US4272503A
Expired / Lapsed
US
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Reductant composition for technetium-99m and method for making technetium-99m labelled ligands
Assignee: Bristol Myers Squibb Pharma Co
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Filing: 1978-05-25
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Granted: 1981-06-09
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Expires: 1998-05-25
Abstract
Abstract Reductant compositions for reducing technetium to produce technetium labelled ligands comprise a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state. Preferably the reducing complex comprises a reducing agent for technetium and a chelating ligand therefor. Technetium labelled ligands are prepared by mixing such ligands with pertechnetate in the presence of the reductant of this invention and separating the reductant from the resulting labelled ligand. Technetium labelled ligands that are substantially free from reducing agent used in their preparation may be made in this manner.
Inventors
- 👤 Leopoldo L. Camin
- 👤 Maria P. Liteplo
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 13:47
CPC Classifications
C; C01; C01G; C01G99/00; C01G99/006; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K51/12; A61K51/1282; A61K2123/00
Claims Analysis
Total Claims: 73
Claim 1
Independent Claim
45 words
A product for reducing technetium comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with a ligand to be labelled.
Claim 2
Dependent Claim
45 words
A product for reducing technetium comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with a ligand to be labelled.
Claim 3
Dependent Claim
24 words
The product of claim 1 wherein said reducing complex comprises a reducing agent and a ligand for binding said reducing agent to said substrate.
Claim 4
Dependent Claim
27 words
The product of claim 2 wherein said reducing agent is selected from the group consisting of stannous ions, ferrous ions, cuprous ions, ferric-ascorbate complexes, and reduced zirconium.
Claim 5
Dependent Claim
17 words
The product of claim 1 wherein said substrate is selected from glass and natural and synthetic polymers.
Claim 6
Dependent Claim
13 words
The product of claim 4 wherein substrate is in the form of particles.
Claim 7
Dependent Claim
15 words
The product of claim 4 wherein said substrate is the inside surface of a vial.
Claim 8
Dependent Claim
21 words
A product for reducing technetium comprising a substrate and a stannous reducing agent bound to the substrate by a chelating ligand.
Claim 9
Dependent Claim
21 words
A product for reducing technetium comprising a substrate and a stannous reducing agent bound to the substrate by a chelating ligand.
Claim 10
Dependent Claim
26 words
The product of claim 7 wherein said chelating ligand is selected from the group consisting of natural and synthetic hetero macrocyclic ligands and hetero polycyclic ligands.
Claim 11
Dependent Claim
21 words
The product of claim 8 wherein said chelating ligand comprises a hetero macrocyclic ligand having a 14 to 16 membered ring.
Claim 12
Dependent Claim
24 words
The product of claim 7 wherein said chelating ligand is a multifunctional compound comprising functional groups selected from --SH, --COOH, --NH 2 and --OH.
Claim 13
Dependent Claim
19 words
The product of claim 7 wherein said chelating ligand is selected from 8-hydroxyquinoline, dihydrolipoamide, aminodiacetic acid and ethylenediaminetriacetic acid.
Claim 14
Dependent Claim
17 words
The product of claim 7 wherein said substrate is selected from glass and natural and synthetic polymers.
Claim 15
Dependent Claim
15 words
The product of claim 7 wherein said substrate is a material having free hydroxy groups.
Claim 16
Dependent Claim
39 words
A product for reducing technetium to form radiolabelled ligands comprising a stannous reducing agent bound to a substrate selected from glass and natural and synthetic polymers by a chelating ligand selected from 8-hydroxyquinoline, dihydrolipoamide, iminiodiacetic acid and ethylenediaminetriacetic acid.
Claim 17
Dependent Claim
39 words
A product for reducing technetium to form radiolabelled ligands comprising a stannous reducing agent bound to a substrate selected from glass and natural and synthetic polymers by a chelating ligand selected from 8-hydroxyquinoline, dihydrolipoamide, iminiodiacetic acid and ethylenediaminetriacetic acid.
