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HIV-1 Integrase Inhibitors for the Treatment of Retroviral Infections

Posted Jun 13 2010 5:00pm

Description of Invention:
This technology describes the structure and activity of N-benzyl derivatives of 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 2,3-dihydro-6,7-dihydroxy-1H-isoindole-1,3(2H)-diones as new HIV-1 integrase inhibitors. HIV, as well as other retroviruses, requires three key viral enzymes for replication: Reverse transcriptase, protease and integrase (IN). A significant number of patients fail to respond to combination therapies consisting of reverse transcriptase and protease inhibitors, due to the development of viral resistance. IN functions by initial processing of viral cDNA in a cleavage step termed 3’-processing (3’-P). This is followed by insertion of the cleaved cDNA into the host genome in a reaction known as “strand transfer” (ST). Certain agents covered under the subject technology have been shown to exhibit selective inhibition of ST reactions relative to 3’-P reactions. These compounds inhibit purified IN in vitro and are also active against HIV-1 derived vectors in cell-based assay. These inhibitors may have a potential therapeutic value for retroviral infections, including AIDS, especially for patients exhibiting drug resistant to current therapy regimes.

The treatment and prevention for HIV infections.

Development Status:
In vitro data available.

Terrence R Burke (NCI)
Xue Z Zhao (NCI)
Yves G Pommier (NCI)
Elena Semenova (NCI)

Relevant Publication:
  1. WG Verschueren et al. Design and optimization of tricyclic phtalimide analogue as novel inhibitors of HIV-1 integrase. J Med Chem. 2005 Mar 24;48(6):1930-1940. [ PubMed abs ]

Licensing Status:
Available for licensing.

Collaborative Research Opportunity:
The National Cancer Institute's Laboratory of Medicinal Chemistry and Laboratory of Molecular Pharmacology are seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize the HIV-1 integrase inhibitors described. Please contact John D. Hewes, Ph.D. at 301-435-3121 or for more information.

Infectious Diseases
Infectious Diseases - Therapeutics
In-vitro Data

For Additional Information Please Contact:
Admin. Licensing Spec-InfectDis
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-496-7057
Fax: 301-402-0220

Ref No: 1671

Updated: 06/2010

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