Government-Owned Inventions; Availability for Licensing and/or Co-Development

AGENCY:

National Institutes of Health, Department of Health and Human Services.

ACTION:

Notice.

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 ncitechtransfer@mail.nih.gov. 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 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: john.hewes@nih.gov.