Government-Owned Inventions; Availability for Licensing, 58858-58860 [E7-20513]
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58858
Federal Register / Vol. 72, No. 200 / Wednesday, October 17, 2007 / Notices
sroberts on PROD1PC70 with NOTICES
adult loses thirty percent of his muscle
mass between the ages of 20 and 70.
Development Status: Early stage.
Inventors: Jay H. Chung et al.
(NHLBI).
Publication: In preparation.
Patent Status: U.S. Provisional
Application No. 60/958,714 filed 06 July
2007 (HHS Reference No. E–068–2007/
0-US–01).
Licensing Status: This technology is
available for exclusive, co-exclusive, or
nonexclusive licensing.
Licensing Contact: Tara L. Kirby,
Ph.D.; 301/435–4426;
tarak@mail.nih.gov.
Collaborative Research Opportunity:
The National Heart Lung and Blood
Institute, Laboratory of Biochemical
Genetics, is seeking statements of
capability or interest from parties
interested in collaborative research to
further develop, evaluate, or
commercialize DNA-PKcs inhibitors for
treatment or prevention of metabolic
and degenerative diseases. Please
contact Jay Chung
(chungj@nhlbi.nih.gov) for more
information.
Predictive Diagnostic Test for AntiDepressant Related Suicide Risk
Description of Technology: A number
of studies have reported a potential link
between antidepressant treatment and
suicides. Although the scientific basis
for this phenomenon is not known, the
Food and Drug Administration (FDA)
required a black box warning of
worsening depression and/or emergence
of suicidality (i.e., development of
suicidal thoughts or behavior) in both
adult and pediatric patients taking
several antidepressants. While use of
antidepressants fell subsequent to the
black box warning, recent studies
suggest that pediatric suicides may
actually be rising. This has led to
concerns that untreated depression due
to the black box warning could
potentially result in an overall increase
in suicides.
To determine whether a genetic basis
for suicidal risk exists for a sub-group of
depressed patients, NIH researchers
genetically screened patients with major
depression treated with the serotonin
selective reuptake inhibitor (SSRI)
citalopram (Celexa) in the NIMH-funded
Sequenced Treatment Alternatives for
Depression (STAR*D) trial. Versions of
two genes coding for components of the
brain’s glutamate chemical messenger
system were linked to suicidal thinking
associated with antidepressant use.
Having both implicated versions
increased risk of such thoughts more
than 14-fold. By identifying those
patients who need close monitoring,
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alternative treatments and/or specialty
care, these genetic tests should prevent
the under prescribing of anti-depressant
drugs and the resulting possibility of
suicide due to sub-optimal treatment.
Applications: Diagnostic tests
predicting the likelihood of suicide
during anti-depressant treatment.
Market: Depression ranks among the
ten leading causes of disability and will
become the second-largest cause of the
global health burden by 2020. An
estimated 121 million people
worldwide suffer from a depressive
disorder for which they require
treatment. It is estimated that 5.8% of
all men and 9.5% of all women will
suffer from a depressive disorder in any
given year and that 17% of all men and
women will suffer from a depressive
disorder at some point in their lives.
Development Status: Clinical data.
Inventors: Francis J. McMahon et al.
(NIMH).
Patent Status: U.S. Provisional
Application No. 60/854,978 Filed 27
Oct 2006 (HHS Reference No. E–157–
2006/0–US–01).
Licensing Status: Available for
licensing.
Licensing Contact: Norbert Pontzer,
Ph.D., J.D.; 301/435–5502;
pontzern@mail.nih.gov.
Collaborative Research Opportunity:
The National Institute of Mental Health
Mood and Anxiety Disorders Program
Genetics Unit is seeking statements of
capability or interest from parties
interested in collaborative research to
further develop, evaluate, or
commercialize the Predictive Diagnostic
Test for Anti-Depressant Related
Suicide. Please contact Dr. Francis
McMahon at mcmahonf@mail.nih.gov
for more information.
Dated: October 11, 2007.
Steven M. Ferguson,
Director, Division of Technology Development
and Transfer, Office of Technology Transfer,
National Institutes of Health.
