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Title: Radionuclide-binding compound, a radionuclide delivery system, a method of making a radium complexing compound, a method of extracting a radionuclide, and a method of delivering a radionuclide

Patent ·
OSTI ID:873235
 [1];  [2];  [2]
  1. Richland, WA
  2. Moscow, ID
+ Show Author Affiliations

The invention pertains to compounds which specifically bind radionuclides, and to methods of making radionuclide complexing compounds. In one aspect, the invention includes a radionuclide delivery system comprising: a) a calix[n]arene-crown-[m]-ether compound, wherein n is an integer greater than 3, and wherein m is an integer greater than 3, the calix[n]arene-crown-[m]-ether compound comprising at least two ionizable groups; and b) an antibody attached to the calix[n]arene-crown-[m]-ether compound. In another aspect, the invention includes a method of making a radium complexing compound, comprising: a) providing a calix[n]arene compound, wherein n is an integer greater than 3, the calix[n]arene compound comprising n phenolic hydroxyl groups; b) providing a crown ether precursor, the crown ether precursor comprising a pair of tosylated ends; c) reacting the pair of tosylated ends with a pair of the phenolic hydroxyl groups to convert said pair of phenolic hydroxyl groups to ether linkages, the ether linkages connecting the crown ether precursor to the calix[n]arene to form a calix[n]arene-crown-[m]-ether compound, wherein m is an integer greater than 3; d) converting remaining phenolic hydroxyl groups to esters; e) converting the esters to acids, the acids being proximate a crown-[m]-ether portion of the calix[n]arene-crown-[m]-ether compound; and f) providing a Ra.sup.2+ ion within the crown-[m]-ether portion of the calix[n]arene-crown-[m]-ether compound.

Research Organization:
Battelle Memorial Institute, Columbus, OH (United States)
DOE Contract Number:
AC06-76RL01830
Assignee:
Battelle Memorial Institute (Richland, WA); Idaho Research Foundation, Inc. (Moscow, ID)
Patent Number(s):
US 6117413
OSTI ID:
873235
Country of Publication:
United States
Language:
English

References (9)

Selective Lower Rim Reactions of 5,17-Upper Rim-Disubstituted Calix[4]arenes 1 journal January 1996
Kinetics and Mechanism of the Sodium Cation Complexation by 5,11,17,23-Tetra-p-tert-butyl-25,26,27,28-tetramethoxycalix[4]arene in Solution journal August 1995
Synthesis and properties of calixcrown telomers journal January 1995
Crown ether derivatives of calix[5]arenes: synthesis and complexation properties journal January 1996
New metal cation-selective ionophores derived from calixarenes: their syntheses and ion-binding properties journal January 1986
The feasibility of 225 Ac as a source of ??-particles in radioimmunotherapy journal January 1993
Radionuclides for Radioimmunotherapy: Criteria for Selection journal July 1993
Selective 1,2-functionalization of calix[4]arenes at the lower rim. Synthesis of a new type of bis-calixcrown ether journal January 1990
Miniature Sodium-Selective Ion-Exchange Optode with Fluorescent pH Chromoionophores and Tunable Dynamic Range journal January 1996

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radionuclide-binding
compound
radionuclide
delivery
method
radium
complexing
extracting
delivering
pertains
compounds
specifically
bind
radionuclides
methods
aspect
comprising
calix
arene-crown-
-ether
integer
ionizable
antibody
attached
providing
arene
phenolic
hydroxyl
crown
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pair
tosylated
reacting
convert
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form
converting
remaining
esters
acids
proximate
crown-
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phenolic hydroxyl
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specifically bind
antibody attach
/424/999/