Claim 18
Dependent Claim
15 words
The product of claim 14 wherein said substrate is the inside surface of a vial.
Claim 19
Independent Claim
74 words
A method for preparing a technetium-99m labelled ligand comprising mixing the ligand to be labelled and pertechnetate in the presence of a reductant, said reductant comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with said ligand to be labelled, and separating said reductant from the technetium labelled ligand.
Claim 20
Independent Claim
74 words
A method for preparing a technetium-99m labelled ligand comprising mixing the ligand to be labelled and pertechnetate in the presence of a reductant, said reductant comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with said ligand to be labelled, and separating said reductant from the technetium labelled ligand.
Claim 21
Dependent Claim
43 words
The method of claim 16 wherein said ligand to be labelled is selected from plasma proteins, gamma globulin, albumin, antibodies and fractions thereof, phytate, fibrinogen, a diphosphonate, a phosphate, a polyamino poly carboxylic acid, gluconate, glucoheptonate, and N-(2,6-dimethylphenylcarbamolymethyl) iminodiacetic acid and its analogs.
Claim 22
Dependent Claim
25 words
The method of claim 16 wherein said reducing complex comprises a reducing agent and a chelating ligand for binding said reducing agent to said substrate.
Claim 23
Dependent Claim
28 words
The method of claim 18 wherein said reducing agent is selected from the group consisting of stannous ions, ferrous ions, cuprous ions, ferric ascorbate complexes, and reduced zirconium.
Claim 24
Dependent Claim
17 words
The method of claim 16 wherein said substrate is selected from glass and natural and synthetic polymers.
Claim 25
Dependent Claim
12 words
The method of claim 20 wherein said substrate is particulate in form.
Claim 26
Dependent Claim
14 words
The method of claim 20 wherein said substrate is the inside of a vial.
Claim 27
Independent Claim
46 words
A method for preparing a technetium-99m labelled ligand comprising mixing the ligand to be labelled and pertechnetate in the presence of a reductant, said reductant comprising stannous reducing agent bound to a substrate by a chelating ligand and separating said reductant from the technetium labelled ligand.
Claim 28
Independent Claim
46 words
A method for preparing a technetium-99m labelled ligand comprising mixing the ligand to be labelled and pertechnetate in the presence of a reductant, said reductant comprising stannous reducing agent bound to a substrate by a chelating ligand and separating said reductant from the technetium labelled ligand.
Claim 29
Dependent Claim
26 words
The method of claim 23 wherein said chelating ligand is selected from the group consisting of natural and synthetic hetero macrocyclic ligands and hetero polycyclic ligands.
Claim 30
Dependent Claim
21 words
The method of claim 24 wherein said chelating ligand comprises a hetero macrocyclic ligand having a 14 to 16 membered ring.
Claim 31
Dependent Claim
24 words
The method of claim 23 wherein said chelating ligand is a multifunctional compound comprising functional groups selected from --SH, --COOH, --NH 2 and --OH.
Claim 32
Dependent Claim
19 words
The method of claim 23 wherein said chelating ligand is selected from 8-hydroxyquinoline, dihydrolipoamide, iminodiacetic acid and ethylenediaminetriacetic acid.
Claim 33
Dependent Claim
17 words
The method of claim 23 wherein said substrate is selected from glass and natural and synthetic polymers.
Claim 34
Dependent Claim
15 words
The method of claim 23 wherein said substrate is a material having free hydroxy groups.
Claim 35
Independent Claim
64 words
A method for preparing a technetium-99m labelled ligand comprising mixing the ligand to be labelled and pertechnetate in the presence of a reductant, said reductant comprising a stannous reducing agent bound to a substrate selected from glass and natural and synthetic polymers by a chelating ligand selected from 8-hydroxyquinoline, dihydrolipoamine, aminodiacetic acid and ethylenediaminetriacetic acid, and separating said reductant from the technetium labelled ligand.
