Aspartic protease inhibitors

US7132420B2 · kind B2 · utility

Assignee

• The United States of America, as represented by the Department of Health and Human Services · US

Inventors

• Ramnarayan Randad · Frederick, US
• John W. Erickson · Barrington, US
• Michael Eissenstat · Frederick, US
• Lucyna Lubkowska · Frederick, US

Key dates

• Filing date: Jun 11, 2003
• Grant date: Nov 7, 2006
• Expiry date: Mar 30, 2024

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention provides an aspartic proteinase-inhibiting compound of the formula:wherein a, b, c, d, and e, can be the same or different and each are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen, wherein R7 and R8 are independently H or an alkyl. Substituents R1 or R2 are each H or an alkyl. Substituent R3 is a straight chain or branched alkyl, alkenyl, or alkynyl substituent, or is a cycloalkyl. Substituent A is OH, NH2, or SH.Further provided are pharmaceutical compositions, which include a therapeutically effective amount of at least one of the foregoing compounds, and therapeutic methods of using the foregoing compounds.