4-fluoroalkyl-3-halophenyl nortropanes

A - Human Necessities – 61 – K

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Details

A61K 51/00 (2006.01) A61K 49/04 (2006.01) A61K 49/06 (2006.01) A61K 51/04 (2006.01) C07D 451/02 (2006.01) C07D 451/04 (2006.01) C07D 451/06 (2006.01)

Patent

CA 2369663

A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes family are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transporter protein with high affinity and selectivity. The invention provides methods of synthesis which incorporate radioisotopic halogens at a last step which permit high radiochemical yield and maximum usable product life. The radiolabeled compounds of the invention are useful as imaging agents for visualizing the location and density of serotonin transporter by PET and SPECT imaging.

Cette invention concerne une série de composés de la familles des 4-fluoroalkyl-3-halophényl nortropanes convenant comme agents diagnostiques et thérapeutiques pour des maladies en rapport avec un dysfonctionnement du transporteur de la sérotonine. Ces composés se lient à une protéine transporteuse de la sérotonine par affinité et sélectivité élevées. La présente invention concerne des procédés de synthèse qui intègrent en dernière instance des halogènes radio-isotopiques permettant un rendement radiochimique élevé et un durée de vie utile maximale du produit. Les composés radiomarqués selon l'invention conviennent comme agents imageurs pour la visualisation de l'emplacement et de la densité de transporteur de la sérotonine par imagerie PET (tomographie par émission de positrons) et SPECT (tomographie d'émission monophotonique).

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