| 摘要 |
<p>PURPOSE:To obtain a new dicarboxylic acid derivative having excellent neutral metalloendopeptidase inhibiting action and useful as an agent for the treatment of hypertension and cardiac insufficiency. CONSTITUTION:The compound of formula I [R is H, lower alkyl, phenyl or OH; R'' is 1-10C alkyl or lower alkyl substituted with aryl, sulfur-containing or nitrogen-containing heterocyclic monocyclic group, etc.; R<2> is (substitutedaryl, 4-8C cycloalkyl or sulfur-containing or nitrogen-containing heterocyclic group; X is O, S or (substituted)imino; Y<1> is imino, O or S and Y<2> is N, or Y<1> is vinylene and Y<2> is CH; (m) is 0-3; (n) is 0 or 1], its ester or their salt, e.g. 4- carboxy-5-{2-[N-((1S)-1-carboxy-3-phenylpropyl)-(L)- phenylalanyl]aminoethyl}thiazole. This compound can be produced by condensing a carboxylic acid of formula II (R<3> is carboxyl-protecting group) or its salt with an amino compound of formula III (R<4> is carboxyl-protecting group) or its salt in the presence of a dehydration agent and optionally removing the protecting group from the condensation product.</p> |
