PURPOSE: To provide a new compound having excellent neutral metalloendopeptidase-inhibitory activity, useful as a hypotensive agent or a medicine for heart failure.
CONSTITUTION: The objective compound of formula I (R is H, lower alkyl or formyl; X is O or S), e.g. N-[(1S)-1-benzyloxycarbonyl-2-(3-indolyl)ethyl)-(L)- phenylalanine p-methoxybenzyl ester. The compound of the formula I can be obtained by condensation reaction between a carboxylic acid of formula II (R" is carboxyl-protecting group) and an amine compound of formula III (R2 is carboxyl-protecting group) in the presence of a dehydrating agent (e.g. carbodiimide). The compound of the present invention, which has diuretic activity, vasodilative activity, renin secretion-suppressive activity, aldosterone secretion-suppressive activity, etc., is useful for treating/preventing hypertension, heart failure, renal insufficiency, etc.
WO/1992/009586 | ACTIVE OXYGEN INHIBITOR |
WO/2011/002951 | COMPOSITIONS FOR TREATING BACTERIAL INFECTIONS |
JPS56133278 | 2-IMINOTHIAZOLIDINE DERIVATIVE AND ITS PREPARATION |
YANO KOJI
OMORI KENJI
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