[Federal Register Volume 78, Number 147 (Wednesday, July 31, 2013)]
[Notices]
[Pages 46356-46357]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2013-18329]
[[Page 46356]]
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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, HHS.
ACTION: Notice.
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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. 209 and 37 CFR Part 404 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.
FOR FURTHER INFORMATION CONTACT: 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.
Arsenical Compounds as Therapeutics for Inflammatory Diseases
Description of Technology: FDA approved Arsenic trioxide (Trisenox
or As2O3) and other arsenical compounds for
treatment of acute inflammatory conditions have been shown to be anti-
inflammasome therapies. Inflammasomes are large cytoplasmic multi-
protein complexes that form in response to intracellular danger signals
and play a key role in many infections by controlling the innate immune
response. Inflammasome activation has been implicated in metabolic
disorders, such as diabetes, and inflammatory diseases, such as gout,
arthritis, and cholesterol-associated atherosclerosis. The technology
relates to arsenical compounds that inhibit a number of inflammasomes,
including the Nlrpl, Nlrp3 and Naip5/Nlrc4, primarily by acting as an
inhibitor of caspase-1 activity in innate immune cells (macrophages).
It was shown that arsenical compounds induce a cellular condition which
inhibits both the autoproteolytic activity of caspase-1, as well as its
ability to cleave cytokine substrates. Further, it was shown that the
inhibition does not occur through direct modification or inhibition of
the caspase-1 enzyme, but rather through induction of a cellular
environment inhibitory to its activity. Efficacy in inhibiting immune
cell recruitment in a mouse model of gout has been demonstrated. The
arsenicals have potential as treatment for a variety of inflammatory
conditions.
Potential Commercial Applications: Therapeutics for rheumatoid
arthritis, gout, colitis and various inflammatory skin diseases.
Competitive Advantages: These FDA-approved compounds have potential
off-target use for treatment of acute inflammatory conditions shown to
be responsive to anti-inflammasome therapies.
Development Stage:
Early-stage
Pre-clinical
In vitro data available
In vivo data available (animal)
Inventors: Mahtab Moayeri, Nolan K. Maier, Stephen H. Leppla (all
of NIAID)
Intellectual Property: HHS Reference No. E-112-2013/0--U.S.
Provisional Application No. 61/784,138 filed March 14, 2013
Licensing Contact: Suryanarayana (Sury) Vepa, Ph.D., J.D.; 301-435-
5020; [email protected].
A Novel HIV-1 Drug Resistant Integrase Inhibitor
Description of Technology: The subject invention describes a novel
and highly potent inhibitor of HIV-1 integrase (IN) that has high
efficacy against the major forms of Raltegravir-resistant mutant forms
of IN. Thus, this IN inhibitor can be developed as a therapeutic for
patients who have developed resistance to current IN inhibitors, such
as Raltegravir and Elvitegravir.
Potential Commercial Applications: HIV therapeutic.
Competitive Advantages:
High efficacy against the major forms of Raltegravir-
resistant mutant forms of IN in in vitro and whole cell assays.
An HIV therapeutic for patients resistant to current IN
inhibitors.
Development Stage:
Early-stage
In vitro data available
Inventors: Xue Zhi Zhao, Steven Smith, Mathieu Metifiot, Barry
Johnson, Christophe Marchand, Stephen Hughes, Yves Pommier, Terrence
Burke (all of NCI)
Publications:
1. Marchand C, et al. HIV-1 IN inhibitors: 2010 update and
perspectives. Curr Top Med Chem. 2009;9(11):1016-37. [PMID 19747122].
2. Liao C, et al. Authentic HIV-1 integrase inhibitors. Future Med.
Chem. 2010 Jul;2(7):1107-22. [PMID 21426159].
Intellectual Property: HHS Reference No. E-093-2013/0--U.S.
Provisional Patent Application No. 61/824,306 filed May 16, 2013.
Related Technology: PCT, WO2008010964 (A1), Merck.
Licensing Contact: Sally Hu, Ph.D., MBA; 301-435-5606;
[email protected].
Potent and Selective Analogues of Modafinil and Uses Thereof
Description of Technology: This invention describes novel analogues
of modafinil, a wake-promoting agent that has been used to treat
narcolepsy and other sleep disorders.
Modafinil has attracted attention for the treatment of cognitive
dysfunction in disorders such as attention-deficit/hyperactivity
disorder (ADHD) as well as cocaine and methamphetamine dependence.
However, modafinil has relatively low affinity for binding to the
dopamine transporter (DAT) to block dopamine reuptake, and is water-
insoluble, thus requiring large doses to achieve pharmacological
effects.
