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US4128653A
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Reduction of blood pressure with carboxyalkylacyl-pipecolic acid derivatives
Assignee: ER Squibb and Sons LLC
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Filing: 1977-02-11
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Granted: 1978-12-05
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Expires: 1997-02-11
Abstract
Abstract New carboxyalkylacylamino acids which are derivatives of proline, pipecolic acid and azetidine-2-carboxylic acid and have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Inventors
- 👤 David W. Cushman
- 👤 Miguel A. Ondetti
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 22:08
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; C07D205/00; C07D205/02; C07D205/04; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
97 words
A method for reducing blood pressure in hypertensive mammals by inhibiting the conversion of angiotensin I to angiotensin II which comprises administering a composition comprising an amount of 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 hydroxy, amino, hydroxyamino or lower alkoxy; R 3 is hydrogen, hydroxy or lower alkyl; m is 3; n is 0, 1 or 2; and physiologically acceptable salts thereof, effective for inhibiting said conversion, and a pharmaceutically acceptable vehicle therefor.
Claim 2
Independent Claim
97 words
A method for reducing blood pressure in hypertensive mammals by inhibiting the conversion of angiotensin I to angiotensin II which comprises administering a composition comprising an amount of 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 hydroxy, amino, hydroxyamino or lower alkoxy; R 3 is hydrogen, hydroxy or lower alkyl; m is 3; n is 0, 1 or 2; and physiologically acceptable salts thereof, effective for inhibiting said conversion, and a pharmaceutically acceptable vehicle therefor.
Claim 3
Dependent Claim
41 words
A method as in claim 1 wherein R is hydroxy or lower alkoxy; R 1 is hydrogen or lower alkyl; R 2 is hydroxy; R 3 and R 4 each is hydrogen; m is 3; and n is 1 or 2.
Claim 4
Dependent Claim
15 words
A method as in claim 1 wherein R 3 and R 4 each is hydrogen.
Claim 5
Dependent Claim
11 words
A method as in claim 1 wherein R 3 is hydrogen.
Claim 6
Dependent Claim
10 words
A method as in claim 1 wherein R is hydroxy.
Claim 7
Dependent Claim
10 words
A method as in claim 1 wherein n is 1.
Claim 8
Dependent Claim
11 words
A method as in claim 1 wherein R 2 is hydroxy.
Claim 9
Dependent Claim
11 words
A method as in claim 1 wherein R 4 is methyl.
Claim 10
Dependent Claim
11 words
A method as in claim 1 wherein R 4 is hydrogen.
Claim 11
Dependent Claim
17 words
A method as in claim 1 wherein R is hydroxy and R 1 is hydrogen or methyl.
Claim 12
Dependent Claim
26 words
A method as in claim 4 wherein R and R 2 each is hydroxy, R 1 is methyl, R 4 is hydrogen and n is 1.
Claim 13
Dependent Claim
26 words
A method as in claim 4 wherein R and R 2 each is hydroxy, R 1 is methyl, R 4 is hydrogen and n is 2.
Claim 14
Dependent Claim
22 words
A method as in claim 4 wherein R and R 2 each is hydroxy, R 1 is methyl and n is 0.
Claim 15
Dependent Claim
36 words
A method as in claim 1 wherein R and R 2 each is hydroxy, R 1 and R 4 each is hydrogen or methyl, R 3 is hydrogen or hydroxy and n is 1 or 2.
Claim 16
Dependent Claim
11 words
A method as in claim 1 wherein R is lower alkoxy.
Claim 17
Dependent Claim
94 words
A composition which inhibits the conversion of angiotensin I to angiotensin II comprising in tablet, capsule, elixir, sterile solution or suspension form an amount of a compound of the formula ##STR15## 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 hydroxy, amino, hydroxyamino or lower alkoxy; R 3 is hydrogen, hydroxy or lower alkyl; m is 3; n is 0, 1 or 2; and physiologically acceptable salts thereof, effective for inhibiting said conversion, and a pharmaceutically acceptable vehicle therefor.
Claim 18
Dependent Claim
94 words
A composition which inhibits the conversion of angiotensin I to angiotensin II comprising in tablet, capsule, elixir, sterile solution or suspension form an amount of a compound of the formula ##STR15## 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 hydroxy, amino, hydroxyamino or lower alkoxy; R 3 is hydrogen, hydroxy or lower alkyl; m is 3; n is 0, 1 or 2; and physiologically acceptable salts thereof, effective for inhibiting said conversion, and a pharmaceutically acceptable vehicle therefor.
References Cited (Backward Citations)
US2627487A
Cited
US3335145A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-12-04 | 1982-06-05 | 1982-12-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-12-04 | 1986-06-05 | 1986-12-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-12-04 | 1990-06-05 | 1990-12-05 | $7700.00 | Window Closed / Lapsed |