PURPOSE: To provide a new compound having angiotensin II antagonistic activity,.highly suppressing angiotonic and vasopressor activity due to angiotensin II, thus useful for treating hypertension, congestive heart failure, cerebral apoplexy, nephropathy, etc.
CONSTITUTION: The objective compound of formula I (X is R1NH, alkyl, alkenyl, aryl, saturated carbon cycle, etc.; Y1 and Y2 are each H, O, S, etc.; Z is CONH, CH2CONH, COCH2CONH, etc.; A1 and A2 are each H, alkyl, alkenyl, aryl, aralkyl, etc. ; R is H, alkyl, alkenyl, etc.; R1 is H, alkyl, cycloalkyl, aryl, etc.), e.g. N-(N-pentyl-N-(2'-(1H-tetrazole-5-yl)biphenyl-4-yl)-methylcarbamoylmethyl)-(R, S)-2-thienylalanine. The compound of the formula I can be obtained by reaction between a compound of formula II (Q is protecting group) and an isocyanate of formula III (G1 is alkyl, aralkyl, etc.) to form a compound of formula IV which is, in turn, deprotected and then hydrolyzed.
SONDA SHUJI
NAKAGAWA HARUTO
UEHATA MASAYOSHI
