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Bone seeking Tc-99m complexes of phosphonate derivatives of bis(aminoalkyl)piperazine

Assignee: Dow Chemical Co
•
Filing: 1984-04-10
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Granted: 1985-12-24
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Expires: 2004-04-10
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Abstract

Abstract Radionuclide complexes of phosphonate derivatives of bis(aminoalkyl)piperazine have been found which are useful for imaging and/or treating therapeutically the skeletal system to detect and treat bone tumors. These complexes clear readily through the kidneys and the ratio of uptake in bone to that in surrounding soft tissue is high.

Inventors

  • 👤 Jaime Simon
  • 👤 David A. Wilson
  • 👤 Wynn A. Volkert
  • 👤 Druce K. Crump

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 19:44
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0489; A61K51/0474; A61K51/0478; C; C07; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/645; C07F9/6509; C07F9/650952; A61K2123/00

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 106 words
A bone seeking complex of a radioactive nuclide and a compound having the structural formula ##STR2## wherein n is 2 or 3 and wherein substituents A, B, X and Y each are independently selected from radicals consisting of hydrogen, hydroxyalkyl (wherein the alkyl group contains 2-6 carbon atoms), methylenephosphonic, methylene-, ethylene- and propylenesulfonic, hydroxymethyl-, hydroxyethyl- and hydroxypropylsulfonic acid radicals, carboxylic acid radicals (having 2-4 carbon atoms) and the alkali or alkaline earth metal, ammonium and amine salts of any of said phosphonic, sulfonic or carboxylic acid derivatives and wherein at least one of A, B, X and Y is a methylenephosphonic acid radical or salt thereof.
Claim 2
Dependent Claim 106 words
A bone seeking complex of a radioactive nuclide and a compound having the structural formula ##STR2## wherein n is 2 or 3 and wherein substituents A, B, X and Y each are independently selected from radicals consisting of hydrogen, hydroxyalkyl (wherein the alkyl group contains 2-6 carbon atoms), methylenephosphonic, methylene-, ethylene- and propylenesulfonic, hydroxymethyl-, hydroxyethyl- and hydroxypropylsulfonic acid radicals, carboxylic acid radicals (having 2-4 carbon atoms) and the alkali or alkaline earth metal, ammonium and amine salts of any of said phosphonic, sulfonic or carboxylic acid derivatives and wherein at least one of A, B, X and Y is a methylenephosphonic acid radical or salt thereof.
Claim 3
Dependent Claim 20 words
The complex of claim 1 wherein each of A, B, X and Y are methylenephosphonic acid radicals or salts thereof.
Claim 4
Dependent Claim 11 words
The complex of claim 1 wherein the radioactive nuclide is Technetium-99m.
Claim 5
Dependent Claim 11 words
The complex of claim 2 wherein the radioactive nuclide is Technetium-99m.
Claim 6
Dependent Claim 16 words
A composition comprising the complex of claim 3 and a reducing agent in a saline solution.
Claim 7
Dependent Claim 16 words
A composition comprising the complex of claim 4 and a reducing agent in a saline solution.
Claim 8
Dependent Claim 13 words
The composition of claim 5 wherein the reducing agent is Sn 2+ .
Claim 9
Dependent Claim 13 words
The composition of claim 6 wherein the reducing agent is Sn 2+ .
Claim 10
Dependent Claim 13 words
The composition of claim 1 wherein the radioactive nuclide is a particle emitter.
Claim 11
Dependent Claim 13 words
The composition of claim 2 wherein the radioactive nuclide is a particle emitter.
Claim 12
Dependent Claim 10 words
The composition of claim 9 wherein the radionuclide is Re-186.
Claim 13
Dependent Claim 10 words
The composition of claim 10 wherein the radionuclide is Re-186.
Claim 14
Dependent Claim 16 words
A composition comprising the complex of claim 11 and a reducing agent in a saline solution.
Claim 15
Dependent Claim 16 words
A composition comprising the complex of claim 12 and a reducing agent in a saline solution.
Claim 16
Dependent Claim 12 words
The composition of claim 13 wherein Sn 2+ is the reducing agent.
Claim 17
Dependent Claim 12 words
The composition of claim 14 wherein Sn 2+ is the reducing agent.
Claim 18
Dependent Claim 18 words
The composition of claim 9 wherein the radionuclide is one of the lanthanide series of the periodic table.
Claim 19
Dependent Claim 18 words
The composition of claim 10 wherein the radionuclide is one of the lanthanide series of the periodic table.
Claim 20
Dependent Claim 121 words
In a process in which the skeletal system is imaged with a complex of a radionuclide the improvement which comprises employing as the complexing agent a compound having the formula ##STR3## wherein n is 2 or 3 and wherein substituents A, B, X and Y each are independently selected from radicals consisting of hydrogen, hydroxyalkyl (wherein the alkyl group contains 2-6 carbon atoms), methylenephosphonic, methylene-, ethylene- and propylenesulfonic, hydroxymethyl-, hydroxyethyl- and hydroxypropylsulfonic acid radicals, carboxylic acid radicals (having 2-4 carbon atoms) and the alkali or alkaline earth metal, ammonium and amine salts of any of the phosphonic, sulfonic or carboxylic acid derivatives and wherein at least one of A, B, X and Y is a methylenephosphonic acid radical or salt thereof.
Claim 21
Dependent Claim 121 words
In a process in which the skeletal system is imaged with a complex of a radionuclide the improvement which comprises employing as the complexing agent a compound having the formula ##STR3## wherein n is 2 or 3 and wherein substituents A, B, X and Y each are independently selected from radicals consisting of hydrogen, hydroxyalkyl (wherein the alkyl group contains 2-6 carbon atoms), methylenephosphonic, methylene-, ethylene- and propylenesulfonic, hydroxymethyl-, hydroxyethyl- and hydroxypropylsulfonic acid radicals, carboxylic acid radicals (having 2-4 carbon atoms) and the alkali or alkaline earth metal, ammonium and amine salts of any of the phosphonic, sulfonic or carboxylic acid derivatives and wherein at least one of A, B, X and Y is a methylenephosphonic acid radical or salt thereof.
Claim 22
Dependent Claim 22 words
The process of claim 19 wherein each of A, B, X and Y is a methylenephosphonic acid radical or a salt thereof.

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Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-12-23 1989-06-24 1989-12-24 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-12-23 1993-06-24 1993-12-24 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-12-23 1997-06-24 1997-12-24 $7700.00 Window Closed / Lapsed

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