PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF

摘要

The present invention relates to new piperazine derivatives having the general formula (I): wherein R1 or a R2 are the same or different or a each represent a hydrogen atom, a substituted or unsub- stituted C1-C8 alkyl group, a substituted or unsub- stituted C3-C6 cycloalkyl group, a substituted or unsubstituted C2-C8 unsaturated alkyl. group, a ketone group, a substituted or unsubstituted aryl group, a substituted or unsubstituted C1-C4 alkoxy group, a substituted or unsubstituted arylhydroxy group, a substituted or unsubstituted amino group, a C1-C4 ester group, a C1-C4 thioester group, a thiol group, a substituted or unsubstituted carboxyl. group, an epoxy group, or a substituted or unsubstituted C1-C4 thio- alkoxy group, or R1 or a R2 are fused to form a C3-C4 saturated or unsaturated chain; R3, R4, R5, R6 or a R7 are the same or different or a each represent a hydrogen atom, a halogen atom, a hydroxy group, a nitro group, a C1-C4 ester group, a lower alkyl group, a C1-C4 thio- alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a lower alkoxy group, a C1-C4 thioalkoxy group, a substituted or unsubstituted aryl group, a substituted or unsubstituted lower arylalkoxy group, a substituted or unsubstituted lower alkylamino group, or a lower alkyl substituted or unsubstituted carbamate group; or two adjacent groups among R3, R4, R5, R6 or a R7 are bonded with each other to form a 1,2- -194- phenylene or 2,3-naphthylene group; X is an oxygen or sulfur atom, or a substituted or unsubstituted imino group; Y is bonded at the 3-position or 4-position of the aromatic ring or a represents an oxygen atom or -NR8- in which R8 has the same meaning as R3; Z is a hydroxy group, a lower alkoxy group, a C1-C4 thioalkoxy group, a substituted or unsubstituted aryloxy group, a lower alkylamino group, or a substituted or unsubsti- tuted cycloamino containing 1-5 nitrogen atoms; A is a nitrogen atom or -CH=; or a their pharmaceutically acceptable acid addition salt. The compounds of formula (i) are useful for the prevention or treatment of tumors in mammals.