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Analogues of Modafinil for treating sleep and attention disorders

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The National Institute on Drug Abuse’s Medicinal Chemistry Section seeks partners interested in collaborative research to co-develop analogues of modafinil for the treatment of drug abuse and sleep and attention disorders.
NIH Reference Number
Product Type
  • narcolepsy
  • attention deficit/hyperactivity disorder (ADHD)
  • modafinil
  • dopamine (DAT)
  • serotonin (SERT)
  • norepinephrine (NET)
Collaboration Opportunity
This invention is available for licensing.
Description of Technology

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
  • Therapeutic agent for substance abuse (such as nicotine, cocaine, methamphetamine, opioids), for attention/cognitive disorders (such as ADHD), and for sleep disorders.
Competitive Advantages
  • Higher affinity for monoamine transporters (DAT, SERT, and NET) compared to modafinil
  • Analogues have lower effective doses
  • Better bioavailability than modafinil
  • Improved water solubility over modafinil
Development Stage
Patent Status
  • U.S. Patent Filed: U.S. Patent Application Number 14/772,486, Filed 03 Sep 2015
  • Foreign Filed: - Patent Application
Related Technologies
  • E-251-2002
Wednesday, December 20, 2017