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

A - Human Necessities – 61 – K

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A61K 51/04 (2006.01) A61K 31/7072 (2006.01) A61P 31/12 (2006.01) A61P 35/00 (2006.01) C07D 239/54 (2006.01) C07H 19/06 (2006.01) C07H 19/09 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2402991

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 concerne des médicaments renfermant comme ingrédient actif des composés étiquetés de manière radioactive de formule générale suivante ou des sels acceptables pharmaceutiquement correspondants. Dans ladite formule, R1 représente l'hydrogène ou C1-8 alkyl linéaire ou ramifié, R2 représente l'hydrogène, l'hydroxyle ou l'halogène, R3 représente l'hydrogène ou le fluor, R4 représente l'oxygène, le soufre ou le méthylène et R5 représente un halogène radioactif. Les médicaments sont stables dans le corps vivant et restent dans la cellule ou sont intégrés dans l'ADN. Ainsi, on les utilise dans le diagnostic de l'activité reproductrice tissulaire ou dans le traitement de maladies prolifératives.

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