Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1981-02-23
1985-07-09
Reamer, James H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
560 39, C07C10130, C07C 3124
Patent
active
045281963
ABSTRACT:
The present invention consists of chelating agents for the treatment of iron overload and methods of using these agents in mammals such as mice and rats. These agents or compositions comprise diesters of dicarboxylic acids, which are phenolic derived and otherwise resemble ethylene and propylenediamine diacetic acids.
The acids are known as: HBED [N,N'-bis(2-hydroxybenzyl)ethylenediamine N,N-diacetic acid]; EHPG [ethylenediamine N,N'-bis(2-hydroxyphenylacetic acid)]; HBPD [N,N'- bis(2-hydoxybenzyl)propylenediamine-N,N'-diacetic acid]; HBHPD [N,N'- bis(2-hydroxybenzyl)-2-hydroxy-1,3-propylenediamine-N,N'-diacetic acid].
Mineral acid addition salts are also included in the spirit of this invention. Such salts as sulfuric, hydrochloric and nitric may be utilized.
In activity it has been found that the odd-numbered carbon atom esters, such a dimethyl and dipentyl, specially of HBED, are of highest activity, as well as the dipentyl ester of the HBPD. In summation, the HBED esters were found to have the highest activity of those esters studied.
REFERENCES:
patent: 4069249 (1978-01-01), Gaudette et al.
Pitt et al., J. Pharmacol. Exp. Ther., 208(1), pp. 12-18, (1979).
Reamer James H.
Roberts, Jr. John S.
The United States of America as represented by the Department of
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