Aspartyl protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 239/95 (2006.01) A61K 31/519 (2006.01) A61P 25/00 (2006.01) C07D 471/14 (2006.01)

Patent

CA 2672293

Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. 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 (la formule chimique doit être insérée ici comme elle apparaît dans l'abrégé sous forme papier) Formule I ou un stéréoisomère, un tautomère, ou un sel ou un solvate pharmaceutiquement acceptable de ceux-ci, dans laquelle R1, R2, R3, R4, R14, V, W, X, Y, Z, p, et le cycle A sont tels que décrits dans la description. L'invention concerne également un procédé destiné à inhiber la protéase d'aspartyle et, en particulier, les procédés destinés à traiter des maladies cardio-vasculaires et des maladies cognitives et neurodégénératives. L'invention concerne également des procédés destinés à traiter des maladies cognitives ou neurodégénératives utilisant les composés représentés par la formule I en combinaison avec un inhibiteur de la cholinestérase, un agoniste muscarinique m1 ou un antagoniste m2.

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