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

Gut-selective opiates

Patent 4730048 Issued on March 8, 1988. Estimated Expiration Date: Icon_subject December 12, 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

3320262

Selective opioid receptor alkylating agents
Patent #: 4362870
Issued on: 12/07/1982
Inventor: Portoghese

Non-addictive narcotic antitussive preparation
Patent #: 4401672
Issued on: 08/30/1983
Inventor: Portoghese

Opiate agonists and antagonists Patent #: 4608376
Issued on: 08/26/1986
Inventor: Pasternak

Inventor

Assignee

Application

No. 06/809051 filed on 12/12/1985

US Classes:

546/45, Nitrogen or divalent chalcogen double bonded directly to carbocyclic ring of the pentacyclo ring system (e.g., morphinones, etc.)546/44, One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)546/46, A single chalcogen is bonded directly to ring carbon of the pentacyclo ring system (e.g., desoxy morphine, etc.)562/560, Ureido, hydrazino, or nitrogen double bonded directly to carbon562/565Polycarboxylic

Examiners

Primary: Daus, Donald G.
Assistant: Rivers, Diana G.

Attorney, Agent or Firm

International Classes

C07D 489/06 (20060101)
C07D 489/00 (20060101)

Abstract

Gut-selective agonist or antagonist opiates of the formula: ##STR1## wherein R is (C1 -C5)alkyl, C3 -C6 (cycloalkyl)alkyl, aryl, aralkyl or trans-(C2 -C5)alkenyl; Z is H or OH, R' is (C=O)-A(B)(C) wherein A is selected from the group consisting of (C1 -C5)alkyl, (C2 -C5)alkenyl and (C2 -C6)alkoxy (alkyl); B is selected from the group consisting of H, amino and a (C1 -C5)alkyl group optionally substituted with CO2 H, OH or phenyl and C is CO2 H, SO3 H, amino or guanidino; and R" is selected from the group consisting of NH-A(B)(C) or is guanidino; and the pharmaceutically-acceptable salts thereof.

Other References

  • D R. Brown et al., Neuropharmacology, 24, 181-191, (1985)
  • L. M. Sayre et al., J. Org. Chem., 45, 3366-68, (1980)
  • Bognar et al., Chemical Abstracts, vol. 71, 13243, (1969)
  • Jiang et al., Chemical Abstracts, vol. 87, 62629s, (1977)
  • Portoghese et al., Chemical Abstracts, vol. 90, 80864f, (1979)
  • Portoghese et al., Chemical Abstracts, vol. 92, 121619s, (1980)
  • Pasternak et al., Chemical Abstracts, vol. 93, 19120f, (1980)
  • Hahn et al., Chemical Abstracts, vol. 104, 102337y, (1986)
  • Remington's Pharmaceutical Sciences, A. Osol, ed., Mack Publishing Co., Easton, Pa., (16th ed., 1980), p. 395
  • Sigma Price List 1987, Sigma Chem. Co., St. Louis, Mo., pp. 197-200
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