[Federal Register: April 18, 1996 (Volume 61, Number 76, 
<BR>[Page 16926-16927]
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<BR>DEPARTMENT OF HEALTH AND HUMAN SERVICES
<BR> 
<BR>Government-Owned Inventions; Availability for Licensing
<BR>
<BR>AGENCY:  National Institutes of Health.
<BR>
<BR>ACTION: Notice.
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<BR>
<BR>    The inventions listed below are owned by agencies of the U.S. 
<BR>Government and are available for licensing in the U.S. in accordance 
<BR>with 35 U.S.C. 207 to achieve expeditious commercialization of results 
<BR>of federally-funded research and development. Foreign patent 
<BR>applications are filed on selected inventions to extend market coverage 
<BR>for U.S. companies and may also be available for licensing.
<BR>
<BR>ADDRESSES: Licensing information and copies of the U.S. patent 
<BR>applications listed below may be obtained by writing to the indicated 
<BR>licensing contact at the Office of Technology Transfer, National 
<BR>Institutes of Health, 6011 Executive Boulevard, Suite 325, Rockville, 
<BR>Maryland 20852-3804 (telephone 301/496-7057; fax 301/402-0220). A 
<BR>signed Confidential Disclosure Agreement (CDA) will be required to 
<BR>receive copies of the patent applications.
<BR>
<BR>Dimeric Arylisoquinoline Alkaloids and Synthesis Methods Thereof
<BR>
<BR>Bringmann, G., Boyd, M.R., Gotz, R., Kelly, T.R. (NCI)
<BR>Filed 23 Dec 94
<BR>Serial No. 08/363,684
<BR>Licensing Contact: Gloria Richmond, 301/496-7056 ext 268
<BR>
<BR>    The present invention relates to a new method of chemical synthesis 
<BR>of known and new dimeric arylisoquinoline alkaloids. These compounds 
<BR>are members of a general class known as naphthylisoquinoline alkaloids. 
<BR>These dimeric alkaloids have been found to be effective inhibitors of 
<BR>HIV replication in human immune cells. The method of this invention 
<BR>provides access not only to known but also heretofore unknown medically 
<BR>useful compounds. The invention also provides for new dimeric 
<BR>arylisoquinoline compounds and derivatives thereof. (portfolio: 
<BR>Infectious Diseases--Therapeutics, antivirals, AIDS)
<BR>
<BR>Dimeric Naphthylisoquinoline Alkaloids and Synthesis Methods Thereof
<BR>
<BR>Bringmann, G., Harmsen, S., Boyd, M.R. (NCI)
<BR>Filed 22 July 94
<BR>Serial No. 08/279,339
<BR>Licensing Contact: Gloria Richmond, 301/496-7056 ext 268
<BR>
<BR>    This invention embodies the synthesis of homodimeric and 
<BR>heterodimeric naphthylisoquinoline alkaloids and derivatives. The 
<BR>methods presented in the invention are advantageous because they 
<BR>permit, for the first time, the in vitro synthesis of compounds for 
<BR>which the only known natural source is the rare tropical vine, 
<BR>Ancistrocladus korupensis of Central Africa. This class of compounds 
<BR>has been demonstrated to be effective in inhibiting the ability of HIV 
<BR>to replicate and infect cells. Therefore, the dimeric alkaloids appear 
<BR>to comprise a novel class of antiviral drugs that may be very useful by 
<BR>themselves or in combination with other treatments. (portfolio: 
<BR>Infectious Diseases--Therapeutics, antivirals, AIDS)
<BR>
<BR>[[Page 16927]]
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<BR>Monomeric Naphthylisoquinoline Alkaloids and Synthesis Methods Thereof
<BR>
<BR>Bringmann, G., Gotz, R., Boyd, M.R. (NCI)
<BR>Filed 22 Jul 94
<BR>Serial No. 08/279,291
<BR>Licensing Contact: Gloria Richmond, 301/496-7056 ext 268
<BR>
<BR>    Monomeric naphthylisoquinoline alkaloids and their derivatives are 
<BR>medically useful for the treatment of parasitic infections including 
<BR>malaria. However, these particular alkaloids are available in a limited 
<BR>supply since they are obtained from scarce plants which have a limited 
<BR>geographic distribution. This invention embodies methods for the 
<BR>preparation of monomeric naphthylisoquinoline alkaloids, including the 
<BR>antiparasitic korupensamines and related compounds, as well as non-
<BR>korupensamines. New, medically useful, naphthylisoquinoline compounds 
<BR>and derivatives are also described. (portfolio: Infectious Diseases--
<BR>Therapeutics, anti-parasitic)
<BR>
<BR>Antimalarial Naphthylisoquinoline Alkaloids and Pharmaceutical 
<BR>Compositions and Medicinal Uses Thereof
<BR>
<BR>Francois, G., Bringmann, G., Phillipson, J.D., Boyd, M.R., Assi, L.A., 
<BR>Dochez, G., Schneider, C., Timperman, G. (NCI)
<BR>Filed 14 Feb 94
<BR>Serial No. 08/195,547
<BR>Licensing Contact: Gloria Richmond, 301/496-7056 ext 268
<BR>
