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Generated: October 22, 2017

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Title: Carboxyalkyl dipeptides and medical use thereof in treating hypertension and congestive heart failure
Abstract:The present invention relates to carboxyalkyl dipeptides which are inhibitors of angiotensin-converting enzyme and are useful as antihypertensive agents and in the treatment of congestive heart failure. The compounds of the present invention are compounds of the formulae ##STR1## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy or lower alkoxy; R.sup.1 is benzyloxylower alkyl or benzylthiolower alkyl; R.sup.2 is benzylthiomethyl, 2-phyenylethylthiomethyl, napthylmethylthiomethyl, methylbenzylthiomethyl, 2-(carboxyphenyl)ethyl or 2-(alkoxycarbonylphenyl)ethyl) and R.sup.3 is hydrogen, lower alkyl or aminolower alkyl.
Inventor(s): Gold; Elijah H. (West Orange, NJ), Neustadt; Bernard R. (West Orange, NJ), Smith; Elizabeth M. (Verona, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Filing Date:Nov 04, 1987
Application Number:07/117,008
Claims:1. A compound represented by the formula ##STR12## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy or lower alkoxy;

R.sup.2 is benzylthiomethyl, 2-phenylethylthiomethyl, naphthylmethylthiomethyl, methylbenzylthiomethyl, carboxyphenylethyl or alkoxycarbonylphenylethyl; and

R.sup.3 is hydrogen, lower alkyl or aminolower alkyl.

2. A compound of claim 1 wherein R is lower alkoxy.

3. A compound of claim 1 wherein R is ethoxy.

4. A compound of claim 1 wherein R.sup.6 is hydroxy.

5. A compound of claim 1 wherein R.sup.3 is lower alkyl.

6. A compound of claim 1 wherein R.sup.3 is methyl.

7. A compound of claim 1 wherein R.sup.2 is benzylthiomethyl.

8. A compound of claim 1 wherein R.sup.2 is 2-phenylethylthiomethyl.

9. A compound of claim 1 wherein R.sup.2 is naphthylmethylthiomethyl.

10. A compound of claim 1 wherein R.sup.2 is methylbenzylthiomethyl.

11. A compound of claim 1 wherein R.sup.2 is carboxyphenylethyl.

12. A compound of claim 1 wherein R.sup.2 is alkoxycarbonylphenylethyl.

13. A compound of claim 12 wherein R.sup.2 is ethoxycarbonylphenylethyl.

14. A compound of claim 1 wherein R is lower alkoxy, R.sup.6 is hydroxy, R.sup.3 is lower alkyl, and R.sup.2 is benzylthiomethyl, 2-phenylethylthiomethyl, naphthylmethylthiomethyl, methylbenzylthiomethyl, carboxyphenylethyl or ethoxycarbonylphenylethyl.

15. A compound of claim 14 wherein R is ethoxy and R.sup.3 is methyl.

16. A compound of claim 14 selected from 1-[N-[1(R)-ethoxycarbonyl-2-(4-methylbenzylthio)ethyl]-(R,S)-alanyl]-cis,s yn-perhydroindole-2(S)-carboxylic acid;

1-[N-[1(S)-ethoxycarbonyl-3-(4-ethoxycarbonylphenyl)propyl]-(S)-alanyl]-cis ,syn-perhydroindole-2(S)carboxylic acid;

1-[N-[1(R)-ethoxycarbonyl-2-(benzylthio)ethyl]-(R,S)-alanyl]-cis,syn-perhyd roindole-2(S)-carboxylic acid;

1-[N-[1(R)-ethoxycarbonyl-2-(phenylthio)ethyl]-(S)-alanyl]-cis,syn-perhydro indole-2(S)-carboxylic acid;

1-[N-[1(R)-ethoxycarbonyl-2-(2-naphthylmethylthio)ethyl]-(S)-alanyl]-cis,sy n-perhydroindole-2(S)-carboxylic acid.

17. A compound of claim 11 wherein R is hydroxy and R.sup.3 is methyl.

18. A compound of claim 17 which is 1-[N-(1(S)-carboxy-3-(4-carboxyphenyl)propyl]-(S)-alanyl]-cis,syn-perhydro indole-2(S)-carboxylic acid.

19. An antihypertensive pharmaceutical composition comprising an antihypertensive effective amount of a compound of claim 1, together with a pharmaceutically acceptable carrier.

20. A method for reducing blood pressure in a hypertensive mammal which comprises administering to such a mammal a composition of claim 19.

21. A method of treating congestive heart failure in a mammal in need of such treatment comprising administering to such a mammal an amount of a compound of claim 1 effective in treating congestive heart failure.
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