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Claims for Patent: 4,587,258

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Claims for Patent: 4,587,258

Title: Angiotensin-converting enzyme inhibitors
Abstract:Novel compounds with angiotensin-converting enzyme inhibitory activity are disclosed. Such compounds are useful in the treatment of cardiovascular disorders, especially hypertension and congestive heart failure, and are useful in the treatment of glaucoma.
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:06/635,390
Patent Claims: 1. A compound represented by the formula ##STR23## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy, lower alkoxy, lower alkenoxy, dilower alkylamino lower alkoxy, acylamino lower alkoxy, acyloxy lower alkoxy, aryloxy, arylloweralkoxy, amino, lower alkylamino, dilower alkylamino, hydroxyamino, aryllower alkylamino, or substituted aryloxy or substituted aryllower alkoxy wherein the substituent is methyl, halo or methoxy;

R.sup.1 is hydrogen, alkyl of from 1 to 10 carbon atoms, including branched and cyclic and unsaturated alkyl groups, substituted lower alkyl wherein the substituent is hydroxy, lower alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, amino, lower alkylamino, diloweralkylamino, acylamino, arylamino, substituted arylamino, guanidino, imidazolyl, indolyl, lower alkylthio, arylthio, substituted arylthio, carboxy, carbamoyl, lower alkoxycarbonyl, aryl, substituted aryl, aralkyloxy, substituted aralkyloxy, aralkylthio, or substituted aralkylthio, wherein the aryl or heteroaryl portion of said substituted aryloxy, heteroaryloxy, arylamino, arylthio, aryl, aralkyloxy or aralkylthio groups is substituted with a group selected from halo, loweralkyl, hydroxy, lower alkoxy, amino, aminomethyl, carboxyl, cyano and sulfamoyl;

R.sup.3 is hydrogen, lower alkyl, phenyl lower alkyl, aminomethylphenyl lower alkyl, hydroxyphenyl lower alkyl, hydroxy lower alkyl, acylamino lower alkyl, amino lower alkyl, dimethylamino lower alkyl, guanidino lower alkyl, imidazolyl lower alkyl, indolyl lower alkyl, or lower alkylthio lower alkyl.

2. A compound of claim 1 which is a cis,endo isomer of octahydrocyclopenta[b]pyrrole-2(S)-carboxylic acid.

3. The compound of claim 1 which is 1-[N-(1(S)-carboethoxy-3-phenylpropyl)-(S)-alanyl]-cis,endo-octahydrocyclo penta[b]pyrrole-2(S)-carboxylic acid.

4. The compound of claim 1 which is 1[N-(1(S)-carboethoxy-3-phenylpropyl)-(S)-alanyl]-cis,endo-octahydrocyclop enta[b]pyrrole-2(S)-carboxylic acid hydrochloride.

5. The compound of claim 1 is 1-[N-(1(S)-carboxy-3-phenylpropyl)-(S)-alanyl]-cis,endo-octahydrocyclopent a[b]pyrrole-2(S)-carboxylic acid.

6. The compound of claim 1 is 1-[N-(1(S)-carboxy-3-phenylpropyl)-(S)-alanyl]-cis,endo-octahydrocyclopent a[b]pyrrole-2(S)-carboxylic acid hydrochloride.

7. The compound of claim 1 which is 1[N.alpha.-(1(S)-carboethoxy-3-phenylpropyl)-(S)-lysyl]-cis,endooctahydroc yclopenta[b]pyrrole-2(S)-carboxylic acid.

8. The compound of claim 1 which is 1[N.alpha.-(1(S)-carboethoxy-3-phenylpropyl)-(S)-lysyl]-cis,endo-octahydro cyclopenta[b]pyrrole-2(S-carboxylic acid hydrochloride.

9. The compound of claim 1 which is 1[N.alpha.-(1(S)-carboethoxy-3-phenylpropyl)-(S)-lysyl]-cis,endo-octahydro cyclopenta[b]pyrrole-2(S)-carboxylic acid dihydrochloride.

10. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboxy-3-phenylpropyl)-(S)-lysyl]-cis,endo-octahydrocyc lopenta[b]pyrrole-2(S)-carboxylic acid.

11. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboxy-3-phenylpropyl)-(S)-lysyl]-cis,endo-octahydrocyc lopenta[b]pyrrole-2(S)-carboxylic acid hydrochloride.

12. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboxy-3-phenylpropyl)-(S)-lysyl]-cis,endo-octahydrocyc lopenta[b]pyrrole-2(S)-carboxylic acid dihydrochloride.

13. The compound of claim 1 which is 1-[N-(1(S)-carboethoxybutyl)-(S)-alanyl]-cis,endo-octahydrocyclopenta[b]py rrole-2(S)-carboxylic acid.

14. The compound of claim 1 which is 1-[N-(1(S)-carboethoxybutyl)-(S)-alanyl]-cis,endo-octahydrocyclopenta[b]py rrole-2(S)-carboxylic acid hydrochloride.

15. The compound of claim 1 which is 1-[N-(1(S)-carboxybutyl)-(S)-alanyl]-cis,endo-octahydrocyclopenta[b]pyrrol e-2(S)-carboxylic acid.

16. The compound of claim 1 which is 1-[N-(1(S)-carboxybutyl)-(S)-alanyl]-cis,endo-octahydrocyclopenta[b]pyrrol e-2(S)-carboxylic acid hydrochloride.

17. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboethoxybutyl)-(S)-lysyl]-cis,endo-octahydrocyclopent a[b]pyrrole-2(S)-carboxylic acid.

18. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboethoxybutyl)-(S)-lysyl]-cis,endo-octahydrocyclopent a[b]pyrrole-2(S)-carboxylic acid hydrochloride.

19. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboethoxybutyl)-(S)-lysyl]-cis,endo-octahydrocyclopent a[b]pyrrole-2(S)-carboxylic acid dihydrochloride.

20. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboxybutyl)-(S)-lysyl]-cis,endo-octahydrocyclopenta[b] pyrrole-2(S)-carboxylic acid.

21. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboxybutyl)-(S)-lysyl]-cis,endo-octahydrocyclopenta[b] - pyrrole-2(S)-carboxylic acid hydrochloride.

22. The compound of claim 1 which is 1-[N.alpha.-(1(S)-carboxybutyl)-(S)-lysyl]cis,endo-octahydrocyclopenta[b]p yrrole-2(S)-carboxylic acid dihydrochloride.

23. A compound of claim 1 which is a cis,exo isomer of octahydrocyclopenta[b]pyrrole-2(S)-carboxylic acid.

24. A compound of claim 1, which is a hydrochloride salt.

25. A compound of claim 1 which is a maleate salt.

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

27. A method for reducing blood pressure in hypertensive mammals which comprises administering to such a mammal a composition comprising an antihypertensive effective amount of a compound of claim 1 together with a pharmaceutically acceptable carrier therefor.

28. A method for treating mammals suffering from congestive heart failure which comprises administering to such a mammal a composition comprising an amount of a compound of claim 1 effective in treating congestive heart failure together with a pharmaceutically acceptable carrier therefor.

29. A method for treating glaucoma in mammals suffering from glaucoma which comprises administering to such a mammal a composition comprising an anti-glaucoma effective amount of a compound of claim 1 together with a pharmaceutically acceptable carrier therefor.

30. A method for reducing blood pressure in hypertensive mammals which comprises administering to such a mammal a composition comprising an antihypertensive effective amount of a compound of claim 1 in combination with a diuretic, together with a pharmaceutically acceptable carrier therefor.
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