To obtain the subject new compound having excellent vasopressin antagonism, and useful as a preventive/therapeutic agent for congestive heart failure, edema (esp. cerebral edema), arginine vasopressin oversecretion syndrome, hypertension, etc., and as a diuretic.
This new compound is shown by formula I [R1 to R6 (except R5) are each H, a lower alkyl, etc.; R5 is H, a lower alkyl, phenyl, etc.; A1 is O, S or NR7; R7 is H or a lower alkyl; A2 is CR8R9; r R8 and R9 are each H, OH, a lower alkyl, etc.; A3 is O, S, NR11 or a single bond; R11 is H or a lower alyl; Z is a halogen, heterocycle, etc.; (m) is 0-6], e.g. N-{2-(2- chloroethoxy)-4-[(5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepin-4-yl) carbonyl]phenyl}-[1,1'-biphenyl]-2-carboxamide. This compound is obtained by the following process: using a compound of formula II as starting material, the compound of formula II is made into a compound of formula III through 6 to 7 processes followed by reaction of the compound of formula III with a compound of the formula Hal-(CH2)m-Z (Hal is a halogen).
WAKITANI YUKIKIYO
JPH08143565A | 1996-06-04 |
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