| 摘要 |
<p>PURPOSE: To obtain the subject new derivative which is a specific substituted thiazolo[3,2-l]azepine derivative having inhibiting actions on atrial natriuretic peptide hydrolases and angiotensin I converting enzymes and useful for treat ment, prevention, etc., of hypertension and cardiac insufficiency. CONSTITUTION: This is a new substituted thiazolo[3,2-a]azepine derivative of formula I [R<1> is H or a protecting group of thiol group; R<2> is H, a lower alkyl, a (substituted)aryl, a (substituted)heteroaryl, a lower alkoxy or a lower alkylthio; R<3> to R<5> are each H, a lower alkyl, a lower alkoxy, a (substituted)aryl, etc.; R<6> and R<7> are each H or a lower alkyl; R<8> is H, a protecting group of carboxyl group; (m) and (n) are each 0, 1 or 2], having inhibiting actions on atrial natriuretic peptide hydrolases [neutral endopeptidases (NEP)] and angiotensin I converting enzymes (ACE) and useful for prevention, treatment, etc., of hypertension, cardiac insufficiency, etc. The compound is obtained by reacting a substituted thiazolo[3,2-a]azepine derivative of formula II with a compound of formula III (R<1a> is the same kind as that of R<1> ).</p> |
