Peptidomimetic inhibitors of psma, compounds comprising...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/22 (2006.01) A61K 31/66 (2006.01) A61P 13/08 (2006.01) A61P 35/00 (2006.01) C07C 229/24 (2006.01)

Patent

CA 2645809

Compounds of the formula, A-L-B, wherein A is glutamate or a glutamate analog; L is a phosphoramidate or a phosphoramidate analog; and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer; and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.

L'invention concerne des composés de formule A-L-B, où A est le glutamate ou un analogue de glutamate, L est un phosphoramidate ou un analogue de phosphoramidate et B est la sérine ou un analogue de la sérine, qui sont de puissants inhibiteurs de l'antigène spécifique de la membrane prostatique (PMSA). Ces composés sont utiles dans le traitement du cancer de la prostate et, lorsqu'ils sont liés chimiquement à un colorant fluorescent, ils permettent de marquer effacement et sélectivement les cellules cancéreuses prostatiques en vue de l'imagerie par fluorescence.

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