US4898724A
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US
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Organis amine phosphonic acid complexes for the treatment of calcific tumors
Assignee: Dow Chemical Co
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Filing: 1987-05-14
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Granted: 1990-02-06
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Expires: 2007-05-14
Abstract
Abstract Particle-emitting radionuclides, e.g. Samarium-153, have been complexed with organic aminoalkylenephosphonic acids wherein the nitrogen and phosphorus are interconnected by an alkylene group or substituted alkylene group. These complexes have been found useful in compositions for the therapeutic treatment of calcific tumors in animals.
Inventors
- 👤 Jaime Simon
- 👤 David A. Wilson
- 👤 Wynn A. Volkert
- 👤 David E. Troutner
- 👤 William F. Goeckeler
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 22:15
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3808; C07F9/3817; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0489; A61K2121/00
Claims Analysis
Total Claims: 34
Claim 1
Independent Claim
80 words
A composition comprising (1) a complex which comprises Sm-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic acid and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective.
Claim 2
Dependent Claim
80 words
A composition comprising (1) a complex which comprises Sm-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic acid and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective.
Claim 3
Dependent Claim
13 words
The composition of claim 1 wherein a physiologically acceptable liquid carrier is present.
Claim 4
Dependent Claim
29 words
The composition of claim 2 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
Claim 5
Dependent Claim
45 words
A composition comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective.
Claim 6
Dependent Claim
45 words
A composition comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective.
Claim 7
Dependent Claim
13 words
The composition of claim 4 wherein a physiologically acceptable liquid carrier is present.
Claim 8
Dependent Claim
29 words
The composition of claim 5 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
Claim 9
Independent Claim
98 words
A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises SM-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic acid and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 10
Independent Claim
98 words
A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises SM-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic acid and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 11
Dependent Claim
11 words
The method of claim 7, wherein the animal is a human.
Claim 12
Dependent Claim
13 words
The method of claim 7 wherein a physiologically acceptable liquid carrier is present.
Claim 13
Dependent Claim
29 words
The method of claim 9 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
Claim 14
Independent Claim
63 words
A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 15
Independent Claim
63 words
A method for the therapeutic treatment of an animal having one or more calcific tumors which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 16
Dependent Claim
11 words
The method of claim 11 wherein the animal is a human.
Claim 17
Dependent Claim
13 words
The method of claim 11 wherein a physiologically acceptable liquid carrier is present.
Claim 18
Dependent Claim
29 words
The method of claim 13 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
Claim 19
Dependent Claim
112 words
A sterile composition suitable for administration to a mammal comprising (1) a complex which comprises Sm-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic acid and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective and wherein the Sm-153 in dosage form is present in an amount containing at least 0.02 mCi per kilogram of body weight of said mammal.
Claim 20
Dependent Claim
112 words
A sterile composition suitable for administration to a mammal comprising (1) a complex which comprises Sm-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic acid and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex, and wherein the resulting composition is therapeutically effective and wherein the Sm-153 in dosage form is present in an amount containing at least 0.02 mCi per kilogram of body weight of said mammal.
Claim 21
Dependent Claim
13 words
The composition of claim 15 wherein a physiologically acceptable liquid carrier is present.
Claim 22
Dependent Claim
29 words
The composition of claim 16 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
Claim 23
Dependent Claim
78 words
A sterile composition suitable for administration to a mammal comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex, and where in the resulting composition is therapeutically effective and wherein the Sm-153 in dosage form is present in an amount containing at least 0.02 mCi per kilogram of body weight of said mammal.
Claim 24
Dependent Claim
78 words
A sterile composition suitable for administration to a mammal comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex, and where in the resulting composition is therapeutically effective and wherein the Sm-153 in dosage form is present in an amount containing at least 0.02 mCi per kilogram of body weight of said mammal.
Claim 25
Dependent Claim
13 words
The composition of claim 18 wherein a physiologically acceptable liquid carrier is present.
Claim 26
Dependent Claim
29 words
The composition of claim 19 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
Claim 27
Independent Claim
94 words
A method for the therapeutic treatment of an animal having bone pain which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises Sm-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 28
Independent Claim
94 words
A method for the therapeutic treatment of an animal having bone pain which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises Sm-153 and at least one of an aminophosphonic acid or a physiologically acceptable salt thereof wherein the aminophosphonic acid is selected from the group consisting of ethylenediaminetetramethylenephosphonic acid, diethylenetriaminepentamethylenephosphonic acid, hydroxyethylethylenediaminetrimethylenephosphonic acid, tris(2-aminoethyl)aminehexamethylenephosphonic acid, bis(aminoethyl)piperazinetetramethylenephosphonic acid, and (1-carboxy)ethylenediaminetetramethylenephosphonic and (2) at least one of the above aminophosphonic acids, or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 29
Dependent Claim
13 words
The method of claim 21 wherein a physiologically acceptable liquid carrier is present.
Claim 30
Dependent Claim
29 words
The method of claim 22 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
Claim 31
Independent Claim
60 words
A method for the therapeutic treatment of an animal having bone pain which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 32
Independent Claim
60 words
A method for the therapeutic treatment of an animal having bone pain which comprises administering to said animal a therapeutically effective amount of a composition comprising (1) a complex which comprises Sm-153 and ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof and (2) ethylenediaminetetramethylenephosphonic acid or a physiologically acceptable salt thereof, in excess of that required to make the complex.
Claim 33
Dependent Claim
13 words
The method of claim 24 wherein a physiologically acceptable liquid carrier is present.
Claim 34
Dependent Claim
29 words
The method of claim 25 wherein the physiologically acceptable liquid carrier is water and the resulting solution is adjusted to have a pH of about 7 to about 8.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-02-05 | 1993-08-07 | 1994-02-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-02-05 | 1997-08-07 | 1998-02-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-02-05 | 2001-08-07 | 2002-02-06 | $7700.00 | Window Closed / Lapsed |