Heterocyclic aspartyl protease inhibitors

Details Heterocyclic aspartyl protease inhibitors Heterocyclic aspartyl protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 409/04 (2006.01) A61K 31/395 (2006.01) A61P 9/00 (2006.01) A61P 25/28 (2006.01) A61P 31/18 (2006.01) A61P 33/02 (2006.01) C07D 487/04 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2626976

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 Ar, R1, R2, R3, R4 and R5 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.

La présente invention a trait à des composés de formule I, dans laquelle: Ar, R1, R2, R3, R4 et R5 sont tels que définis dans la description, ou un stéréoisomère, tautomère, ou un sel ou solvate pharmaceutiquement acceptable de ceux-ci; et à des compositions pharmaceutiques comportant les composés de formule I. L'invention a également trait à un procédé d'inhibition d'aspartyle protéase, et en particulier, à des procédés pour le traitement de maladies cardio-vasculaires, de maladies cognitives et neurodégénératives. L'invention a trait en outre à des procédés de traitement de maladies cognitives ou neurodégénératives mettant en oeuvre les composés de formule I en combinaison avec un inhibiteur de la cholinestérase ou un agoniste du récepteur muscarinique de type M1 ou antagoniste du récepteur muscarinique de type M2.

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