| 摘要 |
A 4-oxo-2-butenoic acid derivative represented by general formula (I) or a pharmaceutically acceptable salt or ester of the same, wherein Ar<1> and Ar<3> represent each phenyl, thienyl or dihydrobenzofuranyl optionally having 1 to 4 substituents; and Ar<2> represents pyridyl, imidazolyl, thiazolyl, pyrimidinyl, pyridazinyl or pyrazinyl wherein an arbitrary hydrogen atom on its heterocycle may be substituted by C1-6 alkyl or C1-6 alkylamino. Because of having a potent antagonism on endothelin which is an endogenous physiologically active peptide, the compound is useful as a drug antagonistic to blood vessel and tracheal muscle contraction in which endothelin participates and, in its turn, as a remedy for human hypertension, pulmonary hypertension, Raynaud's disease, bronchial asthma, arterial sclerosis, acute renal insufficiency, cardiac insufficiency, myocardial infarct, angina pectoris, cerebral infarction, cerebrovascular spasm, gastric ulcer and diabetes. It is also useful as a remedy for reconstriction, prostatic hypertrophy, endotoxin shock, multiple organ failure or disseminated intravascular coagulation caused by endotoxins, ciclosporin-induced renal disorder, and hypertension. |
