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Method of treating abnormal concentrations of TNF ଱

Patent 5385901 Issued on January 31, 1995. 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

2830991

Inventors

Application

No. 955936 filed on 10/02/1992

US Classes:

514/231.5, Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding514/231.2, Morpholines (i.e., fully hydrogenated 1,4- oxazines)514/282, One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)514/327, Chalcogen bonded directly to ring carbon of the piperidine ring514/331, Nitrogen attached indirectly to the piperidine ring by nonionic bonding514/348Chalcogens bonded directly to at least two ring carbons of the six-membered hetero ring

Examiners

Primary: Henley, III, Raymond
Assistant: Criares, T. J.

Attorney, Agent or Firm

Foreign Patent References

  • 1185273 GB. 03/13/1970
  • WO92/09203 WO. 06/13/1992

International Classes

A61K 031/535
A61K 031/44
A61K 031/445

Abstract

Compounds of the structure ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl radicals of 1-6 carbon atoms, the phenyl radical, and the benzyl radical; and wherein R' is selected from the group consisting of the phthalimido radical and the succinimido radical and of the structure ##STR2## wherein X is CH2 or C=O; R" is H, --CH2 CH3, --C6 H5, --CH2 C6 H5, --CH2 CH=CH2, or ##STR3## and hydrolysis products of said compounds wherein R" is H and the piperidino ring or both the piperidino and the imido ring are hydrolyzed are useful for the control of abnormal concentrations of TNF ଱ manifested in septic shock, cachexia and HIV infection without substantially effecting the concentration of other cytokines.

Other References

  • Eger et al., "Synthesis, Central Nervous System Activity and Teratogenicity of a Homothalidomide", Arnzeim.-Forsch./Drug Research, 40 (II), No. 10, pp. 1073-1075 (1990)
  • Eriksson et al., "Synthesis and alkaline hydrolysis of some n-substituted phthalimides", Acta Pharm. Suecica, 10, pp. 63-74 (1973)
  • Fabro et al., "Teratogenic Activity Of Thalidomide And related Compounds", Life Sciences, vol. 3, pp. 987-992, Pergamon Press, Inc. (1964)
  • Fickentscher et al., "Stereochemical Properties and Teratogenic Activity of Some Tetrahydrophthalimides", Molecular Pharmacology, 13, pp. 133-141, Academic Press, Inc. (1977)
  • Flohe et al. "Studies on the Hypothetical Relationship of Thalidomide-induced Embryopathy and Collagen Biosynthesis", Arnzeim.-Forsch./Drug Research, 31 (I), No. 2, pp. 315-320 (1981)
  • Hendler, "The Oxygen Breakthrough", pp. 217-219, William Morrow and Company, New York (1989)
  • Hendler et al., "Thalidomide For Autoimmune Disease", Medical Hypotheses, 10, pp. 437-443 (1983)
  • Jonsson et al., "Chemical structure and teratogenic properties: I. Synthesis and teratogenic activity in rabbits of some derivatives of phthalimide, isoindoline-1-one, 1,2-benzisothiazoline-3-one-1,1-dioxide and 4(3H)-quinazolinone", Acta Pharm. Suecica, 9, pp. 431-446 (1972)
  • Jonsson, "Chemical structure and teratogenic properties: III. A review of available data on structure-activity relationships and mechanism of action of thalidomide analogues", Acta Pharm. Suecica, 9, pp. 521-542 (1972)
  • Jonsson, "Chemical structure and teratogenic properties: IV. An outline of a chemical hypothesis for the teratogenic action of thalidomide", Acta. Pharm. Suecica, 9, pp. 543-562 (1972)
  • Koch, "4 Thalidomide and Congeners as Anti-inflammatory Agents", Progress in Medical Chemistry, vol. 22, pp. 166-242, Elsevier Science Publishers, B.V. (Biomedical Division) (1985)
  • Matsuyama et al., "Cytokines and HIV infection: is AIDS a tumor necrosis factor disease?", AIDS 1991, vol. 5, No. 12, pp. 1405-1417 (1991)
  • Smith et al., "Studies on the Relationship Between the Chemical Structure and Embryotoxic Activity of Thalidomide and Related Compounds", Chemical Structure and Embryopathy, pp. 194-209 (1964
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