A DIARYL BUTYRIC ACID DERIVATIVE AND THE PRODUCTION PROCESS THEREOF

A diaryl butyric acid derivative having the general formula:. whereinR' represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 2 to 4 carbon atoms;R2 represents an alkyl group having 1 to 3 carbon atoms; andX represents a pyrrolidinyl group, a morpholino group, a thiomorpholino group, an amino group, a group having the general formula:whereinA represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, a group having the general formula:whereinB represents a phenyl group, a benzyl group, a aralkyl group having 7 to 9 carbon atoms substituted with or at least one hydroxyl group, a group having the general formula;whereinn is an integer of 0 to 5,D represents a saturated crosslinked ring type hydrocarbon group, a piperidinyl group, a morpholino group, a thiomorpholino group, a pyridyl group, an indolyl group, a piperazinyl group, a pyrrolidinyl group, a carboxyl group, a phenyl group substituted with a hydroxyl, or aryloxy group, an N-[4-(2'-hydroxy-5'-methoxy)phenyl-4-phenyl- butyryl]piperazinyl group, or a piperazinyl group having an alkyl group with 1 to 3 carbon atoms substituted for the hydrogen atom on the nitrogen atom a group having the general formula:whereinm is 2 to 3, f is an integer of 0 to 4, E is a hydrogen atom, a phenyl group, a hydroxyl group, a pyrrolidine-carboxyl group, a 4-(4'-methoxyphenyl)-4-phenylbutylamide group, or a 4-(2'-hyrdroxy-5'-methoxy)phenyl--4-phenylbutyryl group, a group having the general formula:whereinp is an integer of 2 to 4, andF presents a dialkylamino group having 1 to 3 carbon atoms, or a group having the general formula:whereinG represents an aralkyl group having 8 to 9 carbon atoms substituted with at least two hydroxyl groups; or the pharmaceutically acceptable salt thereof.This diaryl butyric acid derivative or the pharmaceutically acceptable salt thereof can be prepared by reacting a benzoxepin derivative having the general formula:whereinR2 is the same as defined above with an amine or alcohol derivative having the general formula;whereinX is the same as defined above in the presence of an acid catalyst at room temperature or at an elevated temperature and, optionally, further reacting the reaction product with an alkylation agent having 1 to 3 carbon atoms or an acylation agent having 2 to 4 carbon atoms, optionally further followed by treated with a pharmaceutically acceptable acid.This diaryl butyric acid derivative or the pharmaceutically acceptable s