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Claims for Patent: 4,470,972

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Claims for Patent: 4,470,972

Title: 7-Carboxyalkylaminoacyl-1,4-dithia-7-azaspiro[4.4]-nonane-8-carboxylic acids
Abstract:This invention relates to 7-carboxyalkyl-aminoacyl-1,4-adithia-7-azaspiro[4.4]nonane-8-carboxylic acids. The compounds of the invention are useful in the treatment of cardiovascular disorders and especially as antihypertensive agents.
Inventor(s): Gold; Elijah H. (West Orange, NJ), Neustadt; Bernard R. (West Orange, NJ), Smith; Elizabeth M. (Verona, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Application Number:06/446,929
Patent Claims: 1. A compound represented by the formula ##STR6## wherein: R is a lower alkyl, benzyl, benzylthio, benzyloxy, phenylthio, or phenoxy;

R.sub.1 is hydroxy or lower alkoxy;

R.sub.2 is hydrogen, lower alkyl or aminoloweralkyl;

and the pharmaceutically acceptable salts thereof.

2. A compound of claim 1 wherein R.sub.2 is methyl.

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

4. A compound of claim 3 wherein R is benzyl.

5. A compound of claim 4 wherein R.sub.1 is ethoxy.

6. A compound of claim 5 which is 7-[N-(1(S)-carboethoxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4 .4]-nonane-8(S)-carboxylic acid hydrochloride.

7. A compound of claim 2 which is 7-[N-(1(S)-carboxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]- nonane-8(S)-carboxylic acid hydrochloride.

8. A compound of claim 2 which is 7-[N-(1(S)-carboxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]- nonane-8(S)-carboxylic acid.

9. A compound of claim 5 which is 7-[N-(1(S)-carboethoxy-3-phenylpropyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4 .4]-nonane-8(S)-carboxylic acid hemimaleate.

10. A compound of claim 1 wherein R.sub.2 is hydrogen.

11. A compound of claim 1 wherein R.sub.2 is aminobutyl.

12. A compound of claim 11 which is 7-[N.alpha.-(1(S)-carboethoxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azas piro[4.4]nonane-8(S)-carboxylic acid dihydrochloride.

13. A compound of claim 11 which is 7-[N.alpha.-(1(S)-carboethoxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azas piro[4.4]nonane-8(S)-carboxylic acid.

14. A compound of claim 11 which is 7-[N.alpha.-(1(S)-carboxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azaspiro [4.4]nonane-8(S)-carboxylic acid dihydrochloride.

15. A compound of claim 11 which is 7-[N.alpha.-(1(S)-carboxy-3-phenylpropyl)-(S)-lysyl]-1,4-dithia-7-azaspiro [4.4]nonane-8(S)-carboxylic acid.

16. A compound of claim 1 wherein R is benzylthio.

17. A compound of claim 1 wherein R is benzyloxy.

18. A compound of claim 1 wherein R is phenylthio.

19. A compound of claim 1 wherein R is phenyloxy.

20. A compound of claim 1 wherein R is lower alkyl.

21. A compound of claim 20 which is 7-[N-(1(S)-carboethoxypentyl)-(S)-alanyl]-1,4-dithia-7-azaspiro [4.4]-nonane-8(S)-carboxylic acid hydrochloride.

22. A compound of claim 20 which is 7-[N-(1(S)-carboethoxybutyl)-(S)-alanyl]-1,4-dithia-7-azaspiro[4.4]-nonane -8(S)-carboxylic acid hydrochloride.

23. A compound of claim 20 which is 7-[N-(1(S)-carboethoxyhexyl)-(S)-alanyl]-1,4[-dithia-7-azaspiro [4.4]-nonane-8(S)-carboxylic acid hydrochloride.

24. A compound of claim 1 wherein the pharmaceutically acceptable salts is an acid salt.

25. A compound of claim 24 wherein the acid salt is hydrochloride or hemimaleate.

26. A pharmaceutical composition comprising an antihypertensive effective amount of a compound according to claim 1 together with a pharmaceutically acceptable carrier.

27. A pharmaceutical composition comprising an antihypertensive effective amount of a compound according to claim 6 together with a pharmaceutically acceptable carrier.

28. A method of treating hypertension in mammals comprising administering to a mammal afflicted with hypertension an effective amount of a compound according to claim 1.

29. A method of treating hypertension in mammals comprising administering to a mammal afflicted with hypertension an effective amount of a compound according to claim 6.
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