Diaryl butyric acid derivative and pharmaceutical use thereof

摘要

A diaryl butyric acid derivative having the general formula: <IMAGE> (I) wherein R1 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; and X represents a variety of substituents. This diaryl butyric acid derivative or the pharmaceutically acceptable salt thereof can be prepared by reacting a benzoxepin derivative having the general formula: <IMAGE> (II) wherein R2 is the same as defined above with an amine or alcohol derivative having the general formula; X-H wherein X is the same as defined above in the presence of an acid catalyst at room temperature or at an elevated temperature and, optionally, further reading the reaction product with an alkylation agent having 1 to 3 carbon atoms or an acylation agent having 2 to 4 carbon atoms. This diaryl butyric acid derivative or the pharmaceutically acceptable salt thereof is effective for ameliorating or treating various symptoms based on cerebral organic disorders and pathergasia.