[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