US4146641A
Expired / Lapsed
US
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Carboxyalkylacylamino acids
Assignee: ER Squibb and Sons LLC
•
Filing: 1978-05-04
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Granted: 1979-03-27
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Expires: 1998-05-04
Abstract
Abstract New carboxyalkylacylamino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Inventors
- 👤 Miguel A. Ondetti
- 👤 David W. Cushman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 01:46
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/64; A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61K31/21; A61K31/215; A61K31/22; A61K31/235; A61K31/24; A61K31/33; A61K31/395; A61K31/40; A61K31/403; A61K31/404; A61K31/405; A61K31/41; A61K31/415; A61P; A61P43/00; C07C; C07C233/00; C07C233/01; C07C233/30; C07C233/45; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/20
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
59 words
A compound of the formula ##STR12## and salts thereof, wherein R 1 is hydrogen, lower alkyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercapto-lower alkylene, lower alkylmercapto-lower alkylene or carbamoyl-lower alkylene; R 2 is hydrogen or lower alkyl; R 3 is lower alkyl or phenyl-lower alkylene; R 4 is hydroxyamino; and n is 1 or 2.
Claim 2
Dependent Claim
59 words
A compound of the formula ##STR12## and salts thereof, wherein R 1 is hydrogen, lower alkyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, mercapto-lower alkylene, lower alkylmercapto-lower alkylene or carbamoyl-lower alkylene; R 2 is hydrogen or lower alkyl; R 3 is lower alkyl or phenyl-lower alkylene; R 4 is hydroxyamino; and n is 1 or 2.
Claim 3
Dependent Claim
10 words
A compound as in claim 1 wherein n is 1.
Claim 4
Dependent Claim
30 words
A compound as in claim 1 wherein R 1 is guanidino-lower alkylene, amino-lower alkylene or phenyl-lower alkylene; R 2 is hydrogen or lower alkyl; and R 3 is lower alkyl.
Claim 5
Dependent Claim
10 words
A compound as in claim 3 wherein n is 2.
Claim 6
Dependent Claim
30 words
A compound as in claim 2 wherein R 1 is guanidino-propyl, amino-C 3 -C 4 -lower alkylene or phenylmethyl; R 2 is hydrogen or methyl; and R 3 is methyl.
Claim 7
Dependent Claim
22 words
A compound as in claim 2 wherein R 1 is phenylmethyl; R 2 is hydrogen or methyl; and R 3 is methyl.
Claim 8
Dependent Claim
11 words
A compound as in claim 6 wherein R 2 is hydrogen.
Claim 9
Dependent Claim
22 words
A compound as in claim 2 wherein R 1 is aminobutyl; R 2 is hydrogen or methyl; and R 3 is methyl.
Claim 10
Dependent Claim
11 words
A compound as in claim 8 wherein R 2 is hydrogen.
Claim 11
Dependent Claim
22 words
A compound as in claim 2 wherein R 1 is guanidinopropyl; R 2 is hydrogen or methyl; and R 3 is methyl.
Claim 12
Dependent Claim
11 words
A compound as in claim 10 wherein R 2 is hydrogen.
Claim 13
Dependent Claim
10 words
A compound as in claim 1 wherein n is 2.
Claim 14
Dependent Claim
12 words
A compound as in claim 1 wherein R 1 is hydroxyphenyl-lower alkylene.
Claim 15
Dependent Claim
18 words
A compound as in claim 13 wherein R 2 is hydrogen or methyl; and R 3 is methyl.
Claim 16
Dependent Claim
20 words
A compound as in claim 1 wherein R 1 is p-hydroxyphenylmethyl; R 2 is hydrogen, and R 3 is methyl.
Claim 17
Dependent Claim
10 words
A compound as in claim 15 wherein n is 2.
Claim 18
Dependent Claim
20 words
A composition comprising about 10 to 500 mg. of a compound of claim 1 and a physiologically acceptable vehicle therefor.
Claim 19
Dependent Claim
20 words
A composition comprising about 10 to 500 mg. of the compound of claim 9 and a physiologically acceptable vehicle therefor.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-26 | 1982-09-25 | 1983-03-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-26 | 1986-09-25 | 1987-03-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-26 | 1990-09-25 | 1991-03-27 | $7700.00 | Window Closed / Lapsed |