OH,-OCH3,烷氧基-(具有2至6个碳原子),-NO2, -NH 2,-NCS,-NHS活化的酯,烷基(2至12个碳原子)或芳基(5至7个碳原子),在某些情况下后者可以被羟基,羟基烷基(1至6个)取代碳原子),硝基,氨基或异硫氰酸酯基团。

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