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N-carboxyalkanoyl derivatives of azetidine-2-carboxylic acid

Assignee: ER Squibb and Sons LLC
•
Filing: 1977-02-11
•
Granted: 1978-04-25
•
Expires: 1997-02-11
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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 Angel Ondetti

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 15:45
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: 20
Claim 1
Independent Claim 56 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 hydroxy, amino, hydroxyamino or lower alkoxy; R 3 is hydrogen, hydroxy or lower alkyl; m is 1; n is 0, 1 or 2 and salts thereof.
Claim 2
Dependent Claim 56 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 hydroxy, amino, hydroxyamino or lower alkoxy; R 3 is hydrogen, hydroxy or lower alkyl; m is 1; n is 0, 1 or 2 and salts thereof.
Claim 3
Dependent Claim 41 words
A compound 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 1; and n is 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 11 words
A compound as in claim 1 wherein R 3 is hydrogen.
Claim 6
Dependent Claim 22 words
A compound as in claim 4 wherein R and R 2 each is hydroxy, R 1 is methyl and n is 0.
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 10 words
A compound as in claim 1 wherein n is 2.
Claim 10
Dependent Claim 11 words
A compound as in claim 1 wherein R 2 is hydroxy.
Claim 11
Dependent Claim 13 words
A compound of claim 1 in which the azetidine is in the L-form.
Claim 12
Dependent Claim 12 words
A compound as in claim 1 wherein R 2 is lower alkoxy.
Claim 13
Dependent Claim 11 words
A compound as in claim 1 wherein R 4 is methyl.
Claim 14
Dependent Claim 11 words
A compound as in claim 1 wherein R 4 is hydrogen.
Claim 15
Dependent Claim 26 words
A compound 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 16
Dependent Claim 17 words
A compound as in claim 1 wherein R is hydroxy and R 1 is hydrogen or methyl.
Claim 17
Dependent Claim 30 words
A compound as in claim 4 wherein R and R 2 each is hydroxy, R 1 and R 4 each is hydrogen or methyl and n is 1 or 2.
Claim 18
Dependent Claim 26 words
A compound 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 19
Dependent Claim 24 words
A composition for reducing blood pressure comprising about 10 to 500 mg. of a compound of claim 1 and a pharmaceutically acceptable vehicle therefor.
Claim 20
Dependent Claim 45 words
A method for reducing blood pressure by inhibiting the conversion of angiotensin I to angiotensin II which comprises administering to a mammal suffering from hypertension a composition comprising about 10 to 500 mg. of a compound of claim 1 and a pharmaceutically acceptable vehicle therefor.

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) 1981-04-24 1981-10-24 1982-04-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-04-24 1985-10-24 1986-04-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-04-24 1989-10-24 1990-04-25 $7700.00 Window Closed / Lapsed

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