01-8374. Government-Owned Inventions; Availability for Licensing

AGENCY:

National Institutes of Heath, Public Health Service, DHHS.

ACTION:

Notice.

SUMMARY:

The inventions listed below are owned by agencies of the U.S. Government and are available for licensing in the U.S. in accordance with 35 U.S.C. 207 to achieve expeditious commercialization of results of federally-funded research and development. Foreign patent applications are filed on selected inventions to extend market coverage for companies and may also be available for licensing.

ADDRESSES:

Licensing information and copies of the U.S. patent applications listed below may be obtained by contacting Sally Hu, Ph.D., Technology Licensing Specialist, Office of Technology Transfer, National Institutes of Health, 6011 Executive Boulevard, Suite 325, Rockville, Maryland 20852-3804; telephone: [phone] ext. 265; fax: [phone]; e-mail: [e-mail]. A signed Confidential Disclosure Agreement will be required to receive copies of the patent applications.

A Method of Inhibiting Viral Replication Targeting the Nucleocapsid Protein

Robert H. Shoemaker, Robert J. Fisher, and Judy A. Mikovits (NCI) DHHS Reference No. E-276-00/0 filed 05 Feb 2001

This invention concerns novel compounds that inhibit replication of retroviruses, such as HIV. These compounds act in a mechanistically distinct way from any other anti-HIV compound and appear to be relatively non-toxic. The compounds exert anti-HIV activity through inhibition of a key step in the viral replication cycle, specifically, the interaction of the nucleocapsid with nucleic acid. Clinical experience in chemotherapy of patients with AIDS has clearly shown that use of combinations of drugs acting through different mechanisms is essential for control of virus replication. Consequently, these compounds are believed to have the potential to substantially enhance anti-HIV therapy by introduction of agents acting by this novel mechanism.

Method of Preparing a Production Intermediate for HIV Protease Inhibitors

Guangyang Wang, Michael A. Eissenstat, and Tatiana Guerassina (NCI) DHHS Reference No. E-188-00/0 filed 24 Jan 2000

The invention describes a novel process amenable for the large-scale practical synthesis of cis-tetrahydro-furo[2,3-b]furan-3-one. This compound is useful as a key intermediate for the synthesis of highly potent and resistance-repellent HIV protease inhibitors that share a common component called bis-tetrahydrofuran (bis-THF). Specifically, the invention provides a method of preparing these precursors by modification of reaction temperatures, conditions and reagents leading to increased yields and purity of the desired intermediates. Such modifications would be useful in the large-scale preparation of highly potent and resistance-repellent HIV protease inhibitors currently under development as antiviral agents useful in treating AIDS.

Dated: March 29, 2001.

Jack Spiegel,

Director, Division of Technology Development and Transfer, Office of Technology Transfer, National Institutes of Health.