Hydroxy-phosphinyl derivatives useful as naaladase inhibitors

C - Chemistry – Metallurgy – 07 – F

Patent

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Details

C07F 9/30 (2006.01) A61K 31/194 (2006.01) A61K 31/66 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07F 9/38 (2006.01) C07F 9/40 (2006.01) C07F 9/44 (2006.01) C07F 9/572 (2006.01) C07F 9/58 (2006.01) C07F 9/655 (2006.01) C07F 9/6553 (2006.01)

Patent

CA 2258587

The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

La présente invention concerne des inhibiteurs de dipeptidases et plus particulièrement des nouveaux dérivés phosphonates, hydroxyphosphinyles et phosphoramidates, lesquels inhibent l'activité enzymatique de la dipeptidase N-acétylée, à liaison .alpha., et acide (NAALADase). On décrit également des compositions pharmaceutiques contenant de tels dérivés ainsi que des procédés d'utilisation de ceux-ci pour inhiber l'activité NAALADase et traiter des maladies de la prostate, notamment à l'aide des composés de l'invention, destinés à inhiber la croissance des cellules du cancer de la prostate.

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