[Federal Register Volume 63, Number 201 (Monday, October 19, 1998)]
[Notices]
[Pages 55880-55882]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 98-27960]
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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. issued patents
and patent applications listed below may be obtained by contacting
Carol Salata, Ph.D., at the Office of Technology Transfer, National
Institutes of Health, 6011 Executive Boulevard, Suite 325, Rockville,
Maryland 20852-3804; telephone: 301/496-7057 ext. 232; fax: 301/402-
0220; e-mail: [email protected] A signed Confidential Disclosure
agreement will be required to receive copies of the patent
applications.
Dimeric Naphthylisoquinoline Alkaloids and Synthesis Methods
Thereof
G Bringmann, S Harmsen, MR Boyd (NCI)
Serial No. 08/279,339 filed 22 Jul 94 (U.S. Patent 5,571,919 issued 05
Nov 96) and Serial No. 08/674,359 filed 01 Jul 96 (U.S. Patent
5,789,594 issued 04 Aug 98)
This invention embodies the synthesis and novel compounds
comprising homodimeric and heterodimeric napthylisoquinoline
[[Page 55881]]
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. The compounds also
have antimalaria activity. Therefore, the dimeric alkaloids appear to
comprise a novel class of antiviral and antiparasitic drugs that may be
very useful by themselves or in combination with other treatments.
Dimeric Arylisoquinoline Alkaloids and Synthesis Methods Thereof
G Bringmann, MR Boyd, R Gotz, TR Kelly (NCI)
Serial No. 08/363,684 filed 23 Dec 94 (U.S. Patent 5,578,729 issued 26
Nov 96) and Serial No. 08/721,084 filed 24 Sep 96 (U.S. Patent
5,786,482 issued 28 Jul 98)
The present invention relates to novel compounds and 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 compounds also have antimalarial activity. 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 derivative thereof.
Monomeric Naphthylisoquinoline Alkaloids and Synthesis Methods
Thereof
G Bringmann, R Gotz, MR Boyd (NCI)
Serial No. 08/279,291 filed 22 Jul 94 (U.S. Patent 5,552,550 issued 03
Sep 96) and Serial No. 08/674,362 filed 01 Jul 96 (U.S. Patent
5,763,613 issued 09 Jun 98)
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.
Monomeric and Dimeric Arylisoquinoline Alkaloids and Derivatives
Thereof
G Bringmann, MR Boyd, M Wenzel (NCI)
Serial No. 09/001,801 filed 31 Dec 97
The present invention provides new monomeric derivatives of the C-
8'-7 linked naphthylisoquinoline alkaloid dioncophylline D. The
invention also provides new C-4 substituted monmeric arylisoquinoline
alkaloid derivatives. The present invention furthermore provides novel
dimeric arylisoquinoline alkaloids comprised of coupled first and
second arylisoquinoline monomers, wherein either or both of said
monomer(s) is (are) monomeric compound(s) of the present invention.
Monomeric and dimeric compounds of the present invention have
medically useful properties, such as antimicrobial properties, more
specifically antimalarial and antiviral properties. Monomeric compounds
of the present invention are also useful as building blocks or
intermediates for synthesis of novel dimeric arylisoquinoline
alkaloids.
Michellamine Antiviral Agents, Compositions, and Treatment Methods
MR Boyd, JH Cardellina, KP Manfredi, JW Blunt, LK Pannell, JB McMahon,
RJ Gulakowski, GM Cragg, G Bringmann, D Thomas, J Jato (NCI)
Serial No. 08/049,824 filed 19 Apr 93 (U.S. Patent 5,455,251 issued 03
Oct 95) and Serial No. 08/457,677 filed 01 Jun 95 (U.S. Patent
5,654,432 issued 05 Aug 97)
Michellamines, structurally novel naphthalene
tetrahydroisoquinoline alkaloids, are a new class of antiviral
compounds present in the plant Ancisrocladus 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 to 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 nonnucleoside 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. Licenses of this invention will be required to
comport with all applicable federal and country-of-collection policies
relating to biodiversity.
Antimalarial Korupensamines and Pharmaceutical Composition and
Medical Uses Thereof
MR Boyd, G Francois, G Bringmann, YF Hallock, KP Manfredi, JH
Cardellina (NCI)
Serial No. 08/195,260 filed 14 Feb 94 (U.S. Patent 5,409,938 issued 25
Apr 95)
The class of compounds known as korupensamines exhibit in vitro and
in viro 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 federally and country-of-collection policies relating to
biodiversity.
Antimalarial Napthylisoquinoline Alkaloids and Pharmaceutical
Compositions and Medicinal Uses Thereof
G Francois, G Bringmann, JD Phillipson, MR Boyd, LA Assi, G Dochez, C
Schneider, G Timperman (NCI)
Serial No. 08/195,547 filed 14 Feb 94 (U.S. Patent 5,639,761 issued 17
Jun 97) and Serial No. 08/843,582 filed 16 Apr 97
This is a new class of napthylisoquinoline alkaloid compounds,
present in plant species of the Ancistrocladaceae and Dionocophyllaceae
plant families which
[[Page 55882]]
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.
Dated: October 13, 1998.
Jack Speigel,
Director, Division of Technology Development and Transfer, Office of
Technology Transfer.
[FR Doc. 98-27960 Filed 10-16-98; 8:45 am]
BILLING CODE 4140-01-M