Investigators at the National Institute of Drug Abuse have
synthesized a series of modafinil analogues that have higher affinity
for the dopamine (DAT), serotonin (SERT) and/or norepinephrine (NET)
transporters and improved water solubility. These novel analogues
present the advantage of higher potency, which may translate into lower
effective doses and better bioavailability over modafinil.
Potential Commercial Applications:
Therapeutic agent for substance abuse (such as nicotine,
cocaine, methamphetamine, opioids)
Therapeutic agent for attention/cognitive disorders (such
as ADHD)
Therapeutic agent for sleep disorders
Competitive Advantages:
Higher affinity for monoamine transporters (DAT, SERT, and
NET)
Lower effective doses
Better bioavailability,
Improved water solubility
Development Stage: Early-stage
Inventors: Amy H. Newman, Oluyomi M. Okunola-Bakare, Jianjing Cao,
Jonathan Katz (all of NIDA)
Intellectual Property: HHS Reference No. E-073-2013/0--U.S.
Provisional Application No. 61/774,878 filed March 8, 2013
Related Technologies:
HHS Reference No. E-251-2002--U.S. Provisional Application
No. 60/410,715.
[[Page 46357]]
HHS Reference No. E-128-2006--PCT Application No. PCT/
US2007/071412.
Licensing Contact: Charlene Sydnor, Ph.D.; 301-435-4689;
[email protected].
Collaborative Research Opportunity: The National Institute on Drug
Abuse is seeking statements of capability or interest from parties
interested in collaborative research to further develop, evaluate or
commercialize Potent and Selective Analogues of Modafinil and Uses
Thereof. For collaboration opportunities, please contact Michelle Kim
Leff, MD, MBA at [email protected].
Translocator Protein 18 kDa PET Radioligands With High Affinities
Regardless of Genotype
Description of Technology: This technology relates to a group of
Translocator protein 18 kDa (TSPO) radioligands for Positron Emission
Tomography (PET) that are specific and accurate, regardless of
genotype. TSPO is a mitochondrial protein expressed in inflammatory
cells, which is a marker for neuroinflammation. Neuroinflammation is
symptomatic of many neuropsychiatric and neurodegenerative disorders,
such as multiple sclerosis, stroke, epilepsy, dementia, and traumatic
brain injuries. Monitoring and quantifying TSPO 18 kDa with
radioligands in PET may have clinical application in understanding,
diagnosing and treating many neuropsychiatric disorders. However,
current TSPO 18 kDa radioligands either lack specificity or, due to
TSPO polymorphisms, have highly variable inter-subject sensitivities
depending on genotype. These new ligands are specific and accurate,
regardless of genotype, allowing simplified interpretation and
quantification of the binding signal.
Potential Commercial Applications: Biomarker or diagnostic for
neuroinflammation
Competitive Advantages: Specific and accurate, regardless of
genotype
Development Stage:
Early-stage
Pre-clinical
In vivo data available (animal)
Inventors: Robert B. Innis, Victor W. Pike, Sam S. Zoghbi, Yi Zhang
(NIMH); Sabrina Castellano (University of Salerno, Italy); Giorgio
Stefancich (University of Trieste, Italy); Sabrina Talia, Federico Da
Settimo, Claudia Martini (University of Pisa, Italy)
Publications:
1. Oh U, et al. Translocator protein PET imaging for glial
activation in multiple sclerosis. J Neuroimmune Pharmacol. 2011
Sep;6(3):354-61. [PMID 20872081]
2. Kreisl WC, et al. Stroke incidentally identified using improved
positron emission tomography for microglial activation. Arch Neurol.
2009 Oct;66(1):1288-9. [PMID 19822787]
3. Hirvonen J, et al. Increased in vivo expression of an
inflammatory marker in temporal lobe epilepsy. J Nucl Med. 2012
Feb;53(2):234-40. [PMID 22238156]
4. Kreisl WC, et al. In vivo radioligand binding to translocator
protein correlates with severity of Alzheimer's disease. Brain. 2013
Jul;136(Pt 7):2228-38. [PMID 23775979]
Intellectual Property: HHS Reference No. E-262-2012/0--U.S.
Provisional Patent Application No. 61/777, 542 filed March 12, 2013
Licensing Contact: Edward (Tedd) Fenn, J.D.; 424-500-2005;
[email protected].
Collaborative Research Opportunity: The National Institute of
Mental Health is seeking statements of capability or interest from
parties interested in collaborative research to further develop,
evaluate or commercialize TSPO radioligands for monitoring
inflammation. For collaboration opportunities, please contact Suzanne
Winfield at [email protected].
Dated: July 25, 2013.
Richard U. Rodriguez,
Director, Division of Technology Development and Transfer, Office of
Technology Transfer, National Institutes of Health.
[FR Doc. 2013-18329 Filed 7-30-13; 8:45 am]
BILLING CODE 4140-01-P