Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Amino acid sequence disclosed in whole or in part; or...
Patent
1981-07-17
1983-01-11
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Amino acid sequence disclosed in whole or in part; or...
A61U 3169
Patent
active
043681948
ABSTRACT:
The use of a mine boranes to inhibit the inflammation process is disclosed. hese boranes, which are boron analogs of .alpha.-amino acids, effectively block the following: general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain. The inflammation associated with pleurisy is also inhibited. The boron analogs are shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz., 10.sup.-6 M.
Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMN migration is unaltered at 10.sup.-4 M. The elevation of cyclic adenosine monophosphate in PMNs correlates positively with in vivo antiarthritic activity. Studies in rodents demonstrate that these boron analogs may be used at safe therapeutic doses. Several compounds per se are included within the scope of the invention.
REFERENCES:
Spielvogel, J.A.C.S. 98 pp. 5102-5103 (1976).
Surjit, J. Chem. Soc., D., p. 1619 (1970).
Wisean-Neilson, Inorg. Chem. 17, pp. 2327-2329 (1978).
Weedip, Inorg., Chem., 13, pp. 1763-1768 (1974).
Wilson "Textbook of Org. Med. & Pharm. Chem.", pp. 39-40 (1954).
Hall Iris H.
McPhail Andrew T.
Spielvogel Bernard F.
Friedman Stanley J.
Gapcynski William G.
Petruncio John M.
The United States of America as represented by the Secretary of
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