[FR Doc. E7–20483 Filed 10–16–07; 8:45 am]
BILLING CODE 4140–01–P
DEPARTMENT OF HEALTH AND
HUMAN SERVICES
National Institutes of Health
Government-Owned Inventions;
Availability for Licensing
National Institutes of Health,
Public Health Service, HHS.
ACTION: Notice.
AGENCY:
SUMMARY: The inventions listed below
are owned by an agency of the U.S.
Government and are available for
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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 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 will
be required to receive copies of the
patent applications.
HIV–1 Integrase Inhibitors for the
Treatment of Retroviral Infections
Description of Technology: This
technology describes the structure and
activity of N-benzyl derivatives of 2,3dihydro-6,7-dihydroxy-1H-isoindol-1ones and 2,3-dihydro-6,7-dihydroxy-1Hisoindole-1,3(2H)-diones as new HIV–1
integrase inhibitors. HIV, as well as
other retroviruses, requires three key
viral enzymes for replication: Reverse
transcriptase, protease and integrase
(IN). A significant number of patients
fail to respond to combination therapies
consisting of reverse transcriptase and
protease inhibitors, due to the
development of viral resistance. IN
functions by initial processing of viral
cDNA in a cleavage step termed 3′processing (3′-P). This is followed by
insertion of the cleaved cDNA into the
host genome in a reaction known as
‘‘strand transfer’’ (ST). Certain agents
covered under the subject technology
have been shown to exhibit selective
inhibition of ST reactions relative to 3′P reactions. These compounds inhibit
purified IN in vitro and are also active
against HIV–1 derived vectors in cellbased assay. These inhibitors may have
a potential therapeutic value for
retroviral infections, including AIDS,
especially for patients exhibiting drug
resistance to current therapy regimes.
Applications: The treatment and
prevention of HIV infections.
Development Status: In vitro data
available.
Inventors: Terrence R. Burke Jr., Xue
Zhi Zhao, Yves Pommier, and Elena
Semenova (NCI).
Related Publication: WG Verschueren
et al. Design and optimization of
tricyclic phtalimide analogue as novel
inhibitors of HIV–1 integrase. J Med
Chem 2005 Mar 24;48(6):1930–1940.
E:\FR\FM\17OCN1.SGM
17OCN1
Federal Register / Vol. 72, No. 200 / Wednesday, October 17, 2007 / Notices
Patent Status: U.S. Provisional
Application No. 60/956,636 filed 17
Aug 2007 (HHS Reference No. E–237–
2007/0–US–01).
Licensing Status: Available for
licensing.
Licensing Contact: Sally Hu, Ph.D.,
M.B.A.; 301/435–5606;
HuS@mail.nih.gov.
Collaborative Research Opportunity:
The National Cancer Institute’s
Laboratory of Medicinal Chemistry and
Laboratory of Molecular Pharmacology
are seeking statements of capability or
interest from parties interested in
collaborative research to further
develop, evaluate, or commercialize the
HIV–1 integrase inhibitors described.
Please contact John D. Hewes, Ph.D. at
301–435–3121 or hewesj@mail.nih.gov
for more information.
sroberts on PROD1PC70 with NOTICES
Thiazepine Inhibitors of HIV–1
Integrase
Description of Technology: The
human immunodeficiency virus (HIV) is
the causative agent of acquired
immunodeficiency syndrome (AIDS).
Drug-resistance is a critical factor
contributing to the gradual loss of
clinical benefit to treatments for HIV
infection. Accordingly, combination
therapies have further evolved to
address the mutating resistance of HIV.
However, there has been great concern
regarding the apparent growing
resistance of HIV strains to current
therapies.
It has been found that a certain class
of compounds including thiazepines
and analogs and derivatives thereof are
effective and selective anti-integrase
inhibitors. These compounds have been
found to inhibit both viral replication
and the activity of purified HIV–1
integrase. The subject invention
provides for such compounds and for
methods of inhibiting HIV integrase.
Inventors: Yves Pommier et al. (NCI).
Patent Status: U.S. Patent No.
