[Federal Register Volume 65, Number 110 (Wednesday, June 7, 2000)]
[Notices]
[Pages 36150-36151]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 00-14343]


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DEPARTMENT OF HEALTH AND HUMAN SERVICES

National Institutes of Health


Government-Owned Inventions; Availability for Licensing

AGENCY: National Institutes of Health, Public Health Service, DHHS.

ACTION: Notice.

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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 Marlene Shinn, 
J.D., at the Office of Technology Transfer, National Institutes of 
Health, 6011 Executive Boulevard, Suite 325, Rockville, Maryland 20852-
3804; telephone: 301/496-7056 ext. 285; fax: 301/402-0220; e-mail: 
[email protected]. A signed Confidential Disclosure Agreement will be 
required to receive copies of the patent applications.

Direct C-14 Oxidation of Opioids

Andrew Coop, Kenner C. Rice (NIDDK)
DHHS Reference No. E-032-99/1 filed 04 May 2000

    Opioid agonist drugs including the 14-hydroxy derivatives are 
utilized in the treatment of pain. The 14-hydroxy substituted opioid 
antagonists have also been found to be useful in the treatment of 
opiate abuse, opiate overdose and alcohol addiction. In addition, there 
are certain derivatives which have been found to be useful in the 
prevention of tolerance to morphine and as immunosuppressants. The 14-
hydroxy agonist and antagonist drugs are produced by a multistep 
process from the starting material, thebaine, which is a minor 
constituent of opium and is generally in short supply. The demand for 
these products has resulted in a steadily increasing cost for thebaine 
and thebaine derivatives.
    The present technology consists of a new and practical, 
nonchromatographic method of preparing 14-hydroxycodeinone by the 
direct oxidation of codeinone with cobalt (III) acetate (easily 
prepared in situ). The technology gives a 51% unoptimized yield of 14-
hydroxycodeinone easily isolated by extractive workup and direct 
crystallization. This process is ultimately based on morphine (which is 
by far the major constituent and cheapest of the opium alkaloids) 
through the sequence: morphine to codeine to codeinone to 14-
hydroxycodeinone. This technology is not limited by the availability of 
thebaine and thus offers more efficient production of the 14-hydroxy 
derivatives from opium.

Use of Oligonucleotides To Target Nucleic Acid Sequences Encoding 
Apolipoprotein B To Decrease Serum Apolipoprotein B and Cholesterol 
Levels

Thomas L Eggerman (FDA), Amy Patterson, Paul F. Torrence (NIDDK), Julie 
K Rhie
DHHS Reference No. E-236-98/0 filed 12 Oct 1999

    Coronary heart disease is caused by the atherosclerotic narrowing 
of the coronary arteries affecting nearly 14 million persons in the 
United States. Approximately 480,000 deaths in 1995 were caused by the 
disease and it is the leading cause of death in the United States 
today. Two of the established causes of atheroscleorosis include 
elevated cholesterol levels and elevations of the major protein 
responsible for carrying cholesterol--apolipoprotein B (apoB). Optimal 
therapy, however is still not available for the most severely affected 
patients, in particular those with familial hypercholesterolemia and 
those with elevated apoB levels.

[[Page 36151]]

    The NIH announces a new gene therapy approach which will lower the 
risk for atheroscleoric heart disease by decreasing plasma cholesterol 
and apoB levels. Our researchers have shown that antisense DNA 
oligonucleotides targeted for apoB decreased apoB mRNA in a human liver 
cell line by up to 80%. This in turn has led to a new gene therapy 
which utilizes a vector designed to produce antisense mRNA targeted for 
apoB. The result is a decrease in liver apoB production, which is the 
major source of circulating apoB. These oligonucleotides and 
oligonucleotide analogs are a novel and useful way of reducing low 
density lipoprotein (LDL) in patients, as well as for research and 
diagnostic purposes.

T20/D178 and T21/D107 Are Activators of Human Phagocyte Formyl 
Peptide Receptors

Ji Ming Wang (NCI), Joost J Oppenheim (NCI), Shao-Bo Su, Wang-Hua Gong, 
Philip M. Murphy (NIAID), Ji-Liang Gao (NIAID)
DHHS Reference No. E-164-99/0 filed 05 May 1999

    The use of immunotherapy to treat inflammatory diseases is 
prescribed to thousands each and every year. In use currently are 
steroidal and non-steroidal anti-inflammatory drugs, which have serious 
side effects including: adrenal suppression, gastrointestinal 
disorders, increased susceptibility to infections, fluid retention and 
bone loss.
    The NIH announces a new technology which can be used in drug 
discovery dealing with the modulation of the immune response. This 
technology identifies two polypeptides, T20/DP178 and T21/DP107, which 
are peptide domains of the HIV-1 envelope protein and are potent 
chemoattractants and activators of human peripheral blood phagocytes 
(monocytes and neutrophils) but not T lymphocytes. These polypeptides 
have been determined to interact with the Formyl Peptide Receptors 
(FPR), which in turn up-regulates the immune response by inducing cell 
migration and calcium mobilization. The activation of FPR class 
receptors by their agonists also results in desensitization of cell 
responses to other chemotactic factors. By identifying analogs to T20/
DP178 and T21/DP107 and then evaluating their ability to bind to the 
FPR, one will be able to determine if the analog is a good candidate 
for either inhibiting or activating the immune response.

    Dated: May 30, 2000.
 Jack Spiegel,
Director, Division of Technology Development and Transfer, Office of 
Technology Transfer, National Institutes of Health.
[FR Doc. 00-14343 Filed 6-6-00; 8:45 am]
BILLING CODE 4140-01-P