[Federal Register Volume 80, Number 162 (Friday, August 21, 2015)]
[Notices]
[Pages 50858-50859]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2015-20694]
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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.
SUPPLEMENTARY INFORMATION: Technology descriptions follow.
Novel Benztropine Analogs for Treatment of Cocaine Abuse and Other
Mental Disorders
Description of Technology: Dopamine is a neurotransmitter that
exerts important effects on locomotor activity, motivation and reward,
and cognition. The dopamine transporter (DAT) is expressed on the
plasma membrane of dopamine synthesizing neurons, and is responsible
for clearing dopamine released into the extra-cellular space, thereby
regulating neurotransmission. The dopamine transporter plays a
significant role in neurotoxicity and human diseases, such as
Parkinson's disease, drug abuse (especially cocaine addiction),
Attention Deficit Disorder/Attention Deficit Hyperactivity Disorder
(ADD/ADHD), and a number of other CNS disorders. Therefore, the
dopamine transporter is a strong target for research and the discovery
of potential therapeutics for the treatment of these indications.
This invention discloses novel benztropine analogs and methods of
using these analogs for treatment of mental and conduct disorders such
as cocaine abuse, narcolepsy, ADHD, obesity and nicotine abuse. The
disclosed analogs are highly selective and potent inhibitors of DAT,
but without an apparent cocaine-like behavioral profile. In addition to
their use as a treatment for cocaine abuse, these compounds have also
shown efficacy in animal models of ADHD and nicotine abuse, and have
also been shown to reduce food intake in animals. They may also be
useful medications for other indications where dopamine-related
behavior is compromised, such as alcohol addiction, tobacco addiction,
and Parkinson's disease.
Potential Commercial Applications:
Drug leads for treatment of cocaine abuse, ADHD, nicotine
abuse, obesity, and other dopamine-related disorders
Imaging probes for dopamine transporter binding sites
Development Stage: Early-stage; In vitro data available
Inventors: Amy H. Newman, Mu-fa Zou, Jonathan L. Katz (all of NIDA)
Intellectual Property: HHS Reference No. E-234-2005/1--US Patent
No. 8,383,817 issued February 26, 2013
Licensing Contact: Betty B. Tong, Ph.D.; 301-594-6565;
[email protected]
Collaborative Research Opportunity: The National Institute on Drug
Abuse, Medicinal Chemistry and Psychobiology Sections, is seeking
statements of capability or interest from parties interested in
collaborative research to further develop, evaluate, or commercialize
medications to treat cocaine abuse and addiction. For collaboration
opportunities please contact John D. Hewes, Ph.D. at
[email protected].
Novel Dopamine Receptor Ligands as Therapeutics for Central Nervous
System Disorders
Description of Technology: The dopamine D3 receptor subtype is a
member of the dopamine D2 subclass of receptors. These receptors have
been implicated in a number of CNS disorders, including psychostimulant
[[Page 50859]]
abuse, psychosis and Parkinson's disease. Compounds that bind with high
affinity and selectivity to D3 receptors can not only provide important
tools with which to study the structure and function of this receptor
subtype, but may also have therapeutic potential in the treatment of
numerous psychiatric and neurologic disorders.
The 4-phenylpiperazine derivatives are an important class of
dopamine D3 selective ligands. However, due to their highly lipophilic
nature, these compounds suffer from solubility problems in aqueous
media and reduced bioavailability. To address this problem, a process
was designed to introduce functionality into the carbon chain linker of
these compounds. Compared to currently available dopamine D3 receptor
ligands, the resulting compounds show improved pharmacological
properties and D3 selectivities but due to their more hydrophilic
nature, these derivatives are predicted to have improved water
solubility and bioavailability.
Potential Commercial Applications:
Therapeutics for a variety of psychiatric and neurologic
disorders
Research tools to study D3 receptor structure and function
Competitive Advantages:
Improved pharmacological properties and selectivity over
existing dopamine D3 receptor ligands
Hydrophilic nature likely to lead to improved water
solubility and bioavailability
Development Stage: Early-stage; In vitro data available
Inventors: Amy H. Newman (NIDA), Peter Grundt (NIDA), Jianjing Cao
(NIDA), Robert Luedtke
Intellectual Property: HHS Reference No. E-128-2006/0--US Patent
No. 8,748,608 issued June 10, 2014
Licensing Contact: Betty B. Tong, Ph.D.; 301-594-6565;
[email protected]
Collaborative Research Opportunity: The National Institute on Drug
Abuse, Medications Discovery Research Branch, is seeking statements of
capability or interest from parties interested in collaborative
research to further develop, evaluate, or commercialize 4-
phenylpiperazine derivatives as dopamine D3 selective ligands. For
collaboration opportunities, please contact Vio Conley, M.S. at 240-
276-5531 or [email protected].
Genome Wide DNase I Hypersensitive Sites Detection in Formalin-Fixed
Paraffin-Embedded Single Cells
Description of Technology: A method of detecting DNase I
hypersensitive sites ((DHS) in a single cell or very small number of
cells, including cells recovered from formalin-fixed paraffin-embedded
(FFPE) tissue slides of patient samples. DHS has revealed a large
number of potential regulatory elements for transcriptional regulation
in various cell types. The application of DNase-Seq techniques to
patient samples can elucidate pathophysiological mechanisms of gene
function in a variety of diseases as well as provide potentially
important diagnostic and prognostic information. Unfortunately, the
current DNase-Seq techniques require large number of cells and are
applicable only to larger biopsies and surgical specimens. This
technique, called Pico-Seq, allows detection when only very small
population of cells are available, such as rare primary tumor cells and
circulating-tumor-cells, isolated by a variety of methods. Pico-Seq
uses conditions capable of restoring the DNase I sensitivity, similar
to native/fresh cells, in tissue/cells from slides processed by
extremely harsh conditions, such as in FFPE tissues.
Potential Commercial Applications:
Diagnostic and prognostic kits
Research kits
Competitive Advantages:
Applicable to very small number of cells down to a single
cell.
Capable of using cells isolated by any of the available
methods, including flow cytometry, biopsies, laser capture
microdissection, and even cells recovered from formalin-fixed paraffin-
embedded tissue slides of patient samples.
Development Stage: Early-stage; In vitro data available
Inventors: Keji Zhao and Tang Qingsong (NHLBI)
Intellectual Property: HHS Reference No. E-254-2014/0--US
Provisional Application No. 62/118,574 filed February 20, 2015
Licensing Contact: Cristina Thalhammer-Reyero, Ph.D., M.B.A.; 301-
435-4507; [email protected]
Dated: August 18, 2015.
Richard U. Rodriguez,
Acting Director, Office of Technology Transfer, National Institutes of
Health.
[FR Doc. 2015-20694 Filed 8-20-15; 8:45 am]
BILLING CODE 4140-01-P