US4046889A
Expired / Lapsed
US
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Azetidine-2-carboxylic acid derivatives
Assignee: ER Squibb and Sons LLC
•
Filing: 1976-02-13
•
Granted: 1977-09-06
•
Expires: 1996-02-13
Abstract
Abstract New proline derivatives and related compounds which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Inventors
- 👤 Miguel Angel Ondetti
- 👤 David W. Cushman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 05:21
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; C07C; C07C321/00; C07C323/00; C07C327/00; C07C53/00; C07C53/15; C07C53/19; C07C57/00; C07C57/52; C07C57/58; C07D205/00; C07D205/02; C07D205/04; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
65 words
A compound of the formula ##STR14## wherein R is hydroxy, amino or lower alkoxy; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 --CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; m is 1; n is 0, 1 or 2. and basic salts thereof.
Claim 2
Dependent Claim
65 words
A compound of the formula ##STR14## wherein R is hydroxy, amino or lower alkoxy; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 --CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; m is 1; n is 0, 1 or 2. and basic salts thereof.
Claim 3
Dependent Claim
53 words
A compound as in claim 1 wherein R is hydroxy or lower alkoxy; R 1 is hydrogen or lower alkyl; R 2 is hydrogen or R 5 --CO; R 3 and R 4 each is hydrogen; R 5 is lower alkyl or phenyl; m is 1 and n is 0, 1 or 2.
Claim 4
Dependent Claim
15 words
A compound as in claim 1 wherein R 3 and R 4 each is hydrogen.
Claim 5
Dependent Claim
15 words
A compound as in claim 1 wherein m is 1 and R 3 is hydrogen.
Claim 6
Dependent Claim
8 words
The L-form of a compound of claim 1.
Claim 7
Dependent Claim
10 words
A compound as in claim 1 wherein R is hydroxy.
Claim 8
Dependent Claim
10 words
A compound as in claim 1 wherein n is 1.
Claim 9
Dependent Claim
14 words
A compound as in claim 1 wherein R 2 is hydrogen or lower alkanoyl.
Claim 10
Dependent Claim
11 words
A compound as in claim 1 wherein R 2 is hydrogen.
Claim 11
Dependent Claim
11 words
A compound as in claim 1 wherein R 2 is acetyl.
Claim 12
Dependent Claim
14 words
A compound as in claim 1 wherein R 1 is hydrogen or lower alkyl.
Claim 13
Dependent Claim
13 words
A compound as in claim 1 wherein R 1 is hydrogen or methyl.
Claim 14
Dependent Claim
17 words
A compound as in claim 1 wherein R is hydroxy and R 1 is hydrogen or methyl.
Claim 15
Dependent Claim
32 words
A composition comprising a compound of claim 1 in an amount sufficient to reduce blood pressure by inhibiting the conversion of angiotension I to angiotension II and a pharmaceutically acceptable vehicle therefor.
Claim 16
Dependent Claim
51 words
A method for reducing blood pressure by inhibiting the conversion of angiotensin I to angiotensin II which comprises administering a composition comprising a compound of claim 1 in an amount sufficient to reduce blood pressure by inhibiting the conversion of angiotension I to angiotension II and a pharmaceutically acceptable vehicle therefor.
Claim 17
Dependent Claim
10 words
A compound as in claim 1 wherein n is 0.
Claim 18
Dependent Claim
23 words
A compound as in claim 16 wherein R is hydroxy, R 1 and R 3 each is hydrogen and R 2 is benzoyl.
Claim 19
Dependent Claim
22 words
A compound as in claim 16 wherein R is hydroxy and R 1 , R 2 and R 3 each is hydrogen.
Claim 20
Dependent Claim
25 words
A compound as in claim 7 wherein R is hydroxy and R 1 , R 2 , R 4 and R 3 each is hydrogen.
Claim 21
Dependent Claim
26 words
A compound as in claim 7 wherein R is hydroxy, R 1 is methyl and R 2 , R 4 and R 3 each is hydrogen.
Claim 22
Dependent Claim
12 words
The compound of claim 18 wherein the azetidine is in the L-form.
Claim 23
Dependent Claim
12 words
The compound of claim 19 wherein the azetidine is in the L-form.
Claim 24
Dependent Claim
12 words
The compound of claim 20 wherein the azetidine is in the L-form.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-09-05 | 1981-03-07 | 1981-09-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-09-05 | 1985-03-07 | 1985-09-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-09-05 | 1989-03-07 | 1989-09-06 | $7700.00 | Window Closed / Lapsed |