Claim 36
Independent Claim
64 words
A method for preparing a technetium-99m labelled ligand comprising mixing the ligand to be labelled and pertechnetate in the presence of a reductant, said reductant comprising a stannous reducing agent bound to a substrate selected from glass and natural and synthetic polymers by a chelating ligand selected from 8-hydroxyquinoline, dihydrolipoamine, aminodiacetic acid and ethylenediaminetriacetic acid, and separating said reductant from the technetium labelled ligand.
Claim 37
Dependent Claim
15 words
The method of claim 30 wherein said substrate is the inside surface of a vial.
Claim 38
Dependent Claim
22 words
A radiopharmaceutical composition comprising technetium-99m labelled ligand and a reducing agent in an amount less than 1.0 μg per ml of composition.
Claim 39
Dependent Claim
22 words
A radiopharmaceutical composition comprising technetium-99m labelled ligand and a reducing agent in an amount less than 1.0 μg per ml of composition.
Claim 40
Dependent Claim
24 words
The composition of claim 32 wherein said labelled ligand is selected from the group consisting of polyhydroxypolycarboxylic acids, aminocarboxylic acids, phosphonates, phosphates and mercaptans.
Claim 41
Dependent Claim
42 words
The composition of claim 33 wherein said labelled ligand is selected from plasma proteins, gamma globulin, albumin, antibodies and fractions thereof, phytate, fibrinogen, ethyhydroxydiphosphonate, methylenediphosphonate, pyrophosphate, ethylenediaminetetraacetic acid and derivatives thereof, diethylenetriaminepentaacetic acid, gluconate, glycoheptonate and N-(2,6-dimethylphenylcarbamoylmethyl) iminodiacetic acid and its analogs.
Claim 42
Dependent Claim
14 words
The composition of claim 32 wherein said composition is substantially free of reducing agent.
Claim 43
Dependent Claim
60 words
A container having therein a ligand to be labelled with technetium-99m for use as a radiopharmaceutical composition and a reductant comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with said ligand to be labelled.
Claim 44
Dependent Claim
60 words
A container having therein a ligand to be labelled with technetium-99m for use as a radiopharmaceutical composition and a reductant comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with said ligand to be labelled.
Claim 45
Dependent Claim
39 words
The container of claim 36 wherein said ligand to be labelled is selected from plasma proteins, gamma globulin, antibodies and fractions thereof, phytate, fibrinogen, ethylhydroxydiphosphonate, methylenediphosphonate, ethylenediaminetetraacetic acid, diethylenetriaminepentaacetic acid, gluconate, glucoheptonate and N-(2,6-dimethylphenylcarbamoylmethyl) iminodiacetic acid and its analogs.
Claim 46
Dependent Claim
25 words
The container of claim 36 wherein said reducing complex comprises a reducing agent and a chelating ligand for binding said reducing agent to said substrate.
Claim 47
Dependent Claim
27 words
The container of claim 38 wherein said reducing agent is selected from the group consisting of stannous ions, ferrous ions, cuprous ions, ferric-ascorbate complexes, and reduced zirconium.
Claim 48
Dependent Claim
17 words
The container of claim 36 wherein said substrate is selected from glass and natural and synthetic polymers.
Claim 49
Dependent Claim
16 words
The container of claim 40 wherein said substrate is in the form of particles or beads.
Claim 50
Dependent Claim
15 words
The container of claim 40 wherein said substrate is the inside surface of said container.
Claim 51
Dependent Claim
33 words
A container having therein a ligand to be labelled with technetium-99m for use as a radiopharmaceutical composition and a reductant comprising a stannous reducing agent bound to a substrate by a chelating ligand.
Claim 52
Dependent Claim
33 words
A container having therein a ligand to be labelled with technetium-99m for use as a radiopharmaceutical composition and a reductant comprising a stannous reducing agent bound to a substrate by a chelating ligand.
Claim 53
Dependent Claim
26 words
The container of claim 43 wherein said chelating ligand is selected from the group consisting of natural and synthetic hetero macrocyclic ligands and hetero polycyclic ligands.
