PIPERAZINE DERIVATIVES AND PHARMACEUTICALS CONTAINING THE SAME

摘要

A piperazine derivative represented by the following formula (I): <IMG> (I) wherein B represents a phenyl or pyridinyl group, m stands for an integer of 2 or 3, p stands for an integer of 1 or 2, R1 represents a hydrogen or halogen atom, A represents -COOR2, -Y-(CH2)n-R3, <IMG> , <IMG> , <IMG> , in which R2 represents a hydrogen atom or a lower alkyl group, Y represents a sulfur or oxygen atom, NH or ?CONH- (? indicates a bond with a (CH2)m group), n stands for an integer of 0-3, R3 represents a cyano, amino, hydroxymethyl, 1Htetrazole, 1-imidazolylcarbonyl, -CO-COOR4, -(CH2)?-COOR4 or -(CH2)?-CONH-R5 group (R4: hydrogen atom or lower alkyl group; e: integer of 0 to 3; and R5: 1H-tetrazole, thiazol-2-yl, thiazolin-2-yl, triazol-5-yl, trimethoxyphenyl or 3,5-dimethyl-4-hydroxyphenyl group), X represents CH or a nitrogen atom and R6 represents a hydrogen atom or a lower alkoxyl group, <IMG> or <IMG> with the proviso that either case where R1, B, p, m and A represent a hydrogen atom, a phenyl group, 1, 2 and -NH-C6H4-COOR4, respectively, or where R1, B, p, m and A represent a chlorine atom, a phenyl group, 1, 2 and -O-CH2COOH, respectively is excluded; or a salt thereof. The compound according to the present invention has strong antihistamic and antiallergic effects and also a high degree of safety so that it is useful as an antihistamic agent, antiallergic agent and/or antiasthmatic drug.