7,015,212 issued 21 Mar 2006 (HHS
Reference No. E–036–1999/0–US–03).
Licensing Status: Available for
exclusive or non-exclusive licensing.
Licensing Contact: Sally Hu, Ph.D.,
M.B.A.; 301/435–5606;
HuS@mail.nih.gov.
Collaborative Research Opportunity:
The Laboratory of Molecular
Pharmacology of the National Cancer
Institute is seeking statements of
capability or interest from parties
interested in collaborative research to
further develop, evaluate, or
commercialize anti-integrase inhibitors.
Please contact John D. Hewes, Ph.D. at
301–435–3121 or hewesj@mail.nih.gov
for more information.
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Quinoline Inhibitors of Retroviral
Integrase
Description of Technology: The
subject invention describes certain
diketo quinolin-4–1 derivatives and
their use as integrase inhibitors in the
treatment of HIV infection. The results
of in vitro integrase inhibition studies
show that these derivatives have
significant anti-integrase activity (e.g.,
an IC50 for strand transfer inhibition of
not greater than 2 µM). Thus, these
derivatives might be potentially
important lead compounds for the
development of integrase inhibitors.
Since HIV integrase is an essential
enzyme for effective viral replication,
the development of such inhibitors of
HIV integrase would thus potentially be
useful and effective in the treatment of
HIV infection.
Inventors: Yves Pommier et al. (NCI).
Patent Status: U.S. Patent Application
No. 10/591,679 filed 01 Sep 2006,
claiming priority to 10 Mar 2004 (HHS
Reference No. E–187–2003/0–US–01).
Licensing Contact: Sally Hu, Ph.D.,
M.B.A.; 301/435–5606;
HuS@mail.nih.gov.
Discovery of Tropolone Inhibitors of
HIV–1 Integrase that can be Used for
the Treatment of Retroviral Infection,
Including AIDS
Description of Technology: This
invention provides pharmaceutical
compositions comprising one or more
HIV–1 integrase inhibitor compounds,
as well as methods for treatment or
prevention of HIV infection. These
compounds are alpha-hydroxytropolone
or its salt, solvate or hydrate, and they
have been shown to inhibit the integrase
by interfering with the enzyme catalytic
site by chelating magnesium ions, and
have been shown to inhibit the strand
transfer reaction. Integrase is an
important target for AIDS therapy since
it is critical for viral replication, and
does not have cellular counterparts,
which can potentially reduce toxic side
effects. Thus, the compounds of this
invention can be developed as novel
anti-viral agents that can be used in
combinational therapy, especially since
they might be less toxic than other antiviral agents.
In addition to licensing, the
technology is available for further
development through collaborative
research opportunities with the
inventors.
Inventors: Yves Pommier et al. (NCI).
Patent Status: PCT Application No.
PCT/US2006/046259 filed 01 Dec 2006,
which published as WO 2007/065007
on 06 Jul 2007 (HHS Reference No. E–
308–2005/0–PCT–02).
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58859
Licensing Contact: Sally Hu, Ph.D.,
M.B.A.; 301/435–5606;
HuS@mail.nih.gov.
Integrase Inhibitors for the Treatment
of Retroviral Infection Including
Human Immunodeficiency Virus-1
Description of Technology: Available
for licensing and commercial
development are stilbenedisulfonic acid
derivatives for treatment of human
immunodeficiency virus-1 (HIV–1) and
other retroviral infections. Current HIV–
1 therapeutic treatments target the viral
protease and reverse transcriptase
enzymes, which are essential for
retroviral infection. However, these
drugs often have limitations due to drug
resistant variants, which render drugs
ineffective. Additionally, such drugs are
often toxic when administered in
combination therapies. Thus, efficacious
inhibitors of retroviral infection that are
devoid of toxicity are presently needed.
The subject invention describes
stilbenedisulfonic acid derivatives,
which target the integrase enzyme of
retroviruses. Similar to protease and
reverse transcriptase activity, integrase
function is essential for retroviral
infection. Integrase catalyzes integration
of reverse transcribed viral DNA into a
host cell’s genome. For this reason,
integrase is considered a rational
therapeutic target for HIV–1 infection.
