Aspartyl protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/395 (2006.01) A61P 9/00 (2006.01) A61P 25/00 (2006.01) A61P 25/28 (2006.01) A61P 31/18 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2610812

Disclosed are compounds of the formula (I) Chemical formula should be inserted here as it appears on the abstract in paper form or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, R, R1, R2, R3 and R4 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, un tautomère, ou un sel ou solvate pharmaceutiquement acceptable desdits composés. Dans ladite formule, U, W, R, R1, R2, R3 et R4 sont tels que définis dans la description. L'invention concerne également des compositions pharmaceutiques comprenant les composés représentés par la formule (I). L'invention concerne en outre la méthode d'inhibition de l'aspartyl protéase, et en particulier, les méthodes de traitement de maladies cardiovasculaires, de maladies cognitives et neurodégénératives. L'invention concerne enfin des méthodes de traitement de maladies cognitives ou neurodégénératives à l'aide des composés représentés par la formule (I) en combinaison avec un inhibiteur de cholinestérase ou un agoniste m1ou un antagoniste m2 muscarinique.

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