Radioiodinated phenols for brachytherapy

A - Human Necessities – 61 – K

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A61K 51/04 (2006.01)

Patent

CA 2334146

The present invention concerns the use of a radioiodinated phenolic compound of formula (II) wherein: m and n are independently 0, 1, 2 or 3 X is a group that is negatively or positively charged at physiological pH, R, R1, R2 and R3 are independently hydrogen, C1-C4 alkyl, or a carboxyl group, and I* is 1231, 1311 or 1251, and its pharmaceutically-acceptable salts. The compound is formulated and used in vivo in an animal in brachytherapy in an implantable catheter. In addition, due to the rapid renal clearance of these compounds, they may be used to study renal function. A process to prepare these compounds is also disclosed.

L'invention concerne l'utilisation d'un composé phénolique radio-iodé représenté par la formule (II) dans laquelle m et n sont indépendamment 0, 1, 2 ou 3, X représente un groupe chargé négativement ou positivement au pH physiologique, R, R<1>, R<2> et R<3> représentent indépendamment hydrogène, alkyle C1-C4 ou un groupe carboxyle et I* représente <123>I, <131>I ou <125>I et ses sels acceptables sur le plan pharmaceutique. On formule ce composé et on l'utilise in vivo sur un animal en curiethérapie dans un cathéter implantable. De plus, étant donné leur élimination rénale rapide, on peut mettre en application ces composés afin d'étudier la fonction rénale. Elle concerne également un procédé servant à préparer ces composés.

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