Aspartyl protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 413/04 (2006.01) A61K 31/553 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2628264

Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein (W, R1, R2, R3, R4, R5, R6, 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, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin (D) and protozoal enzymes. 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 antagonist.

L~invention concerne des composés de formule (I) ou stéréoisomère, tautomère, sel ou solvate pharmaceutiquement acceptable de ces composés. Dans ladite formule, W, R1, R2, R3, R4, R5, R6 et R7 sont tels que définis dans la description. L~invention concerne également des compositions pharmaceutiques comprenant les composés de formule (I). L~invention concerne en outre un procédé d~inhibition de l~aspartyle protéase et, en particulier, des procédés de traitement de maladies cardiovasculaires, de maladies cognitives et neurodégénératives et des procédés d~inhibition du virus d~immunodéficience humain, de plasmépsines, de la cathépsine D et d~enzymes protozoaires. Sont également concernés des procédés de traitement de maladies cognitives ou neurodégénératives au moyen des composés de formule (I) combinés à un inhibiteur de la cholinestérase ou un antagoniste muscarinique.

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