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Details for Patent: 4,046,889

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Details for Patent: 4,046,889

Title: Azetidine-2-carboxylic acid derivatives
Abstract:New proline derivatives and related compounds which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Inventor(s): Ondetti; Miguel Angel (Princeton, NJ), Cushman; David W. (West Windsor, NJ)
Assignee: E. R. Squibb & Sons, Inc. (Princeton, NJ)
Filing Date:Feb 13, 1976
Application Number:05/657,792
Claims:1. A compound of the formula ##STR14## wherein R is hydroxy, amino or lower alkoxy;

R.sub.1 and R.sub.4 each is hydrogen, lower alkyl or phenyl-lower alkyl;

R.sub.2 is hydrogen or R.sub.5 --CO;

R.sub.3 is hydrogen, hydroxy or lower alkyl;

R.sub.5 is lower alkyl, phenyl or phenyl-lower alkyl;

m is 1;

n is 0, 1 or 2.

and basic salts thereof.

2. A compound as in claim 1 wherein R is hydroxy or lower alkoxy; R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or R.sub.5 --CO; R.sub.3 and R.sub.4 each is hydrogen; R.sub.5 is lower alkyl or phenyl; m is 1 and n is 0, 1 or 2.

3. A compound as in claim 1 wherein R.sub.3 and R.sub.4 each is hydrogen.

4. A compound as in claim 1 wherein m is 1 and R.sub.3 is hydrogen.

5. The L-form of a compound of claim 1.

6. A compound as in claim 1 wherein R is hydroxy.

7. A compound as in claim 1 wherein n is 1.

8. A compound as in claim 1 wherein R.sub.2 is hydrogen or lower alkanoyl.

9. A compound as in claim 1 wherein R.sub.2 is hydrogen.

10. A compound as in claim 1 wherein R.sub.2 is acetyl.

11. A compound as in claim 1 wherein R.sub.1 is hydrogen or lower alkyl.

12. A compound as in claim 1 wherein R.sub.1 is hydrogen or methyl.

13. A compound as in claim 1 wherein R is hydroxy and R.sub.1 is hydrogen or methyl.

14. 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.

15. 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.

16. A compound as in claim 1 wherein n is 0.

17. A compound as in claim 16 wherein R is hydroxy, R.sub.1 and R.sub.3 each is hydrogen and R.sub.2 is benzoyl.

18. A compound as in claim 16 wherein R is hydroxy and R.sub.1, R.sub.2 and R.sub.3 each is hydrogen.

19. A compound as in claim 7 wherein R is hydroxy and R.sub.1, R.sub.2, R.sub.4 and R.sub.3 each is hydrogen.

20. A compound as in claim 7 wherein R is hydroxy, R.sub.1 is methyl and R.sub.2, R.sub.4 and R.sub.3 each is hydrogen.

21. The compound of claim 18 wherein the azetidine is in the L-form.

22. The compound of claim 19 wherein the azetidine is in the L-form.

23. The compound of claim 20 wherein the azetidine is in the L-form.
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