Aspartyl protease inhibitors
AssigneeSunesis Pharmaceuticals, Inc.
InventorWenjin Yang
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Abstract
The present invention provides compounds having the formula: 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 (β-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by β-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.
Claims29
An isolated compound having the structure:
- or pharmaceutically acceptable derivative thereof;
- wherein R1 is an aliphatic, heteroaliphatic, aromatic or heteroaromatic moiety, or R1, taken together with R′, may form a cycloheteroaliphatic moiety;
- R2 is an aliphatic, heteroaliphatic, aromatic or heteroaromatic moiety, or R2, taken together with R′, may form a cycloheteroaliphatic moiety;
- R4 is hydrogen, an aliphatic, heteroaliphatic, aromatic or heteroaromatic moiety, or R4, taken together with a substituent present on X2 or X3, may form a cycloaliphatic, cycloheteroaliphatic, aromatic, or heteroaromatic moiety;
- and
- RX2A is hydrogen or an aliphatic, heteroaliphatic, aryl, heteroaryl, -(alkyl)aryl, -(alkyl)heteroaryl, -(heteroalkyl)aryl, or -(heteroalkyl)heteroaryl moiety;
- wherein at least one of R1, R2, RX2A and R4 comprises a cycloheteroaliphatic or heteroaromatic moiety.
Dependencies are inferred from the claim text.