US4560548A
Expired / Lapsed
US
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Bone seeking Tc-99m complexes of phosphonate derivatives of bis(aminoalkyl)piperazine
Assignee: Dow Chemical Co
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Filing: 1984-04-10
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Granted: 1985-12-24
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Expires: 2004-04-10
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
2026-11-01 23:58
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.
References Cited (Backward Citations)
DE1518118A1
Cited
GB1081124A
Cited
US3989730A
Cited
US3852414A
Cited
US3851044A
Cited
US4016249A
Cited
US4082840A
Cited
US3983227A
Cited
US3931396A
Cited
US4032625A
Cited
US4075314A
Cited
US4187284A
Cited
US4234562A
Cited
US4387087A
Cited
US4385046A
Cited
USPTO Annuity & Maintenance Windows
| 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 |