To obtain a new compound which inhibits an endothelin-converting enzyme and is useful a medicine for treating and preventing diseases caused (estimated to be caused) by the endothelin, such as hypertension, arteriosclerosis, cardiovascular diseases, cerebrovascular diseases, and renal diseases.
A compound of formula I [R1 is a (substituted) heteroaryl; R2 is a (substituted) alkyl, an acyl or the like; R3, R4 are each H, a (substituted) alkyl or the like], for example, N-(3,4-methylkenedioxypheny)-N'-(1- benzylbenzimidazol-2-yl)thiourea. The compound of formula I is produced, for example, by a method comprising reacting an amine directive (acid adduct) of formula II (R11 is R1; R31 is R3; provided that when R11 and R31 have each a reactive group such as amino or OH, the reactive groups are protected) with an isothicocyanate derivative of the formula: SCN-R21 (R21 is R2, provided that when R21 has a reactive group such as amino or OH, the reactive group is protected) to obtain the compound of formula III.
SAJI KITARO
OHASHI NAOHITO
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