Further, integrase is a favorable target
because the enzyme has no human
cellular counterpart, which could
interact with a potential integrase
inhibitor and cause harmful side effects.
Recent clinical data with an integrase
inhibitor from Merck shows impressive
clinical activity. The Merck compound
is different from the current invention
and is projected for FDA approval mid
2007. Thus, the subject invention is
valuable for safe and effective treatment
of HIV–1 and other retroviral infections.
Application: Treatment of HIV
infection.
Development Status: The technology
is ready for use in drug discovery and
development.
Inventors: Yves Pommier (NCI), Elena
Semenova (NCI), Christophe Marchand
(NCI).
Patent Status: U.S. Provisional
Application No. 60/849,718 filed 04 Oct
2006 (HHS Reference No. E–264–2006/
0–US–01).
Licensing Status: Available for
exclusive or non-exclusive licensing.
Licensing Contact: Sally Hu, Ph.D.,
M.B.A.; 301/435–5606;
HuS@mail.nih.gov.
E:\FR\FM\17OCN1.SGM
17OCN1
58860
Federal Register / Vol. 72, No. 200 / Wednesday, October 17, 2007 / Notices
Dated: October 10, 2007.
Steven M. Ferguson,
Director, Division of Technology Development
and Transfer, Office of Technology Transfer,
National Institutes of Health.
[FR Doc. E7–20513 Filed 10–16–07; 8:45 am]
BILLING CODE 4140–01–P
DEPARTMENT OF HEALTH AND
HUMAN SERVICES
National Institutes of Health
Government-Owned Inventions;
Availability for Licensing
National Institutes of Health,
Public Health Service, HHS.
ACTION: Notice.
AGENCY:
sroberts on PROD1PC70 with NOTICES
SUMMARY: The inventions listed below
are owned by an agency 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 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 will
be required to receive copies of the
patent applications.
Alpha 1-3 NAcetylgalactosaminyltransferases With
Altered Donor and Acceptor
Specificities, Compositions, and
Methods of Use
Description of Invention: The present
invention relates to the field of
glycobiology, specifically to
glycosyltransferases. The present
invention provides structure-based
design of novel glycosyltransferases and
their biological applications.
The structural information of
glycosyltransferases has revealed that
the specificity of the sugar donor in
these enzymes is determined by a few
residues in the sugar-nucleotide binding
pocket of the enzyme, which is
conserved among the family members
from different species. This
conservation has made it possible to
reengineer the existing
glycosyltransferases with broader sugar
donor specificities. Mutation of these
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residues generates novel
glycosyltransferases that can transfer a
sugar residue with a chemically reactive
functional group to Nacetylglucosarnine (GlcNAc), galactose
(Gal) and xylose residues of
glycoproteins, glycolipids and
proteoglycans (glycoconjugates). Thus,
there is potential to develop mutant
glycosyltransferases to produce
glycoconjugates carrying sugar moieties
with reactive groups that can be used in
the assembly of bio-nanoparticles to
develop targeted-drug delivery systems
or contrast agents for medical uses.
Accordingly, methods to synthesize
N-acetylglucosamine linkages have
many applications in research and
medicine, including in the development
of pharmaceutical agents and improved
vaccines that can be used to treat
disease.
This application claims compositions
and methods based on the structurebased design of alpha 1-3 NAcetylgalactosaminyltransferase (alpha
3 GalNAc-T) mutants from alpha 13galactosyltransferase (a3Gal-T) that can
transfer 2′-modified galactose from the
corresponding UDP-derivatives due to
mutations that broaden the alpha 3GalT donor specificity and make the
enzyme alpha3 GalNAc-T.
Application: Development of
pharmaceutical agents and improved
vaccines.
Developmental Status: Enzymes have
been synthesized and preclinical studies
have been performed.
Inventors: Pradman Qasba, Boopathy
Ramakrishnan, Elizabeth Boeggman,
Marta Pasek (NCI).
Patent Status: PCT Patent Application
filed 22 Aug 2007 (HHS Reference No.
