Piperazine derivatives and pharmaceuticals containing the same

Details Piperazine derivatives and pharmaceuticals containing the same Piperazine derivatives and pharmaceuticals containing the same

C - Chemistry, Metallurgy

07

D

C07D 295/155 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 209/18 (2006.01) C07D 209/42 (2006.01) C07D 213/38 (2006.01) C07D 213/80 (2006.01) C07D 215/26 (2006.01) C07D 243/08 (2006.01) C07D 249/14 (2006.01) C07D 257/04 (2006.01) C07D 257/06 (2006.01) C07D 277/18 (2006.01) C07D 277/46 (2006.01) C07D 295/088 (2006.01) C07D 295/092 (2006.01) C07D 295/13 (2006.01) C07D 295/15 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 417/12 (2006.01) C07D

Patent

CA 2113449

- 67 - ABSTRACT A piperazine derivative represented by the fol- lowing formula (I): Image (I) wherein B represents a phenyl or pyridinyl group, m stands for an integer of 2 or 3, p stands for an in- teger of 1 or 2, R1 represents a hydrogen or halogen atom, A represents -COOR2, -Y-(CH2)n-R3, Image , Image , Image , 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, 1H- tetrazole, 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 - 68 - 3,5-dimethyl-4-hydroxyphenyl group), X represents CH or a nitrogen atom and R6 represents a hydrogen atom or a lower alkoxyl group, Image or Image 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 there- of. 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 anti- asthmatic drug.

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