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Home Vasodialators Substituted-N-carboxymethyl-aminoacylaminoalkanoic-acids-useful-as-antihypertensive-agents

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 Substituted N-carboxymethyl-aminoacylaminoalkanoic acids useful as antihypertensive agents

Details
Inventors: Parsons, William H.; Taub, David;
Assignee: Merck & Co., Inc. (Rahway, NJ)
Primary Examiner: Ford; John M.
Assistant Examiner:
Attorney, Agent or Firm: Mitri; Salvatore C., Sudol; Michael C.

Compounds of the formula: ##STR1## where R.sup.3 is ##STR2## where n is 1-3 and the R.sup.a 's and R.sup.b 's are independently hydrogen or loweralkyl; and pharmaceutically acceptable salts thereof; are inhibitors or angiotensin I converting enzyme useful as antihypertensive agents.

DETAILED DESCRIPTION OF THE INVENTION AND PREFERRED EMBODIMENTS In its broadest aspect, the present invention relates to novel substituted N-carboxymethyl-aminoacylaminoalkanoic acid compounds of the formula: ##STR3## wherein: R is hydrogen; loweralkyl; aralkyl; aryl; or mono- or di-substituted aryl wherein the substituents are chloro; R.
sup.
1 is hydrogen; alkyl of from 1 to 12 carbon atoms which include branched, cyclic and unsaturated alkyl groups; substituted loweralkyl wherein the substituent can be halo, hydroxy, carboxy, carboxamido, loweralkylthio, loweralkoxy, loweralkoxycarbonyl, loweraralkoxycarbonyl, amino, loweralkylamino, lowerdialkylamino, acylamino; substituted loweralkylamino wherein the substituent can be halo, hydroxy, alkoxy or cyano; arloweralkylamino; cyclic amino; oxo, thio or ureido; aryloxy; arylthio; aralkyloxy; aralkylthio; benzofused cycloalkyl or bicycloalkyl of from 8-12 carbon atoms; aryl or heteroaryl which may be mono-, di- or trisubstituted by loweralkyl, hydroxy, loweralkoxy, halo, amino, acylamino, loweralkylthio or aminoloweralkyl; benzofused cycloalkyl or bicycloalkyl of from 8 to 12 carbon atoms; arloweralkyl; arloweralkenyl; heteroloweralkyl and heteroloweralkenyl in which the aryl or heteroaryl rings may be mono-, di- or tri-substituted by halo, loweralkyl, hydroxy, loweralkoxy, amino, loweralkylamino, diloweralkylamino, aminoloweralkyl, acylamino, carboxy, haloloweralkyl, nitro, cyano or sulfonamido; aralkyl or heteroaralkyl which include branched loweralkyl groups; substituted aralkyl or substituted heteroaralkyl which include branched loweralkyl groups wherein the loweralkyl groups can be substituted by amino, acylamino, or hydroxyl and the aryl and heteroaryl groups can be substituted by halo, dihalo, loweralkyl, hydroxy, loweralkoxy, aryloxy, aroyl, arylthio, amino, aminoloweralkyl, loweralkanoylamino, aroylamino, lowerdialkylamino, loweralkylamino, hydroxy, hydroxyloweralkyl, trihaloloweralkyl, nitro, cyano, or sulfonamido; any of the arloweralkyl or alkenyl and heteroloweralkyl or alkenyl groups described above in which the aryl or heteroaryl ring is partially or completely hydrogenated; substituted loweralkyl having the formula R



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