US4339600A
Expired / Lapsed
US
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Compounds for alleviating angiotensin related hypertension
Assignee: ER Squibb and Sons LLC
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Filing: 1978-02-13
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Granted: 1982-07-13
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Expires: 1998-02-13
Abstract
Abstract Compounds for alleviating or reducing angiotensin related hypertension in hypertensive mammals comprising angiotensin converting enzyme inhibitors selected from a group of mercaptoacyl aminoacids.
Inventors
- 👤 Miguel A. Ondetti
- 👤 David W. Cushman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 18:37
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/64; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/20
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
81 words
A compound of the formula ##STR12## or a physiologically acceptable salt thereof, wherein R 1 is hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercapto-lower alkylene, lower alkylmercapto-lower alkylene, carbamoyl-lower alkylene or carboxy-lower alkylene; R 2 and R 3 each is hydrogen, lower alkyl or phenyl-lower alkylene; and R 5 is hydrogen, lower alkanoyl, benzoyl or ##STR13## with the proviso that if R 2 and R 5 are both hydrogen and R 3 is methyl, R 1 is not mercapto-lower alkylene.
Claim 2
Dependent Claim
81 words
A compound of the formula ##STR12## or a physiologically acceptable salt thereof, wherein R 1 is hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercapto-lower alkylene, lower alkylmercapto-lower alkylene, carbamoyl-lower alkylene or carboxy-lower alkylene; R 2 and R 3 each is hydrogen, lower alkyl or phenyl-lower alkylene; and R 5 is hydrogen, lower alkanoyl, benzoyl or ##STR13## with the proviso that if R 2 and R 5 are both hydrogen and R 3 is methyl, R 1 is not mercapto-lower alkylene.
Claim 3
Dependent Claim
61 words
A compound of the formula ##STR14## or a physiologically acceptable salt thereof, wherein R 1 is lower alkyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercapto-lower alkylene, lower alkylmercapto-lower alkylene, carbamoyl-lower alkylene or carboxy-lower alkylene; R 2 and R 3 each is hydrogen, lower alkyl or phenyl-lower alkylene; and R 5 is hydrogen, lower alkanoyl, benzoyl or ##STR15##
Claim 4
Dependent Claim
61 words
A compound of the formula ##STR14## or a physiologically acceptable salt thereof, wherein R 1 is lower alkyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercapto-lower alkylene, lower alkylmercapto-lower alkylene, carbamoyl-lower alkylene or carboxy-lower alkylene; R 2 and R 3 each is hydrogen, lower alkyl or phenyl-lower alkylene; and R 5 is hydrogen, lower alkanoyl, benzoyl or ##STR15##
Claim 5
Dependent Claim
65 words
A compound of the formula ##STR16## or a physiologically acceptable salt thereof, wherein R 1 is hydrogen, lower alkyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercaptolower alkylene, lower alkylmercapto-lower alkylene, carbamoyllower alkylene, or carboxy-lower alkylene; R 2 , R 3 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkylene; and R 5 is hydrogen, lower alkanoyl, benzoyl or ##STR17##
Claim 6
Dependent Claim
65 words
A compound of the formula ##STR16## or a physiologically acceptable salt thereof, wherein R 1 is hydrogen, lower alkyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercaptolower alkylene, lower alkylmercapto-lower alkylene, carbamoyllower alkylene, or carboxy-lower alkylene; R 2 , R 3 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkylene; and R 5 is hydrogen, lower alkanoyl, benzoyl or ##STR17##
Claim 7
Dependent Claim
37 words
A compound as in claim 2 wherein R 1 is guanidino-lower alkylene, amino-lower alkylene, phenyl-lower alkylene or lower alkyl; R 2 and R 5 each is hydrogen; and R 3 is hydrogen, lower alkyl or phenyl-lower alkylene.
Claim 8
Dependent Claim
34 words
A compound as in claim 2 wherein R 1 is guanidinopropyl, aminopropyl, aminobutyl, phenylmethyl, or isobutyl; R 2 and R 5 each is hydrogen; and R 3 is hydrogen, lower alkyl or phenyl-lower alkylene.
Claim 9
Dependent Claim
23 words
A compound as in claim 2 wherein R 1 is phenylmethyl and R 2 , R 3 and R 5 each is hydrogen.
Claim 10
Dependent Claim
16 words
A compound as in claim 2 wherein R 1 is isobutyl and R 3 is hydrogen.
Claim 11
Dependent Claim
23 words
A compound as in claim 2 wherein R 1 is guanidinopropyl and R 2 , R 3 and R 5 each is hydrogen.
Claim 12
Dependent Claim
11 words
A compound as in claim 2 wherein R 5 is ##STR18##
Claim 13
Dependent Claim
12 words
A compound as in claim 9 wherein each R 1 is guanidinopropyl.
Claim 14
Dependent Claim
12 words
A compound as in claim 9 wherein each R 1 is isopropyl.
Claim 15
Dependent Claim
19 words
A compound as in claim 6 wherein R 2 and R 5 each is hydrogen having the name N-(3-mercaptopropanoyl)-L-phenylalanine.
Claim 16
Dependent Claim
19 words
A compound as in claim 7 wherein R 2 and R 5 each is hydrogen having the name N-(3-mercaptopropanoyl)-L-leucine.
Claim 17
Dependent Claim
19 words
A compound as in claim 8, wherein R 2 and R 5 each is hydrogen having the N.sup.α -(3-mercaptopropanoyl)-L-arginine.
Claim 18
Dependent Claim
29 words
A compound as in claim 2 wherein R 1 is guanidinopropyl, R 2 and R 5 each is hydrogen and R 3 is methyl having the name N.sup.α -(3-mercapto-2-methylpropanoyl)-L-arginine.
Claim 19
Dependent Claim
24 words
A compound as in claim 10 wherein each R 2 is hydrogen and each R 3 is methyl, having the name N.sup.α, N.sup.α' -[dithio-3,3'-bis(2-methylpropanoyl)]-bis-L-arginine.
Claim 20
Dependent Claim
22 words
A compound as in claim 11 wherein each R 2 is hydrogen and each R 3 is methyl having the name N,N'-[dithio-3,3'-bis(2-methylpropanoyl)]-bis-L-valine.
Claim 21
Dependent Claim
12 words
A compound as in claim 2 wherein R 1 is hydroxyphenyl-lower alkylene.
Claim 22
Dependent Claim
28 words
A compound as in claim 2 wherein R 1 is (4-hydroxyphenyl)methyl, R 2 and R 5 each is hydrogen and R 3 is methyl having the name N-(3-mercapto-2-methylpropanoyl)-L-tyrosine.
Claim 23
Dependent Claim
28 words
A compound as in claim 2 wherein R 1 is (3,4-dihydroxyphenyl)methyl, R 2 and R 5 each is hydrogen and R 3 is methyl having the name 3-hydroxy-N-(DL-3-mercapto-2-methylpropanoyl)-L-tyrosine.
Claim 24
Dependent Claim
27 words
A compound as in claim 2 wherein R 1 is (3,4-dihydroxyphenyl)methyl and R 2 , R 3 and R 5 each is hydrogen having the name 3-hydroxy-N-(3-mercaptopropanoyl)-L-tyrosine.
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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) | 1985-07-12 | 1986-01-11 | 1986-07-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-07-12 | 1990-01-11 | 1990-07-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-07-12 | 1994-01-11 | 1994-07-13 | $7700.00 | Window Closed / Lapsed |