[Federal Register Volume 61, Number 76 (Thursday, April 18, 1996)]
[Notices]
[Pages 16926-16927]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 96-9527]



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DEPARTMENT OF HEALTH AND HUMAN SERVICES

Government-Owned Inventions; Availability for Licensing

AGENCY:  National Institutes of Health.

ACTION: Notice.

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    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 U.S. 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 writing to the indicated 
licensing contact at the Office of Technology Transfer, National 
Institutes of Health, 6011 Executive Boulevard, Suite 325, Rockville, 
Maryland 20852-3804 (telephone 301/496-7057; fax 301/402-0220). A 
signed Confidential Disclosure Agreement (CDA) will be required to 
receive copies of the patent applications.

Dimeric Arylisoquinoline Alkaloids and Synthesis Methods Thereof

Bringmann, G., Boyd, M.R., Gotz, R., Kelly, T.R. (NCI)
Filed 23 Dec 94
Serial No. 08/363,684
Licensing Contact: Gloria Richmond, 301/496-7056 ext 268

    The present invention relates to a new method of chemical synthesis 
of known and new dimeric arylisoquinoline alkaloids. These compounds 
are members of a general class known as naphthylisoquinoline alkaloids. 
These dimeric alkaloids have been found to be effective inhibitors of 
HIV replication in human immune cells. The method of this invention 
provides access not only to known but also heretofore unknown medically 
useful compounds. The invention also provides for new dimeric 
arylisoquinoline compounds and derivatives thereof. (portfolio: 
Infectious Diseases--Therapeutics, antivirals, AIDS)

Dimeric Naphthylisoquinoline Alkaloids and Synthesis Methods Thereof

Bringmann, G., Harmsen, S., Boyd, M.R. (NCI)
Filed 22 July 94
Serial No. 08/279,339
Licensing Contact: Gloria Richmond, 301/496-7056 ext 268

    This invention embodies the synthesis of homodimeric and 
heterodimeric naphthylisoquinoline alkaloids and derivatives. The 
methods presented in the invention are advantageous because they 
permit, for the first time, the in vitro synthesis of compounds for 
which the only known natural source is the rare tropical vine, 
Ancistrocladus korupensis of Central Africa. This class of compounds 
has been demonstrated to be effective in inhibiting the ability of HIV 
to replicate and infect cells. Therefore, the dimeric alkaloids appear 
to comprise a novel class of antiviral drugs that may be very useful by 
themselves or in combination with other treatments. (portfolio: 
Infectious Diseases--Therapeutics, antivirals, AIDS)

[[Page 16927]]

Monomeric Naphthylisoquinoline Alkaloids and Synthesis Methods Thereof

Bringmann, G., Gotz, R., Boyd, M.R. (NCI)
Filed 22 Jul 94
Serial No. 08/279,291
Licensing Contact: Gloria Richmond, 301/496-7056 ext 268

    Monomeric naphthylisoquinoline alkaloids and their derivatives are 
medically useful for the treatment of parasitic infections including 
malaria. However, these particular alkaloids are available in a limited 
supply since they are obtained from scarce plants which have a limited 
geographic distribution. This invention embodies methods for the 
preparation of monomeric naphthylisoquinoline alkaloids, including the 
antiparasitic korupensamines and related compounds, as well as non-
korupensamines. New, medically useful, naphthylisoquinoline compounds 
and derivatives are also described. (portfolio: Infectious Diseases--
Therapeutics, anti-parasitic)

Antimalarial Naphthylisoquinoline Alkaloids and Pharmaceutical 
Compositions and Medicinal Uses Thereof

Francois, G., Bringmann, G., Phillipson, J.D., Boyd, M.R., Assi, L.A., 
Dochez, G., Schneider, C., Timperman, G. (NCI)
Filed 14 Feb 94
Serial No. 08/195,547
Licensing Contact: Gloria Richmond, 301/496-7056 ext 268

