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Title	NOVEL COMPOUNDS THAT BIND SELECTIVITY TO THE OPIOID RECEPTOR FOR THERAPEUTIC APPLICATIONS
Case Number	00UMS044
Manager	Tamara Wilgers ( wilgerst@umsl.edu )
Abstract	Among the three classes of opioid receptors, delta, kappa, and mu, the delta-selective opioids offer prospects as powerful analgesics without the numerous negative side effects associated with traditional narcotics such as morphine (e.g., narcotic dependence and tolerance, severe constipation and respiratory depression). Moreover, antagonists of the delta-selective opioid can alleviate the behavioral effects of illicit drugs such as cocaine, thus being able to treat addiction to such drugs. Similarly, both delta opioid agonists and antagonists have been shown to accentuate the pain-killing effects and reduce the negative side effects of morphine and other mu opioids when administered concurrently. Researchers working at the University of Missouri-St. Louis discovered that certain triazole compounds (e.g., di- and tri-substituted triazole ring compounds) exhibit high binding affinity and high selectivity for opioid receptors and exhibit excellent bioavailability. These delta-selective opioids offer great potential across a wide range of pharmaceutical applications. POTENTIAL APPLICATIONS Delta-selective opioids are attractive candidates for a broad range of novel pharmaceutical applications: > Powerful, yet safe, analgesics > Treatment or prevention of opioid receptor related diseases and conditions such as pain, anxiety, obesity, depression or stress-related diseases > Agents for treating immune disorders > New treatments for drug addiction (e.g., cocaine, heroin, oxycodone) BENEFITS > Can provide a powerful, yet safe, analgesic to treat pain without the negative side effects of narcotics such as morphine (e.g., addiction, respiratory depression, physical dependence, gastrointestinal problems, memory problems, insomnia, etc.) > Compounds exhibit high binding affinity and high selectivity for the delta opioid receptors > Compounds exhibit excellent bioavailability MARKET The overall pain market in 2007 was estimated to be over $24 billion. The opioids portion of this market, according to Datamonitor, is set to grow from $9.6 billion in 2008 to $11.9 billion in 2018 across the seven major markets. INTELLECTUAL PROPERTY > Priority Date: 02/07/2002 > US Patent #7,045,520 entitled "OPIOID RECEPTOR ACTIVE COMPOUNDS" (issued 05/16/2006) > US Divisional Patent #7,294,720 entitled "OPIOID RECEPTOR ACTIVE COMPOUNDS" (issued 11/13/2007) > US Divisional Patent application #11/857,193 entitled "OPIOID RECEPTOR ACTIVE COMPOUNDS" (filed 09/18/2007) > PCT Patent application #PCT/US2003/03726 entitled "OPIOID RECEPTOR ACTIVE 4- (3-HYDROXYPHENYL) OR 4- (3-ALKOXYPHENYL) -1, 2, 4-TRIAZOLE COMPOUNDS" (filed 02/07/2003) > PCT National Stage applications filed in AU, BE, CA, CH, CZ, DE, EP, ES, FR, GB, IE, JP, MX, MX (divisional), NL, and TR. > Compounds exhibit high binding affinity and high selectivity for opioid receptors > Compounds exhibit excellent bioavailability INVENTORS: William J. Welsh, Seong Jae Yu, Anil Nair
Taxonomy	Technology Categories/Therapeutics/Medical
Keywords	UM-St. Louis, compounds, opioid, analgesics, umsl

Attachments

Name	Size	Description	Download
Opioid-Receptor-Active-Compounds_00UMS044.pdf	257299	Document Type: pdf Submitted by user: wilgerst Submitted on: 05/22/2009, 09:13:43 Business Opportunity Sheet 00UMS044 - Opioid Receptor Active Compounds	Download
Opioid-Receptor-Active-Compounds_00UMS044.pdf	257299	Document Type: pdf Submitted by user: wilgerst Submitted on: 08/14/2009, 15:36:32 00UMS044 Business Opportunity Sheet	Download

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