[Federal Register Volume 81, Number 223 (Friday, November 18, 2016)]
[Notices]
[Page 81787]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2016-27770]
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DEPARTMENT OF HEALTH AND HUMAN SERVICES
National Institutes of Health
Government-Owned Inventions; Availability for Licensing and/or
Co-Development
AGENCY: National Institutes of Health, Department of Health and Human
Services.
ACTION: Notice.
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SUMMARY: The invention listed below is owned by an agency of the U.S.
Government and is available for licensing and/or co-development in the
U.S. 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 and/or co-development.
ADDRESSES: Invention Development and Marketing Unit, Technology
Transfer Center, National Cancer Institute, 9609 Medical Center Drive,
Mail Stop 9702, Rockville, MD 20850-9702.
FOR FURTHER INFORMATION CONTACT: Information on licensing and co-
development research collaborations, and copies of the U.S. patent
applications listed below may be obtained by contacting: Attn.
Invention Development and Marketing Unit, Technology Transfer Center,
National Cancer Institute, 9609 Medical Center Drive, Mail Stop 9702,
Rockville, MD 20850-9702, Tel. 240-276-5515 or email
[email protected]. A signed Confidential Disclosure
Agreement may be required to receive copies of the patent applications.
SUPPLEMENTARY INFORMATION: Technology description follows.
Title of invention: Methods of Making and Using Dopamine D3
Receptor Selective Antagonists/Partial Agonists
Summary of Technology: A library of novel compounds that
selectively bind the dopamine D3 receptor have been designed
and characterized extensively. In vivo rodent studies indicate selected
lead molecules may be useful to treat drug addiction/dependence.
Description of Technology: Dopamine is a major neurotransmitter in
the central nervous system and among other functions is directly
related to the rewarding effects of drugs of abuse. Dopamine signaling
is mediated by D1, D2, D3,
D4 and D5 receptors. The dopamine D3
receptor is a known target to treat a variety of neuropsychiatric
disorders, including substance use disorders (e.g. cocaine and opioid),
schizophrenia and depression. Despite extensive efforts, it has proven
difficult to identify a lead molecule that selectively binds to
D3 receptors (versus D2 receptors, for example),
with the desired pharmacological and pharmacokinetic profile. For
example, metabolic instability or predicted toxicity has precluded
successful translation of previously reported D3R-selective
antagonists to clinical use for cocaine abuse.
The library of compounds is designed to have high affinity and
specificity for the dopamine D3 receptor. Preliminary
studies at National Institute of Drug Abuse (NIDA) indicate that
selected lead compounds have promising in vivo activity in rodents,
including reduced acquisition to self-administration of oxycodone,
inhibition of reinstatement to oxycodone seeking, and ameliorating
naloxone-precipitated withdrawal from oxycodone dependence.
This invention is owned by an agency of the U.S. Government and is
available for licensing and/or co-development 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 and/or co-development.
Potential Commercial Applications:
Treatment of Opioid Use Disorders
Treatment of Schizophrenia
Treatment of Bipolar Disorder
Treatment of cannabis (Tetrahydrocannabinol, THC) dependence
Value Proposition: Despite extensive efforts to develop
D3 receptor-selective compounds, it has proven difficult to
identify a ligand with the desired pharmacological and pharmacokinetic
profile for translation to the clinic. The D3 receptor
ligands described herein may be useful to treat a variety of diseases,
including opioid use disorders and schizophrenia.
Development Stage: Pre-clinical (in vivo validation).
Inventor(s): Amy Newman and Vivek Kumar (NIDA).
Intellectual Property: E-053-2016 United States Provisional Patent
Application No. 62/307,600, filed March 14, 2016, titled ``Dopamine D3
Receptor Selective Antagonists/Partial Agonists; Methods of Making and
Use Thereof''.
Publications: J Med Chem. 2016 Aug 25;59(16):7634-50. doi: 10.1021/
acs.jmedchem.6b00860. Epub 2016 Aug 10.
Collaboration Opportunity: Researchers at the NIDA seek licensing
and/or co-development research collaborations for development of
Dopamine D3 ligands to treat opioid use disorders.
Contact Information: Requests for copies of the patent application
or inquiries about licensing, research collaborations, and co-
development opportunities should be sent to John D. Hewes, Ph.D.,
email: [email protected].
Dated: November 10, 2016.
John D. Hewes,
Technology Transfer Specialist, Technology Transfer Center, National
Cancer Institute.
[FR Doc. 2016-27770 Filed 11-17-16; 8:45 am]
BILLING CODE 4140-01-P