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NOVEL COMPOUNDS THAT BIND SELECTIVITY TO THE OPIOID RECEPTOR FOR THERAPEUTIC APPLICATIONS

详细技术说明

None

*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 APPLICATIONSDelta-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 bioavailabilityMARKETThe 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)INVENTORS: William J. Welsh, Seong Jae Yu, Anil Nair

*Principal Investigation

Name: William Welsh

Department:

Name: Anil Nair, Senior Associate Scientist - Computational Chemistry

Department:

Name: Seong-Jae Yu

Department:

附加资料

Patent Number: US7776898B2
Application Number: US2007857193A
Inventor: Welsh, William J. | Yu, Seong Jae | Nair, Anil
Priority Date: 7 Feb 2002
Priority Number: US7776898B2
Application Date: 18 Sep 2007
Publication Date: 17 Aug 2010
IPC Current: A61K00314196 | A61P000102 | A61P000104 | A61P000304 | A61P000310 | A61P000706 | A61P000910 | A61P001102 | A61P001106 | A61P001108 | A61P001500 | A61P001702 | A61P001704 | A61P001706 | A61P001902 | A61P001906 | A61P002104 | A61P002500 | A61P002504 | A61P002506 | A61P002518 | A61P002522 | A61P002524 | A61P002528 | A61P002702 | A61P002900 | A61P003500 | A61P003702 | A61P004300 | C07D024908 | C07D024910 | C07D024914
US Class: 514383 | 5482622 | 5482648
Assignee Applicant: The Curators of the University of Missourilumbia
Title: Opioid receptor active compounds
Usefulness: Opioid receptor active compounds
Summary: (I) is used for the manufacture of a medicament useful for the treatment of pain (claimed), anxiety, obesity, depression, stress related disease, inflammation (e.g. in a disease like vascular disease, migraine headaches, periarteritis etc), headache, fever, arthritis (including rheumatoid arthritis, spondyloarthopathies, gouty arthritis, osteoarthritis, systemic lupus erythematosus and juvenile arthritis), asthma, bronchitis, menstrual cramps, tendonitis, bursitis, skin related conditions (e.g. psoriasis, eczema, burns and dermatitis), gastrointestinal conditions (e.g. inflammatory bowel disease, Crohn's disease, gastritis, irritable bowel syndrome and ulcerative colitis), cancer (e.g. colorectal cancer), ophthalmic disease (e.g. retinitis, retinopathies, conjunctivitis, uvetitis, ocular photophobia and acute injury to the eye tissue), pulmonary inflammation (such as that associated with viral infections and cystic fibrosis), central nervous system disorders (such as cortical dementias including Alzheimer's disease) and central nervous system damage (e.g. resulting from stroke, ischemia or trauma); for modifying the effects of other biologically active compounds (e.g. for treating narcotic addiction); for combating viral infections.
Novelty: New 4-(3-hydroxyphenyl) or 4-(3-alkoxyphenyl)-1,2,4-triazole compounds useful for treating e.g. pain, anxiety, obesity, depression

主要类别

诊断/治疗

细分类别

癌症/肿瘤

其他

国家/地区

美国