Aspartyl protease inhibitors

Details Aspartyl protease inhibitors Aspartyl protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 239/70 (2006.01) C07D 471/10 (2006.01) C07D 487/10 (2006.01) C07D 491/10 (2006.01) C07D 495/10 (2006.01)

Patent

CA 2610815

Disclosed are compounds of the formula I here or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a and R7, are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

L'invention concerne des composés représentés par la formule (I), ou un stéréoisomère, ou un tautomère, ou un sel ou un solvate de ceux-ci pharmaceutiquement acceptable, dans laquelle U, W, A, R, R1, R2, R6a et R7 sont tels que définis dans la spécification; et des compositions pharmaceutiques comprenant les composés représentés par la formule (I). L'invention concerne également une méthode permettant d'inhiber l'aspartyl protéase et, en particulier, des méthodes permettant de traiter les maladies cardio-vasculaires, cognitives et neurodégénératives. L'invention concerne enfin des méthodes permettant de traiter les maladies cognitives ou neurodégénératives à l'aide des composés représentés par la formule (I) combinés à un inhibiteur de la cholinestérase ou un agoniste muscarinique m1 ou un antagoniste muscarinique m2.

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