US4091088A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Phenolic amino-carboxylic acid complexes for forming radiopharmaceuticals
Assignee: Australian Atomic Energy Commission
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Filing: 1976-09-30
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Granted: 1978-05-23
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Expires: 1996-09-30
Abstract
Abstract A complex of a chelating agent is formed and labelled with technetium-99m. The chelating agent is either an ethylenediamine carboxylic acid or its salt having a phenolic group at each end of the molecule such as EDDHA and HBED or alternatively the phenolic amino carboxylic acid or its salt having a single phenolate group such as HBG or HBS. The complex is a stannous complex which when labelled with technetium-99m has a good balance of lipo-solubility and waater-solubility to permit hepato-biliary imaging. The radiopharmaceutical may be useful for assessing hepatobiliary function in animals including human beings. A particularly useful chelating agent is ethylene-bis-(α-imino-2-hydroxy-5-bromophenyl acetic acid).
Inventors
- 👤 Frederick Charles Hunt
- 👤 John Gerald Wilson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 21:15
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K2121/00; A61K2123/00
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
57 words
A reagent which is adapted to be labelled with technetium-99m for use as a hepato-biliary imaging radiopharmaceutical for use on an animal, the reagent comprising a stannous complex of a phenolic aminocarboxylic acid chelating agent selected from the group consisting of an ethylene diamine di(hydroxy phenyl carboxylic acid) and a di (hydroxy benzyl) ethylene diamine dicarboxylic acid.
Claim 2
Dependent Claim
57 words
A reagent which is adapted to be labelled with technetium-99m for use as a hepato-biliary imaging radiopharmaceutical for use on an animal, the reagent comprising a stannous complex of a phenolic aminocarboxylic acid chelating agent selected from the group consisting of an ethylene diamine di(hydroxy phenyl carboxylic acid) and a di (hydroxy benzyl) ethylene diamine dicarboxylic acid.
Claim 3
Dependent Claim
41 words
A reagent as claimed in claim 1, wherein said chelating agent is selected from the group consisting of ##STR5## wherein X is hydrogen, a halogen or an alkyl group and ##STR6## wherein X is hydrogen, a halogen or an alkyl group.
Claim 4
Dependent Claim
49 words
A reagent which is adapted to be labelled with technetium-99m for use as a hepato-biliary imaging radiopharmaceutical for use on an animal, the reagent comprising a stannous complex of a phenolic aminocarboxylic acid chelating agent containing a single phenolic group, having a balance of both lipo-soluble and water-soluble properties.
Claim 5
Dependent Claim
49 words
A reagent which is adapted to be labelled with technetium-99m for use as a hepato-biliary imaging radiopharmaceutical for use on an animal, the reagent comprising a stannous complex of a phenolic aminocarboxylic acid chelating agent containing a single phenolic group, having a balance of both lipo-soluble and water-soluble properties.
Claim 6
Dependent Claim
23 words
A reagent as claimed in claim 3, wherein said chelating agent is selected from the group consisting of hydroxybenzyl glycine and hydroxybenzyl sarcosine.
Claim 7
Dependent Claim
19 words
A reagent as claimed in claim 4, wherein said phenolic aminocarboxylic acid has lipo-solubilizing substituents in the phenolic ring.
Claim 8
Dependent Claim
14 words
A reagent as claimed in claim 5, wherein said lipo-solubilising substituent is a halogen.
Claim 9
Dependent Claim
18 words
A reagent as claimed in claim 2, wherein the reagent is a stannous chelate of ethylene-bis-(α-imino-2-hydroxy-5-bromophenyl acetic acid).
Claim 10
Dependent Claim
19 words
A reagent as claimed in claim 2, wherein the reagent is a stannous chelate of N,N'-bis-(2-hydroxy-5-bromobenzyl ethylenediamine diacetic acid).
Claim 11
Dependent Claim
52 words
A reagent which is adapted to be labelled with technetium-99m for use as a hepato-biliary imaging radiopharmaceutical on an animal, the reagent being a stannous chelate of a chelating agent selected from the group consisting of hydroxybenzyl glycine and hydroxybenzyl sarcosine having lipo-solubilizing substituents in the phenolic ring and having aliphatic substituents.
