ROMBOUTS, FREDERIK JAN RITA,罗芮塔,羅芮塔,LOVE, CHRISTOPHER JOHN,罗乔恩,羅喬恩,VAN EMELEN, KRISTOF,范艾伦,范艾倫,VAN BRANDT, SVEN FRANCISCUS ANNA,范安娜,范安娜,WU, TONGFEI,吴同飞,吳同飛
申请号：
TW095123449
公开号：
TWI457340B
申请日:
2006.06.29
申请国别(地区):
TW
年份:
2014
代理人:
摘要：
The present invention concerns the compounds of formulatheN-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomerc forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N -X1- represents C1-4alkyl, in particular methyl -X2- represents -C1-4alkyl- or -C1-4alky1-NR7-, in particular propyl, -ethyl-NR7- or -propyl-NR7- -Y- represents-NR2-C1-6alkyl-CO-NR4-, -Het1-C1-6alkyl-CO-NR5- or -Het2-CO-NR6- and wherein the -C1-6alkyl- linker of -NR2-C1-6alkyl-CO-NR4- or -Het1-C1-6alkyl-CO-NR5- is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl R1represents hydrogen, chloro, fluoro or bromo R2represents -C1-4alkyl-, in particular ethyl or methyl R7represents hydrogen R8represents hydrogen R4, R5and R6represent hydrogen Het1is selected from piperazinyl or piperidinyl, in particular -piperazinyl Het2selected from pyrrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.本發明有關一種下式之化合物其N-氧化物形式、醫藥上可接受之加成鹽及立體化學異構形式,其中m係表示1,n係表示1,Z係表示N或C,尤其是N;-X1-係表示C1-4烷基,尤其是甲基;-X2-係表示-C1-4烷基-或-C1-4烷基-NR7-,尤其丙基、-乙基-NR7-或-丙基-NR7-;-Y-係表示-NR2-C1-6烷基-CO-NR4-、-Het1-C1-6烷基-CO-NR5-或-Het2-CO-NR6-且其中-NR2-C1-6烷基-CO-NR4-或-Het1-C1-6烷基-CO-NR5-之-C1-6烷基-鍵合基係視情況經一或若可能則兩個或更多個選自羥基、鹵基及苯基之取代基所取代;R1係表示氫、氯、氟或溴;R2係表示-C1-4烷基-,尤其是乙基或甲基;R7係表示氫;R8係表示氫;R4、R5及R6係表示氫;Het1係選自六氫吡基或六氫吡啶基,尤其是-六氫吡基;Het2係選自吡咯啶基或六氫吡啶基,尤其是吡咯啶基,其中該吡咯啶基係視情況經羥基所取代。
