US4479930A
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Amines coupled wth dicyclic dianhydrides capable of being radiolabeled product
Assignee: University of Massachusetts System
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Filing: 1982-07-26
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Granted: 1984-10-30
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Expires: 2002-07-26
Abstract
Abstract A dicyclic dianhydride rapidly and efficiently couples with a broad variety of amines such as polypeptides and proteins in non-aqueous or aqueous media and then may be chelated with a wide choice of radioisotope metallic cations to yield a radio-labeled product that is stable in vivo. A simple 1-step synthesis of the coupled amine in aqueous solution of neutral pH is described which requires only a few minutes time and with little accompanying hydrolysis.
Inventors
- 👤 Donald J. Hnatowich
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 20:39
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/08; A61K51/10; A61K51/1093; A61K51/081; A61K51/088; A61K2121/00; A61K2123/00
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
65 words
A chemical composition comprising: a primary or secondary amine comprising at least one amine group available for bonding as an amide bond; a radioactive metallic cation; and a chelating agent derived from a compound of the formula ##STR3## wherein R is a linking moiety containing between 1 and 25 carbon atoms, said chelating agent being bound to said amine group and to said metallic cation.
Claim 2
Dependent Claim
65 words
A chemical composition comprising: a primary or secondary amine comprising at least one amine group available for bonding as an amide bond; a radioactive metallic cation; and a chelating agent derived from a compound of the formula ##STR3## wherein R is a linking moiety containing between 1 and 25 carbon atoms, said chelating agent being bound to said amine group and to said metallic cation.
Claim 3
Dependent Claim
17 words
A chemical composition of claim 1 wherein said chelating agent is the dicyclic dianhydride of diethylenetriaminepentaacetic acid.
Claim 4
Dependent Claim
17 words
A chemical composition of claim 1 wherein said chelating agent is the dicyclic dianhydride of ethylenediaminetetraacetic acid.
Claim 5
Dependent Claim
24 words
The composition of claim 1, 2 or 3 wherein the radioactive metallic cation is selected from the group consisting of gallium-67, indium-111 and technetium-99m.
Claim 6
Dependent Claim
15 words
The composition of claim 1, 2 or 3 wherein the amine comprises a polypeptide chain.
Claim 7
Dependent Claim
14 words
The composition of claim 1, 2 or 3 wherein the amine comprises a protein.
Claim 8
Dependent Claim
75 words
A process for making a radionuclide labeled composition comprising the steps of: preparing a solid chelating agent having the formula ##STR4## wherein R is a linking moiety containing between 1 and 25 carbon atoms; mixing said solid chelating agent with a primary or secondary amine containing at least one amine group able to form an amide bond with said chelating agent; and adding a radioactive metallic cation to said conjugate to form a transcomplexed molecule.
Claim 9
Dependent Claim
75 words
A process for making a radionuclide labeled composition comprising the steps of: preparing a solid chelating agent having the formula ##STR4## wherein R is a linking moiety containing between 1 and 25 carbon atoms; mixing said solid chelating agent with a primary or secondary amine containing at least one amine group able to form an amide bond with said chelating agent; and adding a radioactive metallic cation to said conjugate to form a transcomplexed molecule.
Claim 10
Dependent Claim
31 words
The method as recited in claim 7 wherein said chelating agent is selected from the group consisting of the dicyclic dianhydride of diethylenetriaminepentaacetic acid and the dicyclic dianhydride of ethylenediaminetetraacetic acid.
Claim 11
Dependent Claim
22 words
The method as recited in claim 7 wherein said amine is selected from the group consisting of a polypeptide and a protein.
Claim 12
Dependent Claim
23 words
The method as recited in claim 7 wherein said radioactive metallic cation is selected from the group consisting of gallium-67, indium-111 and technetium-99m.
Claim 13
Dependent Claim
61 words
A chemical composition comprising: a primary or secondary amine comprising at least one amine group available for bonding as an amide bond; and a chelating agent derived from a compound of the formula ##STR5## wherein R is a linking moiety containing between 1 and 25 carbon atoms, said chelating agent being bound to said amine group and to said metallic cation.
Claim 14
Dependent Claim
61 words
A chemical composition comprising: a primary or secondary amine comprising at least one amine group available for bonding as an amide bond; and a chelating agent derived from a compound of the formula ##STR5## wherein R is a linking moiety containing between 1 and 25 carbon atoms, said chelating agent being bound to said amine group and to said metallic cation.
Claim 15
Dependent Claim
17 words
A chemical composition of claim 11 wherein said chelating agent is the dicyclic dianhydride of diethylenetriaminepentaacetic acid.
Claim 16
Dependent Claim
17 words
A chemical composition of claim 11 wherein said chelating agent is the dicyclic dianhydride of ethylenediaminetetraacetic acid.
Claim 17
Dependent Claim
17 words
The composition as recited in claim 1, 2 or 3 wherein the amine comprises a polypeptide chain.
Claim 18
Dependent Claim
16 words
The composition as recited in claim 1, 2 or 3 wherein the amine comprises a protein.
Claim 19
Dependent Claim
69 words
A process for making a radionuclide composition capable of chelating metal comprising the steps of: preparing a solid chelating agent derived from a compound having the formula ##STR6## wherein R is a linking moiety containing between 1 and 25 carbon atoms; and mixing said solid chelating agent with a primary or secondary amine containing at least one amine group able to form an amide bond with said chelating agent.
Claim 20
Dependent Claim
69 words
A process for making a radionuclide composition capable of chelating metal comprising the steps of: preparing a solid chelating agent derived from a compound having the formula ##STR6## wherein R is a linking moiety containing between 1 and 25 carbon atoms; and mixing said solid chelating agent with a primary or secondary amine containing at least one amine group able to form an amide bond with said chelating agent.
Claim 21
Dependent Claim
31 words
The method as recited in claim 16 wherein said chelating agent is selected from the group consisting of the dicyclic dianhydride of diethylenetriaminepentaacetic acid and the dicyclic dianhydride of ethylenediaminetetraacetic acid.
Claim 22
Dependent Claim
22 words
The method as recited in claim 16 wherein said amine is selected form the group consisting of a polypeptide and a protein.
References Cited (Backward Citations)
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1987-10-30 | 1988-04-30 | 1988-10-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-10-30 | 1992-04-30 | 1992-10-30 | $3760.00 | Window Closed / Lapsed |
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