Claim 54
Dependent Claim
24 words
The container of claim 43 wherein said chelating ligand is a multifunctional compound comprising functional groups selected from --SH, --COOH, --NH 2 and --OH.
Claim 55
Dependent Claim
19 words
The container of claim 43 wherein said chelating ligand is selected from 8-hydroxyquinoline, dihydrolipoamide, aminodiacetic acid and ethylenediaminetriacetic acid.
Claim 56
Dependent Claim
17 words
The container of claim 43 wherein said substrate is selected from glass and natural and synthetic polymers.
Claim 57
Dependent Claim
15 words
The container of claim 43 wherein said substrate is a material having free hydroxy groups.
Claim 58
Dependent Claim
50 words
A container having therein a ligand to be labelled with technetium-99m for use as a radiopharmaceutical composition and a reductant comprising a stannous reducing agent bound to a substrate selected from glass and natural and synthetic polymers by a chelating ligand selected from 8-hydroxyquinoline, dihydrolipoamide, aminodiacetic acid and ethylenediaminetriacetic acid.
Claim 59
Dependent Claim
50 words
A container having therein a ligand to be labelled with technetium-99m for use as a radiopharmaceutical composition and a reductant comprising a stannous reducing agent bound to a substrate selected from glass and natural and synthetic polymers by a chelating ligand selected from 8-hydroxyquinoline, dihydrolipoamide, aminodiacetic acid and ethylenediaminetriacetic acid.
Claim 60
Dependent Claim
15 words
The container of claim 49 wherein said substrate is the inside surface of said container
Claim 61
Dependent Claim
60 words
A product for reducing technetium comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with a ligand to be labelled, said substrate being sterile and inert under the conditions under which said product is used.
Claim 62
Dependent Claim
60 words
A product for reducing technetium comprising a substrate having attached thereto a reducing complex having sufficient redox potential to reduce technetium from the +7 oxidation state to an oxidation state at which said technetium forms a relatively stable complex with a ligand to be labelled, said substrate being sterile and inert under the conditions under which said product is used.
Claim 63
Dependent Claim
24 words
The product of claim 51 wherein said reducing complex comprises a reducing agent and a ligand for binding said reducing agent to said substrate.
Claim 64
Dependent Claim
27 words
The product of claim 52 wherein said reducing agent is selected from the group consisting of stannous ions, ferrous ions, cuprous ions, ferric-ascorbate complexes, and reduced zirconium.
Claim 65
Dependent Claim
10 words
The product of claim 51 wherein said substrate is glass.
Claim 66
Dependent Claim
14 words
The product of claim 54 wherein said substrate is in the form of particles.
Claim 67
Dependent Claim
15 words
The product of claim 54 wherein said substrate is the inside surface of a vial.
Claim 68
Dependent Claim
14 words
The product of claim 51 wherein said substrate is a natural or synthetic polymer.
Claim 69
Dependent Claim
22 words
The product of claim 51 wherein said reducing complex comprises a stannous reducing agent bound to the substrate by a chelating ligand.
Claim 70
Dependent Claim
24 words
The product of claim 58 wherein said chelating ligand is selected from the group consisting of natural and synthetic hetero-macrocyclic ligands and hetero-polycyclic ligands.
Claim 71
Dependent Claim
20 words
The product of claim 59 wherein said chelating ligand comprises a hetero-macrocyclic ligand having a 14 to 16 membered ring.
Claim 72
Dependent Claim
24 words
The product of claim 58 wherein said chelating ligand is a multifunctional compound comprising functional groups selected from --SH, --COOH, --NH 2 and --OH.
Claim 73
Dependent Claim
19 words
The product of claim 58 wherein said chelating ligand is selected from 8-hydroxyquinoline, dihydrolipoamide, aminodiacetic acid and ethylenediaminetriacetic acid.
References Cited (Backward Citations)
US3784453A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-06-08 | 1984-12-08 | 1985-06-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-06-08 | 1988-12-08 | 1989-06-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-06-08 | 1992-12-08 | 1993-06-09 | $7700.00 | Window Closed / Lapsed |