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Claims for Patent: 4,337,201

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Claims for Patent: 4,337,201

Title: Phosphinylalkanoyl substituted prolines
Abstract:Esters of phosphinylalkanoyl prolines and phosphinylalkanoyl substituted prolines are inhibitors of angiotensin converting enzyme and are useful in the treatment of hypertension.
Inventor(s): Petrillo, Jr.; Edward W. (Pennington, NJ)
Assignee: E. R. Squibb & Sons, Inc. (Princeton, NJ)
Application Number:06/212,911
Patent Claims: 1. A compound having the formula ##STR27## or a salt thereof, wherein R.sub.1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkylalkyl;

one of R.sub.2 and R.sub.4 is ##STR28## and the other is hydrogen, alkyl, arylalkyl or ##STR29## wherein X is hydrogen, alkyl or phenyl and Y is hydrogen, alkyl, phenyl or alkoxy, or together X and Y are --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH-- or ##STR30## R.sub.3 is hydrogen or alkyl; --R.sub.5 --COOR.sub.4 is ##STR31## R.sub.6 is hydrogen, hydroxy, alkyl, halogen, azido, amino, cycloalkyl, aryl, arylalkyl, carbamoyloxy, N,N-dialkylcarbamoyloxy, or --Z--R.sub.9 ;

R.sub.7 and R.sub.7 ' are the same and each is halogen or --Z--R.sub.10, or R.sub.7 and R.sub.7 ' together are .dbd.O, --O--(CH.sub.2).sub.m --O-- or --S--(CH.sub.2).sub.m --S--;

R.sub.8 is hydrogen and R.sub.8 ' is phenyl, 2-hydroxyphenyl or 4-hydroxyphenyl or R.sub.8 and R.sub.8 ' together are .dbd.O;

R.sub.9 is alkyl, aryl, arylalkyl, 1- or 2-naphthyl, or biphenyl;

R.sub.10 is alkyl, aryl or arylalkyl;

Z is oxygen or sulfur;

n is 0 or 1; and

m is 1 or 2;

and wherein the term "aryl" refers to phenyl or phenyl substituted with halogen, alkyl, alkoxy, alkylthio, hydroxy, alkanoyl, nitro, amino, dialkylamino or trifluoromethyl groups; the term "alkyl" refers to groups having 1 to 10 carbon atoms; the term "alkoxy" refers to groups having 1 to 8 carbon atoms; the term "cycloalkyl" refers to groups having 3 to 7 carbon atoms; and the term "alkanoyl" refers to groups having 2 to 9 carbon atoms.

2. A compound in accordance with claim 1 wherein one of R.sub.2 and R.sub.4 is ##STR32## and the other is hydrogen.

3. A compound in accordance with claim 4 wherein R.sub.1 is 4-phenylbutyl and R.sub.3 is hydrogen.

4. A compound in accordance with claim 1 wherein n is 0.

5. A compound in accordance with claim 2 wherein R.sub.2 is hydrogen and R.sub.4 is ##STR33##

6. A compound in accordance with claim 2 wherein R.sub.2 is ##STR34## and R.sub.4 is hydrogen.

7. A compound in accordance with claim 1 wherein --R.sub.5 --COOR.sub.4 is ##STR35##

8. A compound in accordance with claim 1 wherein --R.sub.5 --COOR.sub.4 is ##STR36##

9. A compound in accordance with claim 1 wherein --R.sub.5 --COOR.sub.4 is ##STR37##

10. A compound in accordance with claim 1 wherein --R.sub.5 --COOR.sub.4 is ##STR38##

11. The compound in accordance with claim 1, (S)-7-[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-1,4-dithia-7-azaspiro[4.4 ]nonane-8-carboxylic acid, (2,2-dimethyl-1-oxopropoxy)methyl ester, or a salt thereof.

12. The compound in accordance with claim 1, 1-[[hydroxy(4-phenylbutyl)phosphinyl]acetyl]-L-proline, (2,2-dimethyl-1-oxopropoxy)methyl ester, or a salt thereof.

13. The compound in accordance with claim 1, 1-[[[(2,2-dimethyl-1-oxopropoxy)methoxy](4-phenylbutyl)phosphinyl]acetyl]- L-proline, or a salt thereof.
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