Claim 12
Dependent Claim
52 words
A reagent which is adapted to be labelled with technetium-99m for use as a hepato-biliary imaging radiopharmaceutical on an animal, the reagent being a stannous chelate of a chelating agent selected from the group consisting of hydroxybenzyl glycine and hydroxybenzyl sarcosine having lipo-solubilizing substituents in the phenolic ring and having aliphatic substituents.
Claim 13
Dependent Claim
16 words
A reagent as claimed in claim 9, wherein said lipo-solubilising substituents are selected from the halogens.
Claim 14
Dependent Claim
16 words
A reagent as claimed in claim 4, wherein the reagent is a stannous chelate of N-(o-hydroxybenzyl)glycine.
Claim 15
Dependent Claim
16 words
A reagent as claimed in claim 4, wherein the reagent is a stannous chelate of N-(o-hydroxybenzyl)sarcosine.
Claim 16
Independent Claim
78 words
A method of forming radiopharmaceuticals for assessing hepato-biliary function in animals, comprising reacting a stannous chelate of a chelating agent selected from the group consisting of lipo-solubilizing ring substituted derivatives of ##STR7## wherein X is hydrogen, a halogen or an alkyl group, ##STR8## wherein X is hydrogen, a halogen or an alkyl group, (3) hydroxybenzyl glycine and (4) hydroxybenzyl sarcosine with a radio isotope selected from the group consisting of 111 In or 113m In and 99m Tc.
Claim 17
Independent Claim
78 words
A method of forming radiopharmaceuticals for assessing hepato-biliary function in animals, comprising reacting a stannous chelate of a chelating agent selected from the group consisting of lipo-solubilizing ring substituted derivatives of ##STR7## wherein X is hydrogen, a halogen or an alkyl group, ##STR8## wherein X is hydrogen, a halogen or an alkyl group, (3) hydroxybenzyl glycine and (4) hydroxybenzyl sarcosine with a radio isotope selected from the group consisting of 111 In or 113m In and 99m Tc.
Claim 18
Dependent Claim
34 words
A radiopharmaceutical for assessing hepato-biliary function comprising a lipo-soluble metal chelate in which the metal is a pharmaceutically acceptable radio isotope for an animal and the metal chelate is formed from ethylene-bis(α-imino-2-hydroxy-5-bromophenyl acetic acid).
Claim 19
Dependent Claim
34 words
A radiopharmaceutical for assessing hepato-biliary function comprising a lipo-soluble metal chelate in which the metal is a pharmaceutically acceptable radio isotope for an animal and the metal chelate is formed from ethylene-bis(α-imino-2-hydroxy-5-bromophenyl acetic acid).
Claim 20
Dependent Claim
67 words
A radiopharmaceutical for assessing hepato-biliary function comprising a lipo-soluble metal chelate in which the metal is a pharmaceutically acceptable radio isotope for an animal and the metal chelate is formed from a stannous complex of a chelating agent selected from the group consisting of ##STR9## wherein X is hydrogen, a halogen or an alkyl group and ##STR10## wherein X is hydrogen, a halogen or an alkyl group.
Claim 21
Dependent Claim
67 words
A radiopharmaceutical for assessing hepato-biliary function comprising a lipo-soluble metal chelate in which the metal is a pharmaceutically acceptable radio isotope for an animal and the metal chelate is formed from a stannous complex of a chelating agent selected from the group consisting of ##STR9## wherein X is hydrogen, a halogen or an alkyl group and ##STR10## wherein X is hydrogen, a halogen or an alkyl group.
References Cited (Backward Citations)
USRE23905E
Cited
US2624757A
Cited
FR1431697A
Cited
US3509208A
Cited
US3833590A
Cited
US3749556A
Cited
US3931396A
Cited
US3928552A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-05-22 | 1981-11-21 | 1982-05-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-05-22 | 1985-11-21 | 1986-05-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-05-22 | 1989-11-21 | 1990-05-23 | $7700.00 | Window Closed / Lapsed |