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Pharmaceutical composition and use

Patent 5317022 Issued on May 31, 1994. Estimated Expiration Date: Icon_subject October 2, 2012. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists
Patent #: 4760069
Issued on: 07/26/1988
Inventor: Rzeszotarski ,   et al.

Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists Patent #: 4889860
Issued on: 12/26/1989
Inventor: Rzeszotarski, et al.

Inventors

Assignee

Application

No. 934547 filed on 10/02/1992

US Classes:

514/282One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)

Examiners

Primary: Waddell, Frederick E.
Assistant: Hook, Gregory

Attorney, Agent or Firm

Foreign Patent References

  • 0077521 EP. 04/13/1983
  • 0242417 EP. 10/13/1987

International Class

A61K 031/114

Foreign Application Priority Data

1991-02-04 HU

Abstract

A 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

  • Receptor Binding and Analgesic Properties of Oxymorphazone, S. Galetta, et al., Life Sciences, (1983) vol. 31, pp.1389-1392
  • Long-Acting Opiate Agonists and Antagonists, G. W. Pasternak, Journal of Medicinal Chemistry (1980) vol. 23, No. 6, pp. 674-676
  • Classification of Opioid Receptors, S. J. Paterson, et al. British Medical Bulletin (1983), vol. 39, No. 1, pp. 31-36
  • Prolonged Receptor Blockade by Opioid Receptor Probes, A. Koman et al., Pharmaceutical Research (1986) vol. 3, No. 1, pp. 56-60
  • Synthesis and Binding of 3 H-Oxymorphazone to Rat Brain Membranes, E. Varga, et al., Life Sciences, vol. 40, pp. 1579-1588 (1987)
  • The Case for Multiple Opiate Receptors receptors R. S. Zukin, et al., TINS, May 19, 1984, pp. 160-164
  • Opiate and Analgesia: Evidence for Mediation by a Subpopulation of Opiate Receptors, Science (1980) vol. 208, pp. 514-516
  • Classification of Opioid Receptors, S. J. Paterson, et al., British Medical Bulletin (1983) vol. 39, No. 1 pp. 31-36
  • Naloxazone, a Long-Acting Opiate Antagonist: Effects on Analgesia in Intact Animals and on Opiate Receptor Bkinding in Vitro, G. W. Pasternak, et al., Journal of Pharmacology and Exper. Therap. (1980) vol. 214, No. 3, pp. 455-46
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