674475-59-3Relevant academic research and scientific papers
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety
Ross, Tina Morgan,Battista, Kathleen,Bignan, Gilles C.,Brenneman, Doug E.,Connolly, Peter J.,Liu, Jingchun,Middleton, Steven A.,Orsini, Michael,Reitz, Allen B.,Rosenthal, Dan I.,Scott, Malcolm K.,Vaidya, Anil H.
supporting information, p. 602 - 606 (2015/01/30)
Small molecule (1) has been identified as a selective partial agonist of Opioid Receptor Like-1 (ORL-1) with potential utility for the treatment of anxiety and other disorders. Nociceptin (orphanin FQ) is an endogenous peptide ligand that binds to ORL-1, however it does not bind the classical δ, μ and κ opioid receptors with high affinity. The synthesis of 1 involved using a molecular diversity approach, to rapidly advance a library of compounds for biological testing. A lead selective potent partial agonist (35-fold ORL-1/Mu) progressed to ORL-1 (NOP or OP4) proof of concept testing in advanced studies. The synthetic approach and biological data for the related chemical series will be presented.
HYDROXY ALKYL SUBSTITUTED 1,3,8-TRIAZASPIRO[4.5]DECAN-4-ONE DERIVATIVES USEFUL FOR THE TREATMENT OF ORL-1 RECEPTOR MEDIATED DISORDERS
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Page 138, (2008/06/13)
The present invention is directed to novel hydroxy alkyl substituted 1, 3, 8-triazaspiro[4.5]decan-4-one derivatives of the general formula: wherein all variables are as defined herein, useful in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. More particularly, the compounds of the present invention are useful in the treatment of disorders and conditions such as anxiety, depression, panic, dementia, mania, bipolar disorder, substance abuse, neuropathic pain, acute pain, chronic pain migraine, asthma, cough, psychosis, schizophrenia, epilepsy, hypertension, obesity, eating disorders, cravings, diabetes, cardiac arrhythmia, irritable bowel syndrome, Crohn's disease, urinary incontinence, adrenal disorders, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), Alzheimer's disease, for improved cognition or memory and for mood stabilization.
