Patent US4849414A successfully refreshed from Google Patents.
US4849414A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Substituted aminoalkanoylaminoalkyl phosphonate angiotensin converting enzyme inhibitors
Assignee: ER Squibb and Sons LLC
•
Filing: 1987-05-20
•
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 12:27
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)
US4555506A
Cited
US4716155A
Cited
US4452790A
Cited
US4616005A
Cited
US4634689A
Cited
US4670422A
Cited
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 |