Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof

US6642237B1 · kind B1 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• James R. Tata · Westfield, US
• Kevin T. Chapman · Emeryville, US
• Joseph L. Duffy · Cranford, US
• Nancy J. Kevin · East Brunswick Township, US
• Yuan Cheng · Newbury Park, US
• Thomas A. Rano · Somerville, US
• Fengqi Zhang · Edison, US
• Tracy Huening · Madison, US
• Brian Anthony Kirk · Berkeley Heights, US
• Zhijian Lu · Clinton, US
• Subharekha Raghavan · Teaneck, US
• Fred J. Fleitz · Willingboro, US
• Daniel Petrillo · Perth, AU
• Joseph D. Armstrong, III · Westfield, US
• Richard J. Varsolona · Scotch Plains, US
• David Askin · Hackettstown, US
• R. Scott Hoerrner · Westfield, US
• Robert Purick · Edison, US

Key dates

• Filing date: Nov 21, 2000
• Grant date: Nov 4, 2003
• Expiry date: Nov 21, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.