Drugs for the diagnosis of tissue-reproductive activity or...

A - Human Necessities – 61 – K

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A61K 51/04 (2006.01) A61K 31/7042 (2006.01) A61K 31/7072 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2618466

An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: (see formula I) wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1-8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

L'invention porte sur un agent qui comprend un composé radiomarqué, comme ingrédient actif, représenté par la formule suivante, ou un sel pharmaceutiquement acceptable de celui-ci : (voir formule I) où R1 représente un hydrogène ou un groupe alkyle linéaire ou ramifié ayant 1-8 atomes de carbone, R2 représente un hydrogène ou un substituant hydroxyle ou halogène, R3 représente un substituant hydrogène ou fluor, R4 représente un oxygène, un souffre ou un substituant méthylène et R5 représente un substituant halogène radioactif. Comme l'agent est stable in vivo et demeure dans les cellules ou est intégré à l'ADN, il peut ainsi servir au diagnostic d'une prolifération tissulaire ou au traitement d'une maladie proliférative.

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