U.S. patents available from 1976 to present.
U.S. patent applications available from 2005 to present.

Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists

Patent 4760069 Issued on July 26, 1988. Estimated Expiration Date: Icon_subject September 23, 2005. 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

3135758

3153042

3320262

Inventors

Assignee

Application

No. 06/778800 filed on 09/23/1985

US Classes:

514/282, One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)546/45Nitrogen or divalent chalcogen double bonded directly to carbocyclic ring of the pentacyclo ring system (e.g., morphinones, etc.)

Examiners

Primary: Rizzo, Nicholas S.
Assistant: Rivers, Diana G.

Attorney, Agent or Firm

International Classes

C07D 489/00 (20060101)
C07D 489/08 (20060101)

Abstract

A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a long-acting analgesic or opiate abuse treatment agent or appetite suppressant having the general formula: ##STR1## wherein R is methyl, cyclopropylmethyl or allyl, and R1 is an unsubstituted or substituted aryl, aralkyl, heteroaryl, heteroaralkyl or a cycloalkyl group with or without a heteroatom like S,O,N; and the pharmaceutically acceptable salts thereof.

Other References

  • Rapoport, et al., J. Organic Chem., vol. 15, pp. 1103-1106 (1950)
  • Bentley, "The Chemistry of the Morphine Alkaloids", Oxford (1954) pp. 180, 259
  • Sawa, et al., Tetrahedron, vol. 24, pp. 6185-6196 (1968)
  • Hahn, et al., J. Pharm. & Pharmacology, vol. 35(17), pp. 833-836 (12/83)
  • Ko, et al., J. Med. Chem., vol. 27(12), pp. 1727-1729 (12/84)
  • Koolpe, et al., J. Med. Chem., vol. 28(7), pp. 949-957 (7/85)
  • Mohamed, et al., Chemical Abstracts, vol. 104, 8886t (196)
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