Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-04-03
2004-02-03
Rotman, Alan L. (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C546S224000
Reexamination Certificate
active
06686377
ABSTRACT:
BACKGROUND OF THE INVENTION
Fentanyl is an opioid analgesic that is roughly one-hundred fold more potent than morphine. Chemically, it is a 1,4-disubstituted piperidine molecule with agonist properties at the &mgr;-opioid receptor. This type of receptor is found in the brain as well as in various peripheral tissues and in the spinal chord. A transdermal delivery system for fentanyl has been described. This system delivers fentanyl at rates between 25 and 100 &mgr;g/hour. Due to severe side effects, the fentanyl transdermal system described in the art is indicated only in the management of chronic pain in patients requiring continuous opioid analgesia for pain that cannot be managed by lesser means. Because serious or life-threatening hypoventilation could occur, the use of fentanyl transdermal treatment is strongly contraindicated in children younger than 12 years of age, in the management of acute or post-operative pain, including use in outpatient surgery, and in general in any situation where pain can be managed by non-opioid therapy.
The development of a short-acting transdermal fentanyl analog system would be of great value. A soft fentanyl analog has been described in the art. Remifentanyl (Ultiva®) is marketed by Glaxo Wellcome as an ultrashort acting opioid for intravenous analgesia in anaesthetic cocktails. Due to its high degree of efficiency against extreme pain, a safe soft analog of fentanyl could be used in cases of pain management that are not presently suitable for the current opioid therapy.
BRIEF SUMMARY OF THE INVENTION
The subject invention provides novel analogs of fentanyl opioids. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention to a person in need of such treatment.
REFERENCES:
patent: 0 383 579 (1990-08-01), None
Lutz et al, Chemical Abstract, vol. 122 No. 23235, “A pharmacodynamic model to investigate the structur-activity profile of a series of novel opioid analgesics”, (1994).*
James et al, Journal of Pharmacology an Experimental Therapeutics, vol. 259 No. 2 pp 712-718 “Opioid receptor activity of G 87084B” (1991).*
Feldman, P., et al., “Design, Synthesis, and Pharmacological Evaluation of Ultrashort- to Long-Acting Opioid Analgetics”,Journal of Medicinal Chemistry,1991, pp. 2202-2208, vol. 34, No. 7, American Chemical Society.
Database CA [Online] Chemical Abstracts Service, Columbus, Ohio, US; Yang, Yulong et al.: “Anesthetic effect of some 4-substituted fentanyl derivatives in mice” retrieved from STN Database accession No. 130:32672 (abstract) & Huaxi Yaoxue Zazhi (1998), 13(2), 80-82 (abstract).
Lutz, M. et al. (1994) “A pharmacodynamic model to investigate the structure-activity profile of a series of novel opioid analgesics”Journal of Pharmacology and Experimental Therapeutics271(2):795-803, abstract only.
ARYx Therapeutics
Covington Raymond
Rotman Alan L.
Saliwanchik Lloyd & Saliwanchik
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