abstract |
ABSTRACT This invention relates to a biphenylmethane derivative represented by the following formula (I): (I) wherein A represents a group or in which R1 represents a hydrogen atom, a lower alkyl group, a lower-cycloalkyl group, a substituted or un-substituted phenyl group, a substituted or un-substituted aralkyl group, a substituted or un-substituted acyl group or an amino acid residue; X represents an oxygen atom or a sulfur atom, Y represents a nitrogen atom or a group =CR2-, Z represents an oxygen atom, a nitrogen atom or a group =CR3-, said Y and Z not being hetero atoms at the same time, R2 and R3 each independently represents a hydrogen atom, a halogen atom, a substituted or un-substituted lower alkyl group, a protected or un-protected carboxyl group, a lower-cyclo alkyl group, a lower alkenyl group, a lower alkoxyl group, a lower alkylthio group or an aryl group or R2 and R3 may form a substituted or unsubstituted benzene ring together with the adjacent carbon atoms; and B represents a cyano group, a protected or unprotected carboxyl group or a protected or unprotected tetrazol-5-yl group; or a salt thereof. The compound has a potent angiotensin II antagonist activity and antihypertensive effect so that it is useful as a therapeutic for circulatory diseases such as hypertension, heart diseases and cerebral apoplexy. |