Amide derivatives.

摘要

Amide derivatives of the formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="13" wi="74" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein either R<Sup>1</Sup> is aryl or heterocyclic and A is a direct link, or R<Sup>1</Sup> is aryl or heterocyclic, or hydrogen, or halogeno, hydroxy, amino, guanidino, mercapto, carboxy, carbamoyl, or a substituted derivative thereof, and A<Sup>1</Sup> is alkylene, alkenylene, cycloalkylene or cycloalkenylene; wherein X is carbonyl or hydroxymethylene or substituted derivatives thereof; wherein A<Sup>2</Sup> is alkylene, alkenylene or alkylidene; wherein R<Sup>2</Sup> is hydrogen or alkyl which is unsubsituted or which bears an aryl substituent, or R<Sup>2</Sup> has the formula -Q<Sup>2-</Sup>R<Sup>20</Sup> as defined below; wherein R<Sup>3</Sup> is hydrogen, alkyl or a carbonyl-containing group; wherein R<Sup>4</Sup> is hydrogen or alkyl which is unsubstituted or which bears a halogeno, hydroxy, amino, guanidino, carboxy, carbamoyl, mercapto, alkoxy, alkylamino, dialkylamino, cyclic amino, alkylthio, alkanoylamino, alkoxycarbonylamino, alkoxycarbonyl, aryl or heterocyclyl substituent; wherein -NR<Sup>5</Sup>-CR<Sup>6</Sup>R<Sup>16</Sup>-Q<Sup>1</Sup>-R<Sup>10</Sup> is an amino acid residue, <Sup>R5,</Sup> R<Sup>6</Sup> and R<Sup>16</Sup> being defined in claim 1, wherein Q<Sup>1</Sup> and Q<Sup>2</Sup>, which may be the same or different, each is carbonyl (-CO-) or methylene (-CH<Sub>2</Sub>-); and wherein R<Sup>10</Sup> and R<Sup>20</Sup>, which may be the same or different, is hydroxy, amino or a substituted derivative thereof or hydroxyamino or arylthio; or a salt thereof where appropriate; processes for their manufacture and pharmaceutical compositions containing them. The compounds are inhibitors of angiotensin converting enzyme and may be used in the treatment of hypertension.