    This is a new class of napthylisoquinoline alkaloid compounds, 
present in plant species of the Ancistrocladaceae and Dioncophyllaceae 
plant families which are found in tropical Africa and southern and 
southeast Asia, that exhibit effective antimalarial properties and 
offer important new weapons in the treatment of this devastating 
disease. The deadliest malarial parasites have become resistant to 
previously effective antimalarial drugs; therefore, effective new 
antimalarial drugs are urgently needed. These new naphthylisoquinoline 
compounds effectively inhibit the growth, reproduction, and pathologic 
effects of a broad spectrum of Plasmodia parasites, including drug-
resistant strains. Licensees of this invention will be required to 
comport with all applicable federal and country-of-collection policies 
relating to biodiversity. (portfolio: Infectious Diseases--
Therapeutics, anti-parasitic)

Antimalarial Korupensamines and Pharmaceutical Compositions and Medical 
Uses Thereof

Boyd, M.R., Francois, G., Bringmann, G., Hallock, Y.F., Manfredi, K.P., 
Cardellina, J.H. (NCI)
Serial No. 08/195,260
U.S. Patent No. 5,409,938 issued 25 Apr 95
Licensing Contact: Steve Ferguson, 301/496-7735 ext 266

    The class of compounds known as korupensamines exhibit in vitro and 
in vivo antimalarial activity and offer a potent new means for treating 
and controlling this devastating disease. As many as 2-3 million people 
worldwide die from malaria each year, and many more suffer from long-
term chronic infection. The deadliest malarial parasites have become 
resistant to previously effective antimalarial drugs such as 
chloroquine and other clinically useful agents; therefore, effective 
new antimalarial drugs are urgently needed. These korupensamine 
compounds, which are isolated from a new species of the plant genus 
Ancistrocladus which is found in tropical Africa and southern and 
southeast Asia, effectively inhibit the growth, reproduction, and 
pathologic effects of a broad spectrum of Plasmodia parasites when 
given alone or in conjunction with previously available antimalarial 
agents. Licensees of this invention will be required to comport with 
all applicable federal and country-of-collection policies relating to 
biodiversity. (portfolio: Infectious Diseases--Therapeutics, anti-
parasitic)

Michellamine Antiviral Agents, Compositions, and Treatment Methods

Boyd, M.R., Cardellina, J.H., Manfredi, K.P., Blunt, J.W., Pannell, 
L.K., McMahon, J.B., Gulakowski, R.J., Cragg, G.M., Bringmann, G., 
Thomas, D., Jato, J. (NCI)
U.S. Patent 5,455,251 issued 3 Oct 95
Serial No. 08/049,824 (CIP of 07/684,197 with a priority date of 12 Apr 
91)
Licensing Contact: Gloria H. Richmond, 301/496-7056 ext 268

    Michellamines, structurally novel naphthalene 
tetrahydroisoquinoline alkaloids, are a new class of antiviral 
compounds present in the plant Ancistrocladus korupensis. The 
Ancitrocladaceae is a small paleotropical family, with 20 species known 
from Asia and tropical Africa. A. korupensis contains three distinct 
michellamines, A, B, and C. Michellamine B, the most prevalent and 
potent of the three, is capable of inhibiting two distinct stages of 
the HIV life cycle. The compound is able to inhibit HIV-induced cell 
killing of infected cells but has no effect on HIV virons or initial 
binding of HIV to target cells. In addition, michellamine B inhibits 
the enzymatic activity of both the normal HIV reverse transcriptase and 
the activity of several mutant transcriptases which are resistant to 
several nonucleoside inhibitors. The claims of this invention relate to 
michellamine compounds and derivatives, methods for the isolation of 
the michellamines from A. korupensis, and methods for the 
administration of these antiviral compounds for treating patients 
infected with HIV. Licensees of this invention will be required to 
comport with all applicable federal and country-of-collection policies 
relating to biodiversity. (portfolio: Infectious Diseases--
Therapeutics, anti-virals, AIDS)

    Dated: April 9, 1996.
Barbara M. McGarey,
Deputy Director, Office of Technology Transfer.
[FR Doc. 96-9527 Filed 4-17-96; 8:45 am]
BILLING CODE 4140-01-M