Smart pro-drugs of serine protease inhibitors

Details Smart pro-drugs of serine protease inhibitors Smart pro-drugs of serine protease inhibitors

A - Human Necessities

61

K

A61K 38/00 (2006.01) C07K 5/06 (2006.01) C07K 5/08 (2006.01) C07K 5/10 (2006.01) C07K 7/06 (2006.01)

Patent

CA 2484551

The present invention relates to prodrugs of protease inhibitors, such as inhibitors of proteosome, DPOP IV, FAP.alpha. and the like. These ~pro- inhibitors~ are activated, i.e., cleaved by an ~activated protease~ to release an active inhibitor moiety in proximity to a ~target protease~: The identity of activating protease and target protease can be the same (such pro- inhibitors being refered to as ~Target-Activated Smart Protease Inhibitors~ or ~TASPI~) or different (e.g., ~Target-Directed Smart Protease Inhibitors~ or ~TDSPI~). After activation of the pro-inhibitor, the active inhibitor moiety can self-inactive by, e.g., intramolecular-cyclization or cis-trans isomerization.

L'invention concerne des promédicaments d'inhibiteurs de protéases, tels que des inhibiteurs de protéosome, DPP IV, FAP.alpha. etc. Lesdits pro-inhibiteurs sont activés, par exemple, clivés par une protéase d'activation pour éliminer la fraction d'inhibiteurs actifs à proximité d'une protéase cible. L'identité des protéases d'activation et des protéases cibles peuvent être la même (telle que des pro-inhibiteurs faisant référence à des inhibiteurs de protéase smart activées sur la cible ou TASPI) ou différente (par exemple (des ibhibiteurs de protéases smart dirigées sur la cible ou TDSPI). Après l'activation dudit pro-inhibiteur, la fraction de l'inhibiteur actif peut elle-même se désactiver, par exemple, par cyclisation intramoléculaire ou ismérisation cis-trans.

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