E–279–2007/0–PCT–01).
Licensing Status: Available for
exclusive or non-exclusive licensing.
Licensing Contact: Peter A. Soukas,
J.D.; 301/435–4646;
soukasp@mail.nih.gov.
Collaborative Research Opportunity:
The National Cancer Institute’s
Nanobiology Program is seeking
statements of capability or interest from
parties interested in collaborative
research to further develop, evaluate, or
commercialize structure-based design of
novel glycosyltransferases. Please
contact John D. Hewes, Ph.D. at 301–
435–3121 or hewesj@mail.nih.gov for
more information.
Beta 1,4-Galactosyltransferases With
Altered Donor and Acceptor
Specificities, Compositions and
Methods of Use
Description of Invention: The present
invention relates to the field of
glycobiology, specifically to
PO 00000
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Fmt 4703
Sfmt 4703
glycosyltransferases. The present
invention provides structure-based
design of novel glycosyltransferases and
their biological applications.
The structural information of
glycosyltransferases has revealed that
the specificity of the sugar donor in
these enzymes is determined by a few
residues in the sugar-nucleotide binding
pocket of the enzyme, which is
conserved among the family members
from different species. This
conservation has made it possible to
reengineer the existing
glycosyltransferases with broader sugar
donor specificities. Mutation of these
residues generates novel
glycosyltransferases that can transfer a
sugar residue with a chemically reactive
functional group to Nacetylglucosarnine (GlcNAc), galactose
(Gal) and xylose residues of
glycoproteins, glycolipids and
proteoglycans (glycoconjugates). Thus,
there is potential to develop mutant
glycosyltransferases to produce
glycoconjugates carrying sugar moieties
with reactive groups that can be used in
the assembly of bio-nanoparticles to
develop targeted-drug delivery systems
or contrast agents for medical uses.
Accordingly, methods to synthesize
N-acetylglucosamine linkages have
many applications in research and
medicine, including in the development
of pharmaceutical agents and improved
vaccines that can be used to treat
disease.
The invention claims beta (1,4)galactosyltransferase I mutants having
altered donor and acceptor and metal
ion specificities, and methods of use
thereof. In addition, the invention
claims methods for synthesizing
oligosaccharides using the beta (1,4)galactosyltransferase I mutants and to
using the beta (1,4)-galactosyltransferase
I mutants to conjugate agents, such as
therapeutic agents or diagnostic agents,
to acceptor molecules. More
specifically, the invention claims a
double mutant beta 1,4
galactosyltransferase, human beta-1,4Tyr289Leu-Met344His-Gal-T1,
constructed from the individual
mutants, Tyr289Leu-Gal-T1 and
Met344His-Gal-T1, that transfers
modified galactose in the presence of
magnesium ion, in contrast to the wildtype enzyme which requires manganese
ion.
Application: Development of
pharmaceutical agents and improved
vaccines.
Developmental Status: Enzymes have
been synthesized and preclinical studies
have been performed.
E:\FR\FM\17OCN1.SGM
17OCN1
]]>Agencies
[Federal Register Volume 72, Number 200 (Wednesday, October 17, 2007)]
[Notices]
[Pages 58858-58860]
From the Federal Register Online via the Government Printing Office [www.gpo.gov]
[FR Doc No: E7-20513]
-----------------------------------------------------------------------
DEPARTMENT OF HEALTH AND HUMAN SERVICES
National Institutes of Health
Government-Owned Inventions; Availability for Licensing
AGENCY: National Institutes of Health, Public Health Service, HHS.
ACTION: Notice.
-----------------------------------------------------------------------
SUMMARY: The inventions listed below are owned by an agency 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 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 will be required to receive
copies of the patent applications.
