PURPOSE: To obtain a new mercapto-amido derivative and a salt thereof having double inhibitory activity against neutral endopeptidase EC 3.4.24.11 and angiotensinase, thus useful as a medicine.
CONSTITUTION: This mercapto-amido derivative (and a salt thereof) is expressed by formula I [R1 is a lower alkyl, cyclo(lower)alkyl, aryl or heterocycle; R2 is a heterocycle, lower alkyl or H; X is S, -, or lower alkylene; Y is -, or lower alkylene; (n) is 0 or 1], e.g. N-[(S)-2-mercaptomethylpentanoyl]-3-(1,3- benzothiazol-2-yl)-(S)-alanine. The compound of formula I is obtained by reaction between a compound of formula II and a compound of formula III. Of the compounds of formula I, a compound of formula IV is esp. preferable. This new compound is useful for preventing and treating various cardiovascular disorders such as hypertension, heart failure and stenocardia, renal failure, periodic edema, hyperaldosteronism, hypercalciuria, etc.
TAKIMOTO KOICHI
TAKENAKA KOHEI
KOBAYASHI YUIKO
OKITSU OSAMU
