PURPOSE: To provide a new compound having an angiotensin II antagonizing action and useful for treating hypertension and the like.
CONSTITUTION: A compound of formula I [R1 is CO2H, SO3H, PO3H2 or the like; R2 is H, OH, OCOCH3, a halogen or the like; X is (CH2)mCONH, O, NH or the like; R3 is a 4-9C alkyl, a 4-9C alkenyl or the like; R4 is CONH (1-4C alkyl) or the like; (m) is 0, 1] or its salt, solvate. (R)-1-[1-oxo -2-[4-(2- sulfobenzoyl)amino -1H-imidazol-1-yl]octyl -4-cis-(4-carboxymethylphenoxy)-L- proline. The compound of the formula I is obtained by coupling a compound of formula II with a compound of formula III (R9 is O, S) or the like to reduce the nitro group of the compound of the formula II, and subsequently coupling the obtained aminoimidazole with a compound of formula IV or the like. The compound of the formula I is useful for treating congestive heart insufficiency, dysgnosia, hypertensive renal diseases, renal insufficiency accompanied by diabetes, glaucoma and the like.
HAUSER KENNETH LEE (US)
LIFER SHERRYL LYNN (US)
MARSHALL WINSTON STANLEY (US)
PALKOWITZ ALAN DAVID (US)
PFEIFER WILLIAM (US)
REEL JON KEVIN (US)
SIMON RICHARD LEE (US)
STEINBERG MITCHELL IRVIN (US)
TAKEUCHI KUMIKO (US)
THRASHER KENNETH JEFF (US)
WHITESITT CELIA ANN (US)