HIV-1 Integrase Inhibitors for the Treatment of Retroviral Infections
Description of Technology: This technology describes the structure
and activity of N-benzyl derivatives of 2,3-dihydro-6,7-dihydroxy-1H-
isoindol-1-ones and 2,3-dihydro-6,7-dihydroxy-1H-isoindole-1,3(2H)-
diones as new HIV-1 integrase inhibitors. HIV, as well as other
retroviruses, requires three key viral enzymes for replication: Reverse
transcriptase, protease and integrase (IN). A significant number of
patients fail to respond to combination therapies consisting of reverse
transcriptase and protease inhibitors, due to the development of viral
resistance. IN functions by initial processing of viral cDNA in a
cleavage step termed 3'-processing (3'-P). This is followed by
insertion of the cleaved cDNA into the host genome in a reaction known
as ``strand transfer'' (ST). Certain agents covered under the subject
technology have been shown to exhibit selective inhibition of ST
reactions relative to 3'-P reactions. These compounds inhibit purified
IN in vitro and are also active against HIV-1 derived vectors in cell-
based assay. These inhibitors may have a potential therapeutic value
for retroviral infections, including AIDS, especially for patients
exhibiting drug resistance to current therapy regimes.
Applications: The treatment and prevention of HIV infections.
Development Status: In vitro data available.
Inventors: Terrence R. Burke Jr., Xue Zhi Zhao, Yves Pommier, and
Elena Semenova (NCI).
Related Publication: WG Verschueren et al. Design and optimization
of tricyclic phtalimide analogue as novel inhibitors of HIV-1
integrase. J Med Chem 2005 Mar 24;48(6):1930-1940.
[[Page 58859]]
Patent Status: U.S. Provisional Application No. 60/956,636 filed 17
Aug 2007 (HHS Reference No. E-237-2007/0-US-01).
Licensing Status: Available for licensing.
Licensing Contact: Sally Hu, Ph.D., M.B.A.; 301/435-5606;
HuS@mail.nih.gov.
Collaborative Research Opportunity: The National Cancer Institute's
Laboratory of Medicinal Chemistry and Laboratory of Molecular
Pharmacology are seeking statements of capability or interest from
parties interested in collaborative research to further develop,
evaluate, or commercialize the HIV-1 integrase inhibitors described.
Please contact John D. Hewes, Ph.D. at 301-435-3121 or
hewesj@mail.nih.gov for more information.
Thiazepine Inhibitors of HIV-1 Integrase
Description of Technology: The human immunodeficiency virus (HIV)
is the causative agent of acquired immunodeficiency syndrome (AIDS).
Drug-resistance is a critical factor contributing to the gradual loss
of clinical benefit to treatments for HIV infection. Accordingly,
combination therapies have further evolved to address the mutating
resistance of HIV. However, there has been great concern regarding the
apparent growing resistance of HIV strains to current therapies.
It has been found that a certain class of compounds including
thiazepines and analogs and derivatives thereof are effective and
selective anti-integrase inhibitors. These compounds have been found to
inhibit both viral replication and the activity of purified HIV-1
integrase. The subject invention provides for such compounds and for
methods of inhibiting HIV integrase.
Inventors: Yves Pommier et al. (NCI).
Patent Status: U.S. Patent No. 7,015,212 issued 21 Mar 2006 (HHS
Reference No. E-036-1999/0-US-03).
Licensing Status: Available for exclusive or non-exclusive
licensing.
Licensing Contact: Sally Hu, Ph.D., M.B.A.; 301/435-5606;
HuS@mail.nih.gov.
Collaborative Research Opportunity: The Laboratory of Molecular
Pharmacology of the National Cancer Institute is seeking statements of
capability or interest from parties interested in collaborative
research to further develop, evaluate, or commercialize anti-integrase
inhibitors. Please contact John D. Hewes, Ph.D. at 301-435-3121 or
hewesj@mail.nih.gov for more information.
Quinoline Inhibitors of Retroviral Integrase
Description of Technology: The subject invention describes certain
diketo quinolin-4-1 derivatives and their use as integrase inhibitors
in the treatment of HIV infection. The results of in vitro integrase
inhibition studies show that these derivatives have significant anti-
integrase activity (e.g., an IC50 for strand transfer inhibition of not
greater than 2 [mu]M). Thus, these derivatives might be potentially
important lead compounds for the development of integrase inhibitors.
