首页> 外国专利> 18F FLUORO-BENZOYL LABELLED BIOLOGICAL ACTIVE COUMPOUNDS AS DIAGNOSITIC IMAGING AGENTS AS WELL AS BENZOTRIAZOL-1-YLOXY-BENZOYL, 2,5-DIOXO-PYRROLIDIN-1-YLOXY) BENZOYL AND TRIMETHYLAMMONIO-BENZOYL PRECURSERS

18F FLUORO-BENZOYL LABELLED BIOLOGICAL ACTIVE COUMPOUNDS AS DIAGNOSITIC IMAGING AGENTS AS WELL AS BENZOTRIAZOL-1-YLOXY-BENZOYL, 2,5-DIOXO-PYRROLIDIN-1-YLOXY) BENZOYL AND TRIMETHYLAMMONIO-BENZOYL PRECURSERS

机译:18F氟-苯并标记的生物活性化合物作为诊断成像剂,以及苯并三唑-1-羟基-苯甲酰基,2,5-二氧代-吡咯烷-1-基苯甲酰和三甲基氨-苯甲酰前体

摘要

The present invention relates to radiolabelled substitute benzene compounds for diagnostic imaging. The present invention provides methods for preparation of such compounds, in particular, preparation of novel compounds which serve as precursors for 18F-labeling, and the use of thus 18F-labe!ed compounds for diagnostic imaging. Formula (A), wherein one of -Y1, -Y2, -Y3 Y4 and -Y5 is -A-B-D-P, wherein -A-B-D- is a bond or spacer, P is peptide, peptidomimetic, oligonucleotide or small molecule. K is LG-O or W, wherein: LG- is selected from the group comprising Formula (B), wherein T is H or Cl, Q is CH or N, K is absent or is C=O. W is radioactive or non-radioactive isotope of fluorine, more preferably 18F.
机译:本发明涉及用于诊断成像的放射性标记的取代苯化合物。本发明提供了制备此类化合物的方法,特别是制备了用作18 F-标记前体的新型化合物,以及由此标记的18 F-化合物用于诊断成像的用途。式(A),其中-Y 1,-Y 2,-Y 3,Y 4和-Y 5之一是-A-B-D-P,其中-A-B-D-是键或间隔基,P是肽,拟肽,寡核苷酸或小分子。 K为LG-O或W,其中:LG-选自式(B),其中T为H或Cl,Q为CH或N,不存在K或为C = O。 W是氟的放射性或非放射性同位素,更优选为18F。

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