National Institutes of Health, Public Health Service, DHHS.
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.
Licensing information and copies of the U.S. patent applications listed below may be obtained by contacting Dennis Penn, at the Office of Technology Transfer, National Institutes of Health, 6011 Executive Boulevard, Suite 325, Rockville, Maryland 20852-3804; telephone: 301/496-7056 ext. 211; fax: 301/402-0220; e-mail: email@example.com. A signed Confidential Disclosure Agreement will be required to receive copies of the patent applications.
Preparation and Use of Androgenic Compounds
Richard P. Blye and Hyun K. Kim (NICHD) DHHS Reference Nos. E-069-00/0 filed 31 Mar 2000 and E-069-00/1 filed 04 Apr 2000.
The technology describes the finding of the orally active androgenic compound, 7α, 11β-dimethyl-19-nortestosterone 17-bucyclate (Also known as CDB-4386A). This 17-bucyclate androgen compound is orally bioavailable and possesses greater potency than Methyltestosterone, the only oral androgen commercially available in this country. Too, this compound may be injected as an aqueous suspension, whereas other injectable androgens require an oil diluent. Androgens find use in the treatment of male hypogonadism regardless of the cause. Consequently they are used for the treatment of hypogonadotropic hypogonandism, as the androgenic component of male hormonal contraceptives and for androgen supplementation in hormone replacement therapy (HRT) in both men and women.
Process for Preparing 17-Alpha-Acetoxy-11-Beta-[4-(N,N-Dimethylamino)phenyl]-21-Methoxy-19-Norpregna-4,9-Diene-3,20-Dione, Intermediates Useful in the Process, and Processes for Preparing Such Intermediates
Hyun K. Kim (NICHD), and Pemmaraju Rao, James Cessac, and Anne Marie Simmons of the Southwest Foundation for Biomedical Research DHHS Reference No. E-013-00/0 filed 29 Dec 1999.
This invention relates to a process for preparing 17-alpha-acetoxy-11-beta-[4-(N,N-dimethylamino)phenyl]-21-methoxy-19-norpregna-4,9-diene-3,20-dione. This method substantially increases the yield over existing methods and will substantially reduce the cost of production of this compound. Other advantages include: (1) Use of smaller quantities of solvent and reagent; (2) use of intermediates, reagents, or byproducts which are relatively safe to handle and dispose of, no use of chromatography; (3) a purification procedure easier to practice on large scale from kilograms to multi-kilograms, including no use of chromatography if possible; and (4) in some cases, recycling the by-products was successfully achieved.
Novel Anti-thrombin Peptide From Mosquito Salivary Gland
Jesus G. Valenzuela, Jose M.C. Ribeiro, and Ivo Francischetti (NIAID) DHHS Reference No. E-143-99/0 filed 29 Jun 1999.
Currently, treatment and prophylaxis of thrombotic diseases involve therapeutic agents which act in one of two different ways. The first type inhibits a-thrombin activity or a-thrombin formation, thus preventing clot formation. The second category accelerates thrombolysis and dissolves the blood clot, thereby removing it from the blood vessel and unblocking the flow of blood. Heparin is an example of the first class and is widely used; however, heparin is less effective in treating patients with an anti-thrombin III deficiency. Hirudin is an example of the second class of anti-thrombotic drugs.
This invention relates to an anti-thrombin (Anophelin) isolated from the salivary glands of the mosquito Anopheles albimanus. The purified peptide inhibits thrombin induced platelet aggregation, thrombin esterolytic activity, and thrombin cleavage of fibrinogen. This peptide has no homologies to proteins of known function in GenBank, and is a novel, specific, and tight binding inhibitor of α-thrombin.
Ichthyosiform Skin Diseases
Peter M. Steinert, Nemes Zoltan and Lyuben Marckov (NIAMS) DHHS Reference No. E-149-99/0 filed 23 Jun 1999.
Many inherited autosomal recessive ichthyoses (ARI) are caused by improper or incomplete lipid barrier function in the skin due to genetic errors of either protein or lipid synthesis. It is previously known that the mutations in the transglutaminase 1 gene resulting in inactive enzyme is the cause of one ARI disease termed lamellar ichthyosis. This relates to the discovery that a principal function of the enzyme is to attach ceramide lipids for complete protein/lipid barrier function in the skin. This invention also describes how to: (1) Make large quantities of this enzyme that can be stored in a stable form which can be readied for use at short notice; (2) a simple way to make synthetic ceramide lipid analogs that function the same way as normal skin ceramides; and (3) make synthetic lipid vesicles that can carry, in a stable fashion, both the enzyme and synthetic ceramide so that it might be applied to affected ARI skin in order to provide ameliorative therapy. Start Printed Page 50207
High Sensitivity Phage Display Protein Detection Method
Carl R. Merril (NIMH) DHHS Reference No. E-185-98/0 filed 14 Apr 1999.
This new technology extends the range of protein detection appreciably under the absolute limit of 0.01ng for the Silver stain method. In an average protein molecule this amounts to 20 million molecules. The average cellular concentration of protein is 5000 molecules, so that an amplification system is needed to detect protein on that level. In this method, phage that display specific ligands or antibodies provide such an amplification system and therefore allow for detection. In addition, a particular phage expressing a known binding protein may be used to identify a specific protein and aid in the purification of that specific protein. The identification ability has both diagnostic and therapeutic potential.
The key novel feature of this technology in the market place would be its high sensitivity and the numerous benefits associated with it. It opens up whole new areas of analysis, such as on the cellular level, allowing for looking at protein variations within a single cell. Theoretically, as little as one protein molecule could be detectable.
The potential market for this invention would be in several distinct areas: Research—incorporation into kits to perform complete assays; Purification—aiding in the manufacturing process; Diagnostic—detection of variations of a specific protein within a cell; Therapeutic—identification of specific drug targets through the ability to bind to receptor sites.Start Signature
Dated: August 3, 2000.
Director, Division of Technology Development and Transfer, Office of Technology Transfer, National Institutes of Health.
[FR Doc. 00-20922 Filed 8-16-00; 8:45 am]
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