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EP0225409A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Organic amine phosphonic acid complexes for the treatment of calcific tumors

Assignee: Dow Chemical Co
•
Filing: 1985-12-02
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Granted: —
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Expires: 2005-12-02
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Abstract

Abstract Particle-emitting radionuclides (Y-90 and In-115) have been complexed with phosphonic acid derivatives of organic amine or substituted organic amine compounds wherein the nitrogen and phosphorus are interconnected by an alkylene group. These complexes have been found useful in the treatment of calcific tumors in animals.

Inventors

  • 👤 Jaime Simon
  • 👤 Wynn A. Volkert
  • 👤 David A. Wilson
  • 👤 David E. Troutner
  • 👤 William F. Goeckeler

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-07 12:46
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0489; A61K51/0474; A61K51/0478; C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3808; C07F9/3817; A61K2121/00

Claims Analysis

Total Claims: 25
Claim 1
Independent Claim 46 words
A therapeutically effective complex of a paticle-emitting radionuclide of yttrium or indium with an aminophosphonic acid derivative which is ethylene- diaminetetramethylenephosphonic acid (EDTMP), diethylenetriaminepentamethylenephosphonic acid (DTPMP), hydroxyethylethylenediaminetrimethylene­phosphonic acid (HEEDTMP), nitrilotrimethylene­phosphonic acid (NTMP) or tris(2-aminoethyl) aminehexamethylenephosphonic acid (TTHMP) or a physiologically acceptable salt of such a complex.
Claim 2
Dependent Claim 46 words
A therapeutically effective complex of a paticle-emitting radionuclide of yttrium or indium with an aminophosphonic acid derivative which is ethylene- diaminetetramethylenephosphonic acid (EDTMP), diethylenetriaminepentamethylenephosphonic acid (DTPMP), hydroxyethylethylenediaminetrimethylene­phosphonic acid (HEEDTMP), nitrilotrimethylene­phosphonic acid (NTMP) or tris(2-aminoethyl) aminehexamethylenephosphonic acid (TTHMP) or a physiologically acceptable salt of such a complex.
Claim 3
Dependent Claim 14 words
A complex as claimed in Claim 1, characterized in that said radionuclide is Y-90.
Claim 4
Dependent Claim 14 words
A complex as claimed in Claim 1, characterized in that said radionuclide is In-115.
Claim 5
Dependent Claim 18 words
A complex as claimed any one of the preceding claims, which also comprises an additional rare earth radionuclide.
Claim 6
Dependent Claim 23 words
A complex as claimed in Claim 4, wherein the additional rare earth radionuclide is an isotope of gadolinium, holmium, lutetium, samarium or ytterbium.
Claim 7
Dependent Claim 25 words
A complex as claimed in Claim 5, wherein the additional rare earth radionuclide is gadolinium-159 (Gd-159), holmium-166 (Ho-166), lutetium-177 (Lu-177), samarium-153 (Sm-153) or ytterbium-175 (Yb-175).
Claim 8
Dependent Claim 13 words
A complex as claimed in Claim 6, wherein the additional radionuclide is Sm-153.
Claim 9
Dependent Claim 23 words
A complex as claimed in any one of Claims 1 to 7, characterized in that the aminophosphonic acid derivative is ethylenediaminetetramethylenephosphonic acid (EDTMP).
Claim 10
Dependent Claim 23 words
A complex as claimed in any one of Claims 1 to 7, characterized in that the aminophosphonic acid derivative is diethylenetriaminepentamethylene­phosphonic acid (DTPMP).
Claim 11
Dependent Claim 24 words
A complex as claimed in any one of Claims 1 to 7, characterized in that the aminophosphonic acid derivative is hydroxyethylethylenediaminetrimethylene phosphonic acid (HEEDTMP).
Claim 12
Dependent Claim 23 words
A complex as claimed in any one of Claims 1 to 7, characterized in that said aminophosphonic acid derivative is nitrilotrimethylenephosphonic acid (NTMP).
Claim 13
Dependent Claim 24 words
A complex as claimed in any one of Claims 1 to 7, characterized in that the aminophosphonic acid derivative is tris(2-aminoethyl) aminehexamethylene­phosphonic acid (TTHMP)>
Claim 14
Dependent Claim 40 words
A process for the preparation of a therapeutically effective complex as claimed in Claim 1, characterized in that a radionuclide which is Y-90 or In-115 is contacted with an aminophosphonic acid derivative which is EDTMP, DTPMP, HEEDTMP, NTMP or TTHMP.
Claim 15
Dependent Claim 27 words
A process as claimed in Claim 13, wherein the said contact is carried out in the presence of water at a pH of from 5 to 11.
Claim 16
Dependent Claim 20 words
A process as claimed in Claim 13 or Claim 14, wherein the said contact is carried out at elevated temperature.
Claim 17
Dependent Claim 27 words
A process as claimed in any one of Claims 13 to 15, including the step of adjusting the pH of the complex to from 7 to 8.
Claim 18
Dependent Claim 21 words
A process as claimed in any one of Claims 13 to 16, characterized in that said aminophosphonic acid derivative is EDTMP.
Claim 19
Dependent Claim 21 words
A process as claimed in any one of Claims 13 to 16, characterized in that the aminophosphonic acid derivative is DTPMP.
Claim 20
Dependent Claim 21 words
A process as claimed in any one of Claims 13 to 16, characterized in that the aminophosphonic acid derivative is HEEDTMP.
Claim 21
Dependent Claim 21 words
A process as claimed in any one of Claims 13 to 16, characterized in that the aminophosphonic acid derivative is NTMP.
Claim 22
Dependent Claim 21 words
A process as claimed in any one of Claims 13 to 16, characterized in that the aminophosphonic acid derivative is TTHMP.
Claim 23
Dependent Claim 33 words
A process as claimed in any one of Claims 13 to 16, characterized in that the aminophosphonic and said radionuclide acid derivative are contacted in a molar ratio of from 0.1:1 to 3000:1.
Claim 24
Dependent Claim 19 words
A complex as claimed in any one of Claims 1 to 12, for use in the treatment of cancer.
Claim 25
Dependent Claim 26 words
The use of a complex as claimed in any one of Claims 1 to 12, in the manufacture of a medicament for the treatment of cancer.

References Cited (Backward Citations)

EP0164843A2 Cited

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