US4849414A
Expired / Lapsed
US
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Substituted aminoalkanoylaminoalkyl phosphonate angiotensin converting enzyme inhibitors
Assignee: ER Squibb and Sons LLC
•
Filing: 1987-05-20
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Granted: 1989-07-18
•
Expires: 2007-05-20
Abstract
Abstract Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Inventors
- 👤 Melanie J. Loots
- 👤 Donald S. Karanewsky
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 12:13
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/6561; C07F9/28; C07F9/38; C07F9/40; C07F9/4003; C07F9/4006; C07F9/4071; C07F9/4075; C07F9/553; C07F9/572; C07F9/5728; C07F9/645; C07F9/6503; C07F9/6506
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
66 words
A compound of the formula ##STR156## including a pharmaceutically acceptable salt thereof wherein: R 1 is methyl or --(CH 2 ) 4 --NH 2 ; R 2 is methyl, n-butyl, or benzyl; R 3 is hydrogen, sodium ion, potassium ion, calcium ion, or lithium ion; R 4 is methyl, n-butyl, --(CH 2 ) 4 --NH 2 , ##STR157## and R 24 is --NH 2 , ##STR158##
Claim 2
Dependent Claim
66 words
A compound of the formula ##STR156## including a pharmaceutically acceptable salt thereof wherein: R 1 is methyl or --(CH 2 ) 4 --NH 2 ; R 2 is methyl, n-butyl, or benzyl; R 3 is hydrogen, sodium ion, potassium ion, calcium ion, or lithium ion; R 4 is methyl, n-butyl, --(CH 2 ) 4 --NH 2 , ##STR157## and R 24 is --NH 2 , ##STR158##
Claim 3
Dependent Claim
12 words
The compound of claim 1 wherein: R 24 is NH 2 .
Claim 4
Dependent Claim
31 words
The compound of claim 2 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; and R 4 is --CH 3 .
Claim 5
Dependent Claim
35 words
The compound of claim 2 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; and R 4 is --(CH 2 ) 4 --NH 2 .
Claim 6
Dependent Claim
35 words
The compound of claim 2 wherein: R 1 is --CH 3 ; R 2 is benzyl; R 3 and R 6 are both hydrogen; and R 4 is --(CH 2 ) 4 --NH 2 .
Claim 7
Dependent Claim
29 words
The compound of claim 2 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; and R 4 is n-butyl.
Claim 8
Dependent Claim
10 words
A compound of claim 1 wherein R 24 is ##STR159##
Claim 9
Dependent Claim
39 words
The compound of claim 7 wherein R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR160##
Claim 10
Dependent Claim
43 words
The compound of claim 7 wherein: R 1 is --(CH 2 ) 4 --NH 2 ; R 2 is benzyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR161##
Claim 11
Dependent Claim
39 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is benzyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR162##
Claim 12
Dependent Claim
35 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both lithium; R 4 is --CH 3 ; and R 24 is ##STR163##
Claim 13
Dependent Claim
33 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both lithium; R 4 is n-butyl; and R 24 is ##STR164##
Claim 14
Dependent Claim
43 words
The compound of claim 7 wherein: R 1 is --(CH 2 ) 4 --NH 2 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR165##
Claim 15
Dependent Claim
33 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is ##STR166## and R 24 is ##STR167##
Claim 16
Dependent Claim
33 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is ##STR168## and R 24 is ##STR169##
Claim 17
Dependent Claim
39 words
The compound of claim 7 wherein; R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR170##
Claim 18
Dependent Claim
39 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR171##
Claim 19
Dependent Claim
39 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR172##
Claim 20
Dependent Claim
39 words
The compound of claim 7 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; R 4 is --(CH 2 ) 4 --NH 2 ; and R 24 is ##STR173##
Claim 21
Dependent Claim
10 words
A compound of claim 1 wherein R 24 is ##STR174##
Claim 22
Dependent Claim
29 words
The compound of claim 20 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both lithium; and R 4 is n-butyl.
Claim 23
Dependent Claim
10 words
A compound of claim 1 wherein: R 24 is ##STR175##
Claim 24
Dependent Claim
35 words
The compound of claim 22 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; and R 4 is --(CH 2 ) 4 --NH 2 .
Claim 25
Dependent Claim
10 words
A compound of claim 1 wherein R 24 is ##STR176##
Claim 26
Dependent Claim
35 words
The compound of claim 24 wherein: R 1 is --CH 3 ; R 2 is n-butyl; R 3 and R 6 are both hydrogen; and R 4 is --(CH 2 ) 4 --NH 2 .
Claim 27
Dependent Claim
27 words
A pharmaceutical composition useful for treating hypertension in a mammalian species comprising a pharmaceutically acceptable carrier and an anti-hypertensive effective amount of a compound of claim 1.
Claim 28
Dependent Claim
21 words
The method of treating hypertension in a mammalian host which comprises administering an effective amount of the composition of claim 6.
References Cited (Backward Citations)
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Cited
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Cited
US4670422A
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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) | 1992-07-17 | 1993-01-16 | 1993-07-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-17 | 1997-01-16 | 1997-07-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-17 | 2001-01-16 | 2001-07-18 | $7700.00 | Window Closed / Lapsed |