Aspartyl protease inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 237/22 (2006.01) A61K 31/166 (2006.01) A61P 25/28 (2006.01) C07C 237/12 (2006.01) C07C 237/14 (2006.01) C07C 311/08 (2006.01) C07C 311/16 (2006.01) C07D 211/04 (2006.01) C07D 213/04 (2006.01) C07D 241/08 (2006.01) C07D 249/08 (2006.01) C07D 275/02 (2006.01) C07D 285/06 (2006.01) C07D 307/02 (2006.01) C07D 333/02 (2006.01) C07K 5/02 (2006.01)

Patent

CA 2529739

The present invention provides compounds having the formula: (I) wherein R1, R', R2, R3, R3~, R4, X1, X2 and X3 are as defined herein, and pharmaceutical compositions thereof. The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. In certain embodiments, compounds inhibit BACE (.beta.-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by .beta.-amyloid deposits in the brain (including, but not limited to, Alzheimer's Disease). The present invention also provides methods for preparing compounds of the invention.

L'invention se rapporte à des composés représentés par la formule (I) dans laquelle R?1¿, R', R?2¿, R?3¿, R?3'¿, R?4¿, X?1¿, X?2¿ et X?3¿ sont tels que définis ci-après, et à des compositions pharmaceutiques associées. L'invention concerne aussi des procédés d'inhibition des protéases, notamment des aspartyl-protéases. Dans certains modes de réalisation, des composés inhibent BACE (enzyme de clivage APP du site .szlig.), et sont par conséquent utiles dans le traitement ou la prévention d'une maladie caractérisée par des dépôts de .szlig.-amyloïde dans le cerveau (y compris, entre autres, la maladie d'Alzheimer). Cette invention porte aussi sur des procédés de préparation de ces composés.

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