Patent ReferencesOximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists Patent #: 4889860 Inventors
AssigneeApplicationNo. 934547 filed on 10/02/1992US Classes:514/282One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)ExaminersPrimary: Waddell, Frederick E.Assistant: Hook, Gregory Attorney, Agent or FirmForeign Patent References
International ClassA61K 031/114Foreign Application Priority Data1991-02-04 HUAbstractA biologically active preparation for human or veterinary use for the selective blockade of opioid binding sites of the brain responsible for respiratory depression containing in a biologically active quantity the codeinone derivative of general formula (I) or its saltR1 means amino--, hydroxyl--, --NH--phenyl or --NH--CO--NH2 groups,R2 means a hydrogen atom or a hydroxyl group.The invention also covers a process for selective blocking the opioid binding sites of the brain responsible for respiratory depression by administering to a patient in need of an analgetic a preparation containing a codeinone derivative of general formula (I) or its salt preferably three times per day in doses of 2,5-5 mg.A preferred feature of the inventions is an analgetic composition containing a codeinone derivative of general formula (I) and in a mass ratio of 1 : 2-3 morphine of the formula (IV) or an other, biologically equipotent agonist type opiate or opioid compound and optionally inert, pharmaceutically acceptable accompanying materials.Other References
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