This PDF is the current document as it appeared on Public Inspection on 11/17/2016 at 08:45 am.
National Institutes of Health, Department of Health and Human Services.
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.
Invention Development and Marketing Unit, Technology Transfer Center, National Cancer Institute, 9609 Medical Center Drive, Mail Stop 9702, Rockville, MD 20850-9702.Start Further Info
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 firstname.lastname@example.org. A signed Confidential Disclosure Agreement may be required to receive copies of the patent applications.End Further Info End Preamble Start Supplemental 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 D3 R-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@example.com.Start Signature
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]
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