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Aspartic Protease Inhibitors, Compositions, and Associated Therapeutic Methods

Posted Feb 27 2011 7:00pm

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.

Ramnarayan S Randad (NCI)
John W Erickson (NCI)
Michael A Eissenstat (NCI)
Lucyna Lubkowska (NCI)

Patent Status:
HHS, Reference No. E-210-1998/0
US, , Patent No. 6,613,764, Issued 02 Sep 2003
US, , Patent No. 7,132,420, Issued 07 Nov 2006
PCT, Application No. PCT/US00/00265 filed 06 Jan 2000

Infectious Diseases
Infectious Diseases - Therapeutics

For Licensing Information Please Contact:
Sally Hu Ph.D., M.B.A.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325 Room 21,
Rockville, MD 20852
United States
Phone: 301-435-5606
Fax: 301-402-0220

Ref No: 1221

Updated: 02/2011

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