EP0176288A1
Expired / Lapsed
EP
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Aminocarboxylic acid complexes for the treatment of calcific tumors
Assignee: Dow Chemical Co
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Filing: 1985-09-12
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Granted: —
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Expires: 2005-09-12
Abstract
Abstract Particle-emitting radionuclides, e.g. Samarium-153, are complexed with aminocarboxylic acid derivatives having at least one of the amine hydrogens replaced by a carboxyalkyl radical to provide complexes having log of stability constant (Log K) from 13 to 20. Physiologically acceptable salts of these complexes are also contemplated. The complexes are useful in the treatment of calcific tumors.
Inventors
- 👤 Jaime Simon
- 👤 David A. Wilson
- 👤 Wynn A. Volkert
- 👤 David E. Troutner
- 👤 William F. Goeckeler
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-04 07:54
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61P; A61P35/00; A61K2121/00
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
49 words
A therapeutically effective complex of a particle-emitting rare earth radionuclide with an organic aminocarboxylic acid derivative having at least one of the amine hydrogens replaced by a carboxyalkyl radical or a physiologically acceptable salt thereof wherein the log of the stability constant (Log K) is from 13 to 20.
Claim 2
Dependent Claim
49 words
A therapeutically effective complex of a particle-emitting rare earth radionuclide with an organic aminocarboxylic acid derivative having at least one of the amine hydrogens replaced by a carboxyalkyl radical or a physiologically acceptable salt thereof wherein the log of the stability constant (Log K) is from 13 to 20.
Claim 3
Dependent Claim
22 words
A complex as claimed in Claim 1, wherein the radionuclide is Gadolinium-159 (Gd-159), Holmium-166 (Ho-666), Lutetium-177 (Lu-177), Samarium-153 (Sm-153) or Ytterbium-175 (Yb-175).
Claim 4
Dependent Claim
20 words
A complex as claimed in Claim 1 or Claim 2, wherein said organic aminocarboxylic acid derivative is an ethylenediaminecarboxylic acid.
Claim 5
Dependent Claim
15 words
A complex as claimed in Claim 3, wherein said ethylenediaminecarboxylic acid is an ethylenediamineacetic acid.
Claim 6
Dependent Claim
14 words
A complex as claimed in Claim 4, wherein said ethylenediamineacetic acid is ethylenediaminetetraacetic acid.
Claim 7
Dependent Claim
31 words
A complex as claimed in Claim 4, wherein at least one of the amine hydrogens of said ethylenediamineacetic acid is replaced by a hydroxyalkyl :radical containing 2 or 3 carbon atoms.
Claim 8
Dependent Claim
14 words
A complex as claimed in Claim 6, wherein said ethylenediamineacetic acid is hydroxyethylethylenediaminetriacetic acid.
Claim 9
Dependent Claim
31 words
A complex as claimed in any one of Claims 1 to 7, wherein the said aminocarboxylic acid derivative is in the form of a physiologically acceptable salt of an alkali metal.
Claim 10
Dependent Claim
15 words
A complex as claimed in Claim 8, wherein the alkali metal is sodium or potassium.
Claim 11
Dependent Claim
28 words
A composition for the treatment of calcific tumors comprising a complex as claimed in any one of the preceding claims with a physiologically acceptable carrier or diluent therefor.
Claim 12
Dependent Claim
34 words
A composition as claimed in Claim 10 in unit dosage form, wherein each unit dose contains a therapeutic amount of said complex, said amount exceeding that required for use as a diagnostic skeletal agent.
Claim 13
Dependent Claim
58 words
A process for the preparation of a therapeutically effective complex as claimed in any one of Claims 1 to 9, wherein a rare earth radionuclide is contacted with an organic aminocarboxylic acid derivative having at least one of the amine hydrogens replaced by a carboxyalkyl radical in the presence of water at a pH from 5 to 11.
Claim 14
Dependent Claim
13 words
A process as claimed in Claim 12, wherein the aqueous mixture is heated.
Claim 15
Dependent Claim
22 words
A process as claimed in Claim 12 or Claim 13, wherein the pH of the complex is adjusted from 7 to 8.
Claim 16
Dependent Claim
32 words
A process as claimed in any one of Claims 12 to 14, wherein said organic aminocarboxylic acid derivative and said radionuclide are contacted in a molar ratio of from 0.1:1 to 3000:1.
Claim 17
Dependent Claim
20 words
A complex as defined in any one of Claims 1 to 9, for use in the treatment of calcific tumors.
Claim 18
Dependent Claim
27 words
The use of a complex as defined in any one of Claims 1 to 9 in the manufacture of a medicament for the treatment of calcific tumors.
References Cited (Backward Citations)
EP0083129A1
Cited
DE3401052A1
Cited
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