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US4574079A
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Radiolabeled angiotensin converting enzyme inhibitors for radiolabeling mammalian organ sites
Assignee: Boston University
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Filing: 1983-05-27
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Granted: 1986-03-04
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Expires: 2003-05-27
Abstract
Abstract Radiolabeled angiotensin converting enzyme inhibitors having the general formula: ##STR1## wherein X is a radiolabeling substituent, preferably a radiolabeling halogen substituent such as 123 I, 125 I, 131 I, 75 Br or 77 Br, Y is hydroxy, alkoxy containing from 1 to 6 carbon atoms, phenoxy, benzyloxy, or amino, R 1 is hydrogen or methyl, R 2 is hydrogen, an ester moiety hydrolyzable under mammalian in vivo conditions, such as alkyl of 1 or 2 carbon atoms, phenyl or benzyl, or an ionically bonded anion of a physiologically acceptable non-toxic salt, and m is an integer of from 1 to 6, are useful as in vivo radioimaging compounds for mammalian sites.
Inventors
- 👤 Haralambos P. Gavras
- 👤 James W. Ryan
- 👤 Alfred Chung
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 22:02
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/041; A61K51/044; A61K51/0468; A61K51/047; A61K2123/00
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
73 words
A radiolabeled angiotensin converting enzyme (ACE) inhibitor having the general formula: ##STR17## wherein X is a radiolabeling substituent, Y is hydroxy, alkoxy containing from 1 to 6 carbon atoms, phenoxy, benzyloxy or amino, R 1 is hydrogen or methyl, R 2 is hydrogen, an ester moiety hydrolyzable under mammalian in vivo conditions or an ionically bonded anion of a physiologically acceptable non-toxic salt, and m is an integer of from 1 to 6.
Claim 2
Dependent Claim
73 words
A radiolabeled angiotensin converting enzyme (ACE) inhibitor having the general formula: ##STR17## wherein X is a radiolabeling substituent, Y is hydroxy, alkoxy containing from 1 to 6 carbon atoms, phenoxy, benzyloxy or amino, R 1 is hydrogen or methyl, R 2 is hydrogen, an ester moiety hydrolyzable under mammalian in vivo conditions or an ionically bonded anion of a physiologically acceptable non-toxic salt, and m is an integer of from 1 to 6.
Claim 3
Dependent Claim
16 words
A radiolabeled ACE inhibitor as described in claim 1 wherein X is a radiolabeling halogen substituent.
Claim 4
Dependent Claim
23 words
A radiolabeled ACE inhibitor as described in claim 2 wherein X is 123 I, 125 I, 131 I, 75 Br or 77 Br.
Claim 5
Dependent Claim
16 words
A radiolabeled ACE inhibitor as described in claim 2 wherein X is a radiolabeling iodine substituent.
Claim 6
Dependent Claim
56 words
A radiolabeled ACE inhibitor having the general formula: ##STR18## wherein X' is a radiolabeling iodine substituent, R 1 is hydrogen or methyl, R 2 is hydrogen, an ester moiety hydrolyzable under mammalian in vivo conditions or an ionically bonded anion of a physiologically acceptable non-toxic salt, and m is an integer of from 1 to 6.
Claim 7
Dependent Claim
56 words
A radiolabeled ACE inhibitor having the general formula: ##STR18## wherein X' is a radiolabeling iodine substituent, R 1 is hydrogen or methyl, R 2 is hydrogen, an ester moiety hydrolyzable under mammalian in vivo conditions or an ionically bonded anion of a physiologically acceptable non-toxic salt, and m is an integer of from 1 to 6.
Claim 8
Dependent Claim
3 words
N-[L-1-carboxy-2-(4-hydroxy-3- 123 iodophenyl)ethyl]-Ala-L-Pro.
Claim 9
Dependent Claim
3 words
N-[L-1-carboxy-2-(4-hydroxy-3- 123 iodophenyl)ethyl]-Ala-L-Pro.
Claim 10
Dependent Claim
3 words
N-[L-1-carboxy-2-(4-hydroxy-3- 125 iodophenyl)ethyl]-Ala-L-Pro.
Claim 11
Dependent Claim
3 words
N-[L-1-carboxy-2-(4-hydroxy-3- 125 iodophenyl)ethyl]-Ala-L-Pro.
Claim 12
Dependent Claim
3 words
N-[L-1-carboxy-2-(4-hydroxy-3- 131 iodophenyl)ethyl]-Ala-L-Pro.
Claim 13
Dependent Claim
3 words
N-[L-1-carboxy-2-(4-hydroxy-3- 131 iodophenyl)ethyl]-Ala-L-Pro.
Claim 14
Dependent Claim
58 words
A method of radioimaging a mammalian site which comprises administering into a blood vessel in the mammal a dose of from about 0.01 mg to about 15 mg, per kilogram of body weight, of a radiolabeled angiotensin converting enzyme (ACE) inhibitor as described in claim 1, and then scanning the mammal to produce an image of the site.
Claim 15
Dependent Claim
57 words
A method as described in claim 9 wherein said mammal is a human being, said radiolabeled ACE inhibitor is N-[L-1-carboxy-2-(4-hydroxy-3- 123 iodophenyl)ethyl]-Ala-L-Pro or N-[L-1-carboxy-2-(4-hydroxy-3- 131 iodophenyl)ethyl]-Ala-L-Pro, administered in a dose of from about 0.05 mg to about 5 mg per kilogram of body weight, and the total radioactivity from said dose is less than about 100 μCi.
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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) | 1989-03-03 | 1989-09-02 | 1990-03-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-03-03 | 1993-09-02 | 1994-03-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-03-03 | 1997-09-02 | 1998-03-04 | $7700.00 | Window Closed / Lapsed |