Since HIV integrase is an essential enzyme for effective viral
replication, the development of such inhibitors of HIV integrase would
thus potentially be useful and effective in the treatment of HIV
infection.
Inventors: Yves Pommier et al. (NCI).
Patent Status: U.S. Patent Application No. 10/591,679 filed 01 Sep
2006, claiming priority to 10 Mar 2004 (HHS Reference No. E-187-2003/0-
US-01).
Licensing Contact: Sally Hu, Ph.D., M.B.A.; 301/435-5606;
HuS@mail.nih.gov.
Discovery of Tropolone Inhibitors of HIV-1 Integrase that can be Used
for the Treatment of Retroviral Infection, Including AIDS
Description of Technology: This invention provides pharmaceutical
compositions comprising one or more HIV-1 integrase inhibitor
compounds, as well as methods for treatment or prevention of HIV
infection. These compounds are alpha-hydroxytropolone or its salt,
solvate or hydrate, and they have been shown to inhibit the integrase
by interfering with the enzyme catalytic site by chelating magnesium
ions, and have been shown to inhibit the strand transfer reaction.
Integrase is an important target for AIDS therapy since it is critical
for viral replication, and does not have cellular counterparts, which
can potentially reduce toxic side effects. Thus, the compounds of this
invention can be developed as novel anti-viral agents that can be used
in combinational therapy, especially since they might be less toxic
than other anti-viral agents.
In addition to licensing, the technology is available for further
development through collaborative research opportunities with the
inventors.
Inventors: Yves Pommier et al. (NCI).
Patent Status: PCT Application No. PCT/US2006/046259 filed 01 Dec
2006, which published as WO 2007/065007 on 06 Jul 2007 (HHS Reference
No. E-308-2005/0-PCT-02).
Licensing Contact: Sally Hu, Ph.D., M.B.A.; 301/435-5606;
HuS@mail.nih.gov.
Integrase Inhibitors for the Treatment of Retroviral Infection
Including Human Immunodeficiency Virus-1
Description of Technology: Available for licensing and commercial
development are stilbenedisulfonic acid derivatives for treatment of
human immunodeficiency virus-1 (HIV-1) and other retroviral infections.
Current HIV-1 therapeutic treatments target the viral protease and
reverse transcriptase enzymes, which are essential for retroviral
infection. However, these drugs often have limitations due to drug
resistant variants, which render drugs ineffective. Additionally, such
drugs are often toxic when administered in combination therapies. Thus,
efficacious inhibitors of retroviral infection that are devoid of
toxicity are presently needed.
The subject invention describes stilbenedisulfonic acid
derivatives, which target the integrase enzyme of retroviruses. Similar
to protease and reverse transcriptase activity, integrase function is
essential for retroviral infection. Integrase catalyzes integration of
reverse transcribed viral DNA into a host cell's genome. For this
reason, integrase is considered a rational therapeutic target for HIV-1
infection. Further, integrase is a favorable target because the enzyme
has no human cellular counterpart, which could interact with a
potential integrase inhibitor and cause harmful side effects. Recent
clinical data with an integrase inhibitor from Merck shows impressive
clinical activity. The Merck compound is different from the current
invention and is projected for FDA approval mid 2007. Thus, the subject
invention is valuable for safe and effective treatment of HIV-1 and
other retroviral infections.
Application: Treatment of HIV infection.
Development Status: The technology is ready for use in drug
discovery and development.
Inventors: Yves Pommier (NCI), Elena Semenova (NCI), Christophe
Marchand (NCI).
Patent Status: U.S. Provisional Application No. 60/849,718 filed 04
Oct 2006 (HHS Reference No. E-264-2006/0-US-01).
Licensing Status: Available for exclusive or non-exclusive
licensing.
Licensing Contact: Sally Hu, Ph.D., M.B.A.; 301/435-5606;
HuS@mail.nih.gov.
[[Page 58860]]
Dated: October 10, 2007.
Steven M. Ferguson,
Director, Division of Technology Development and Transfer, Office of
Technology Transfer, National Institutes of Health.
[FR Doc. E7-20513 Filed 10-16-07; 8:45 am]
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