| 摘要 |
<p>Polypeptide derivatives containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues are of the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="23" wi="71" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein, for example in a preferred embodiment R is t-butyloxycarbonyl, m and n are each 0 or 1, their sum being at least 1; R is cyclohexylmethyl; R<Sup>2</Sup> is 2-methylpropyl, 2-methyl-2--propenyl, benzyl, 4-chlorobenzyl, 3-chlorobenzyl, 4-methylbenzyl, 4-methoxybenzyl, 3,4-dichlorobenzyl, 2-chlorobenzyl or cyclohexylmethyl; R<Sup>3</Sup> is hydrogen; R<Sup>4</Sup> is hydrogen, methyl, 4-aminobutyl, 2-carboxyethyl, 3-(ethoxycarbonyl)propyl or 3-(benzyloxycarbonyl)propyl; W is phenylalanyl, W<Sup>1</Sup> is histidyl and W<Sup>2</Sup> is lysyl.</p><p>These compounds are useful for inhibiting the angiotensinogen cleaving action of the enzyme renin having particular utility in the treatment of hypertension.</p> |
