US4384123A
Expired / Lapsed
US
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Phosphinylalkanoyl substituted prolines
Assignee: ER Squibb and Sons LLC
•
Filing: 1981-11-30
•
Granted: 1983-05-17
•
Expires: 2001-11-30
Abstract
Abstract Esters of phosphinylalkanoyl prolines and phosphinylalkanoyl substituted prolines are inhibitors of angiotensin converting enzyme and are useful in the treatment of hypertension.
Inventors
- 👤 Edward W. Petrillo, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 18:22
CPC Classifications
C; C07; C07D; C07D495/00; C07D495/02; C07D495/10; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/553; C07F9/572; C07F9/6561; C07F9/65615
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
144 words
A compound having the formula ##STR27## or a non-toxic, physiologically acceptable salt thereof, wherein R 1 is alkyl, aryl, arylalkyl, cycloalkyl, or cylcoalkylalkyl; R 2 and R 4 each is independently hydrogen, alkyl or arylalkyl; R 3 is hydrogen or alkyl; --R 5 --COOR 4 is ##STR28## R 6 is cycloalkyl or aryl; R 7 and R' 7 together are --S--(CH 2 ) 2 --S--; and n is 0 or 1; and wherein the term "aryl" refers to phenyl or phenyl substituted with halogen, alkyl, alkoxy, alkylthio, hydroxy, alkanoyl, nitro, amino, dialkylamino, or trifluoromethyl groups; the term "alkyl" refers to groups having 1 to 10 carbon atoms; the term "alkoxy" refers to groups having 1 to 8 carbon atoms; the term "cycloalkyl" refers to groups having 3 to 7 carbon atoms; and the term "alkanoyl" refers to groups having 2 to 9 carbon atoms.
Claim 2
Dependent Claim
144 words
A compound having the formula ##STR27## or a non-toxic, physiologically acceptable salt thereof, wherein R 1 is alkyl, aryl, arylalkyl, cycloalkyl, or cylcoalkylalkyl; R 2 and R 4 each is independently hydrogen, alkyl or arylalkyl; R 3 is hydrogen or alkyl; --R 5 --COOR 4 is ##STR28## R 6 is cycloalkyl or aryl; R 7 and R' 7 together are --S--(CH 2 ) 2 --S--; and n is 0 or 1; and wherein the term "aryl" refers to phenyl or phenyl substituted with halogen, alkyl, alkoxy, alkylthio, hydroxy, alkanoyl, nitro, amino, dialkylamino, or trifluoromethyl groups; the term "alkyl" refers to groups having 1 to 10 carbon atoms; the term "alkoxy" refers to groups having 1 to 8 carbon atoms; the term "cycloalkyl" refers to groups having 3 to 7 carbon atoms; and the term "alkanoyl" refers to groups having 2 to 9 carbon atoms.
Claim 3
Dependent Claim
11 words
A compound in accordance with claim 1 wherein n is 0.
Claim 4
Dependent Claim
17 words
A compound in accordance with claim 1 wherein each of R 2 and R 4 is hydrogen.
Claim 5
Dependent Claim
14 words
A compound in accordance with claim 1 wherein --R 5 --COOR 4 is ##STR29##
Claim 6
Dependent Claim
14 words
A compound in accordance with claim 1 wherein --R 5 --COOR 4 is ##STR30##
Claim 7
Dependent Claim
15 words
The compound in accordance with claim 1, (S)-7-[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid, or a physiologically acceptable salt thereof.
Claim 8
Dependent Claim
14 words
The compound in accordance with claim 1, (cis)-4-cyclohexyl-1-[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-L-proline, or a physiologically acceptable salt thereof.
Claim 9
Dependent Claim
14 words
The compound in accordance with claim 1, (cis)-1-[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-4-phenyl-L-proline, or a physiologically acceptable salt thereof.
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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) | 1986-05-16 | 1986-11-15 | 1987-05-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-05-16 | 1990-11-15 | 1991-05-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-05-16 | 1994-11-15 | 1995-05-17 | $7700.00 | Window Closed / Lapsed |