Aspartic Protease Inhibitors, Compositions, and Associated Therapeutic Methods
Description of Invention:
The human immunodeficiency virus (HIV) is the causative agent of acquired immunodeficiency syndrome (AIDS). Drug-resistance is a critical factor contributing to the gradual loss of clinical benefit to treatments for HIV infection. Accordingly, combination therapies have further evolved to address the mutating resistance of HIV. However, there has been great concern regarding the apparent growing resistance of HIV strains to current therapies.
The subject invention provides compounds which may serve as therapeutic candidates for inhibition of HIV-1 PR (protease) and thus serve in controlling AIDS, as well as having anti-malarial properties. These compounds may be used in combination with other protease inhibitors or inhibitors of HIV-1 reverse transcriptase, especially in patients who have developed resistance to other HIV protease inhibitors. These inhibitors have high potency, lower molecular weight, and lower lipophilicity than previous compounds, as well as a better profile towards drug resistant mutant strains of HIV.
Inventors:
Ramnarayan S. Randad (NCI) John W. Erickson (NCI) Michael A. Eissenstat (NCI) Lucyna Lubkowska (NCI)
Patent Status:
DHHS Reference No. E-210-1988/0 --
U.S. Patent No. 6,613,764 issued 02 Sep 2003
U.S. Patent No. 7,132,420 issued 07 Nov 2006
For Additional Information Please Contact: Sally Hu PhD MBA
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: (301) 435-5606
Email: hus@mail.nih.gov
Fax: (301) 402-0220
