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Potent and Selective Analogues of Modafinil and Uses Thereof

Posted Jul 24 2013 8:00pm

Description of Invention:
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.

  • 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

  • Higher affinity for monoamine transporters (DAT, SERT, and NET)
  • Lower effective doses
  • Better bioavailability
  • Improved water solubility

Development Status:

Amy H Newman (NIDA)
Jianjing Cao (NIDA)
Oluyomi M Okunola-Bakare (NIDA)

Patent Status:
HHS, Reference No. E-073-2013/0
US, Application No. 61/774,878 filed 08 Mar 2013

Related Technologies:
US, Application No. 12/664,668 filed 15 Dec 2009, Reference No. E-128-2006/0

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 .

For Licensing Information Please Contact:
Charlene Sydnor Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-4689
Fax: 301-402-0220

Ref No: 2595

Updated: 07/2013

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