Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1992-01-17
1995-04-04
Rollins, John W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514579, 514663, 514673, 424 9, 424639, A61K 3113
Patent
active
054038626
ABSTRACT:
Several new powerful chelating agents, suitable for the removal of a variety of certain heavy metal ions from the body by oral application, have been synthesized and tested. Structurally, these compounds are partially lipophilic polyaminocarboxylic acids (PACA). They were synthesized in non-aqueous media from triethylenetetramine (TT) by monoalkylation of a primary amino group, followed by exhaustive carboxymethylation of the remaining amino groups using ethylbromoacetate and subsequent alkaline hydrolysis of the ester. Gel permeation chromatography of a mixture of the PACA and actinide elements have shown these substances to be strong chelating agents similar to EDTA or DTPA. In contrast to their non-lipophilic counterparts EDTA and DTPA, compositions of the present inventions exhibit appreciable absorption from the intestine and, therefore, can be administered orally. By varying the length of the alkyl chain, the chelons can be directed primarily to selected target organs. In addition, the compounds can be modified to target particular absorbed metals.
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Unpublished Annual Report of work in progress under U.S. Department of Energy Contract EY76C020119, Mar. 31, 1977, pp. 196 through 202.
Bruenger Friedrich W.
Miller Scott C.
Rollins John W.
University of Utah Research Foundation
Wilson James O.
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