Accession Number : ADD011303

Title :   Pharmacologically Active Amine Boranes.

Descriptive Note : Patent,


Personal Author(s) : Spielvogel,B F ; McPhail,A T ; Hall,I H

Report Date : 11 Jan 1983

Pagination or Media Count : 8

Abstract : The use of amine boranes to inhibit the inflammation process is disclosed. These 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 relase of lysosomal enzymes from liver and polymophonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz., .000001 M. Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMB migration is unaltered at .0001 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.

Descriptors :   *Patents, *Antiinflammatory agents, *Amines, *Boranes, Boron, Analogs, Amino acids, Inflammation, Arthritis, Pain, Inhibition, Respiratory diseases, Enzyme inhibitors, Prostaglandin, Synthesis, Oxidation, Phosphorylation, Polymorphonuclear neutrophils, Adenosine phosphates, Cyclic compounds, Interactions, Rodents, Test methods, Dosage

Subject Categories : Pharmacology

Distribution Statement : APPROVED FOR PUBLIC RELEASE