Potent and Selective Analogues of Modafinil and Uses Thereof

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.

Potential Commercial Applications: Competitive Advantages:
  • 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 Stage:


Related Invention(s):


Amy Newman (NIDA)  ➽ more inventions...

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Intellectual Property:
US Application No. 14/772,486
US Application No. 15/830,244
US Application No. 61/774,878
PCT Application No. PCT/US2014/021514
Patent applications filed in Europe, Canada and Australia

Collaboration 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 James D. Hewes, Ph.D. at john.hewes@nih.gov.

Licensing Contact:
Benfeard Williams, Ph.D.
Email: benfeard.williams@nih.gov
Phone: 240.276.6606

OTT Reference No: E-073-2013/0
Updated: Oct 11, 2017