<BR>    This is a new class of napthylisoquinoline alkaloid compounds, 
<BR>present in plant species of the Ancistrocladaceae and Dioncophyllaceae 
<BR>plant families which are found in tropical Africa and southern and 
<BR>southeast Asia, that exhibit effective antimalarial properties and 
<BR>offer important new weapons in the treatment of this devastating 
<BR>disease. The deadliest malarial parasites have become resistant to 
<BR>previously effective antimalarial drugs; therefore, effective new 
<BR>antimalarial drugs are urgently needed. These new naphthylisoquinoline 
<BR>compounds effectively inhibit the growth, reproduction, and pathologic 
<BR>effects of a broad spectrum of Plasmodia parasites, including drug-
<BR>resistant strains. Licensees of this invention will be required to 
<BR>comport with all applicable federal and country-of-collection policies 
<BR>relating to biodiversity. (portfolio: Infectious Diseases--
<BR>Therapeutics, anti-parasitic)
<BR>
<BR>Antimalarial Korupensamines and Pharmaceutical Compositions and Medical 
<BR>Uses Thereof
<BR>
<BR>Boyd, M.R., Francois, G., Bringmann, G., Hallock, Y.F., Manfredi, K.P., 
<BR>Cardellina, J.H. (NCI)
<BR>Serial No. 08/195,260
<BR>U.S. Patent No. 5,409,938 issued 25 Apr 95
<BR>Licensing Contact: Steve Ferguson, 301/496-7735 ext 266
<BR>
<BR>    The class of compounds known as korupensamines exhibit in vitro and 
<BR>in vivo antimalarial activity and offer a potent new means for treating 
<BR>and controlling this devastating disease. As many as 2-3 million people 
<BR>worldwide die from malaria each year, and many more suffer from long-
<BR>term chronic infection. The deadliest malarial parasites have become 
<BR>resistant to previously effective antimalarial drugs such as 
<BR>chloroquine and other clinically useful agents; therefore, effective 
<BR>new antimalarial drugs are urgently needed. These korupensamine 
<BR>compounds, which are isolated from a new species of the plant genus 
<BR>Ancistrocladus which is found in tropical Africa and southern and 
<BR>southeast Asia, effectively inhibit the growth, reproduction, and 
<BR>pathologic effects of a broad spectrum of Plasmodia parasites when 
<BR>given alone or in conjunction with previously available antimalarial 
<BR>agents. Licensees of this invention will be required to comport with 
<BR>all applicable federal and country-of-collection policies relating to 
<BR>biodiversity. (portfolio: Infectious Diseases--Therapeutics, anti-
<BR>parasitic)
<BR>
<BR>Michellamine Antiviral Agents, Compositions, and Treatment Methods
<BR>
<BR>Boyd, M.R., Cardellina, J.H., Manfredi, K.P., Blunt, J.W., Pannell, 
<BR>L.K., McMahon, J.B., Gulakowski, R.J., Cragg, G.M., Bringmann, G., 
<BR>Thomas, D., Jato, J. (NCI)
<BR>U.S. Patent 5,455,251 issued 3 Oct 95
<BR>Serial No. 08/049,824 (CIP of 07/684,197 with a priority date of 12 Apr 
<BR>91)
<BR>Licensing Contact: Gloria H. Richmond, 301/496-7056 ext 268
<BR>
<BR>    Michellamines, structurally novel naphthalene 
<BR>tetrahydroisoquinoline alkaloids, are a new class of antiviral 
<BR>compounds present in the plant Ancistrocladus korupensis. The 
<BR>Ancitrocladaceae is a small paleotropical family, with 20 species known 
<BR>from Asia and tropical Africa. A. korupensis contains three distinct 
<BR>michellamines, A, B, and C. Michellamine B, the most prevalent and 
<BR>potent of the three, is capable of inhibiting two distinct stages of 
<BR>the HIV life cycle. The compound is able to inhibit HIV-induced cell 
<BR>killing of infected cells but has no effect on HIV virons or initial 
<BR>binding of HIV to target cells. In addition, michellamine B inhibits 
<BR>the enzymatic activity of both the normal HIV reverse transcriptase and 
<BR>the activity of several mutant transcriptases which are resistant to 
<BR>several nonucleoside inhibitors. The claims of this invention relate to 
<BR>michellamine compounds and derivatives, methods for the isolation of 
<BR>the michellamines from A. korupensis, and methods for the 
<BR>administration of these antiviral compounds for treating patients 
<BR>infected with HIV. Licensees of this invention will be required to 
<BR>comport with all applicable federal and country-of-collection policies 
<BR>relating to biodiversity. (portfolio: Infectious Diseases--
<BR>Therapeutics, anti-virals, AIDS)
<BR>
<BR>    Dated: April 9, 1996.
<BR>Barbara M. McGarey,
<BR>Deputy Director, Office of Technology Transfer.
<BR>[FR Doc. 96-9527 Filed 4-17-96; 8:45 am]
<BR>BILLING CODE 4140-01-M
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