EP0164843A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Organic amine phosphonic acid complexes for the treatment of calcific tumors
Assignee: Dow Chemical Co
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Filing: 1985-04-15
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Granted: —
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Expires: 2005-04-15
Abstract
Abstract Particle-emitting radionuclides, eg. Samarium-153, 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
2026-11-04 12:55
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K51/0489; A61P; A61P35/00; C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3808; C07F9/3817; A61K2121/00
Claims Analysis
Total Claims: 31
Claim 1
Independent Claim
54 words
A therapeutically effective complex of a paticle-emitting radionuclide which is gadolinium-159 (Gd-159), holmium-166 (Ho-166), lutetium-177 (Lu-177), samarium-153 (Sm-153) or ytterbium-175 (Yb-175) with an aminophosphonic acid derivative which is ethylenediaminetetramethylenephosphonic 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
54 words
A therapeutically effective complex of a paticle-emitting radionuclide which is gadolinium-159 (Gd-159), holmium-166 (Ho-166), lutetium-177 (Lu-177), samarium-153 (Sm-153) or ytterbium-175 (Yb-175) with an aminophosphonic acid derivative which is ethylenediaminetetramethylenephosphonic 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
18 words
A complex as claimed in Claim 1, characterized in that said radionuclide is Gd-159, Lu-177, Sm-153 and Yb-175.
Claim 4
Dependent Claim
23 words
A complex as claimed in Claim 2, characterized in that said radionuclide is selected from the group consisting of Lu-177, Sm-153 or Yb-175.
Claim 5
Dependent Claim
14 words
A complex as claimed in Claim 3, characterized in that said radionuclide is Sm-153.
Claim 6
Dependent Claim
14 words
A complex as claimed in Claim 3, characterized in that said radionuclide is Lu-177.
Claim 7
Dependent Claim
14 words
A complex as claimed in Claim 3, characterized in that said radionuclide is Yb-175.
Claim 8
Dependent Claim
15 words
7 . A complex as claimed in Claim 2, characterized in said radionuclide is Gd-159.
Claim 9
Dependent Claim
23 words
A complex as claimed in any one of Claims 1 to 7, characterized in that said 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 said 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 said 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 nitri-lotrimethylenephosphonic acid (NTMP).
Claim 13
Dependent Claim
24 words
A complex as claimed in any one of Claims 1 to 7, characterized in that said aminophosphonic acid derivative is tris(2-aminoethyl) aminehexamethylenephosphonic acid (TTHMP).
Claim 14
Dependent Claim
43 words
A process for the preparation of a therapeutically effective complex as claimed in Claim 1, characterized in that a radionuclide which is Gd-159, Ho-166, Lu-177, Sm-153, or Yb-175 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
22 words
A process-as claimed in any one of Claims 13 to 16, characterized in that said radionuclide is Gd-159, Lu-177, Sm-153 or Yb-175.
Claim 19
Dependent Claim
17 words
A process as claimed in Claim 17, characterized in that said radionuclide is Lu-177, Sm-153 or Yb-175.
Claim 20
Dependent Claim
13 words
A process as claimed in Claim 18, characterized in that'said radionuclide is Sm-153.
Claim 21
Dependent Claim
14 words
A process as claimed in Claim 18, characterized in that said radionuclide is Lu-177.
Claim 22
Dependent Claim
14 words
A process as claimed in Claim 18, characterized in that said radionuclide is Yb-175.
Claim 23
Dependent Claim
14 words
A process as claimed in Claim 17, charaterized in that said radionuclide is Gd-159.
Claim 24
Dependent Claim
20 words
A-process as claimed in any one of Claims 13 to 22, characterized in that said aminophosphonic acid derivative is EDTMP.
Claim 25
Dependent Claim
21 words
A process as claimed in any one of Claims 13 to 22, characterized in that said aminophosphonic acid derivative is DTPMP.
Claim 26
Dependent Claim
21 words
A process as claimed in any one of Claims -13 to 22, characterized in that said aminophosphonic acid derivative is HEEDTMP.
Claim 27
Dependent Claim
21 words
A process as claimed in any one of Claims 13 to 22, characterized in that said aminophosphonic acid derivative is NTMP.
Claim 28
Dependent Claim
21 words
A process as claimed in any one of Claims 13 to 22, characterized in that said aminophosphonic acid derivative is TTHMP.
Claim 29
Dependent Claim
33 words
A process as claimed in any one of Claims 13 to 28, characterized in that said aminophosphonic and said radionuclide acid derivative are contacted in a molar ratio of from 0.1:1 to 3000:1.
Claim 30
Dependent Claim
19 words
A complex as claimed in any one of Claims 1 to 12, for use in the treatment of cancer.
Claim 31
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)
No citation records indexed.
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