Methods for treating neurodegenerative disorders using aspartyl protease inhibitors

US7119105B2 · kind B2 · utility

Assignee

• The Regents of the University of California · US

Inventors

• Jonathan A. Ellman · Guilford, US
• Gary Lynch · Irvine, US
• Irwin D. Kuntz · Greenbrae, US
• Xiaoning Bi · Irvine, US
• Christina E. Lee · Berkeley, US
• A. Geoffrey Skillman · San Francisco, US
• Tasir Haque · Wilmington, US

Key dates

• Filing date: Feb 5, 2004
• Grant date: Oct 10, 2006
• Expiry date: Feb 5, 2024

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to () non-peptide aspartyl protease inhibitors; (ii) methods for modulating the processing of an amyloid precursor protein (APP); (iii) methods for modulating the processing of a tau protein (τ-protein); and (iv) methods for treating neurodegenerative diseases. For instance, in one embodiment, the present invention provides a method for modulating the processing of an amyloid precursor protein (APP), the method comprising contacting a composition containing the APP with an aspartyl protease inhibitor having the formula:wherein:R1, R2 and R3 are members independently selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl, substituted aryloxyalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, heterocycles, substituted heterocycles, heterocyclicalkyl and substituted heterocyclicalkyl; and R5 and R6 are independently selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl and substituted aryloxyalkyl; or R5 and R6 and the carbons to which they a…