The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.
[EN] NOVEL DRUGS FOR DEMENTIA<br/>[FR] NOUVEAUX MEDICAMENTS CONTRE LA DEMENCE
申请人:TERNANSKY ROBERT
公开号:WO2007038772A1
公开(公告)日:2007-04-05
[EN] The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety. [FR] L'invention concerne des composés qui sont des promédicaments contenant un fragment de système de délivrance chimique ("chemical delivery system" ou CDS) et un fragment d'inhibiteur de cystéine protéase. Le fragment CDS cible le promédicament sur le cerveau ou le système nerveux central. L'inhibiteur de cystéine protéase inhibe les cystéine protéases lors de la libération du promédicament. Les inhibiteurs de cystéine protéase sont efficaces dans le traitement de la démence, de la maladie d'Alhzheimer et de la démence vasculaire. Le ciblage du cerveau ou du système nerveux central offre des avantages significatifs dans le traitement de ces états et maladies. Un médicament CDS préféré est composé d'un fragment CDS de dihydrotrigoneline couplé à un fragment d'inhibiteur de cystéine protéase de peptide d'époxysuccinile.