PURPOSE: To provide a new amino acid derivative which inhibits the activity of human plasma resin and are useful for controlling renin-dependent hypertension or hyperaldosteronism.
CONSTITUTION: The compound of formula I, e.g. 2S-(4-amino-piperidinocarbonyl- Phe-β A1a-amino)-1-cyclohexyl-6-methylheptan-3R,4S-diol, is obtained by allowing a carboxylic acid of formula II to react with a compound of formula III. In the formula I, X is H, R5-OCmH2m-CO-, R5-Cm-H2m-CO-, R5-SO2-, etc.; W is CH2, O, NH; R1 is H, A; R2, R3, R5 are each H, A, Ar, Ar-alkyl, Het, cycloalkyl, bi- or tri-cycloalkyl, etc.; Ar is substitutable phenyl, naphthyl; Het is a saturated or unsaturated 5- or 6-membered heterocyclic group having 1-4 N, O and/or S, which may be fused to a benzene ring and may have substituent; A is an alkyl.
KURAUSU YOTSUTO SHIYUMITSUCHIE
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