JAROSKOVA, LIBUSE,杰斯可,傑斯可,LINDERS, JOANNES THEODORUS MARIA,林德思,林德思,VAN DER VEKEN, LOUIS JOZEF ELISABETH,肯陆思,肯陸思,WILLEMSENS, GUSTAAF HENRI MARIA,威马斯,威馬斯,BISCHOFF, FRANCOIS PAUL,彼戚甫,彼戚甫
申请号：
TW094129417
公开号：
TWI365067B
申请日:
2005.08.29
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, S, NR6, SO or SO2 R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy- R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of &mdashO&mdashCH2&mdash (a), &mdashNR7&mdashCH2&mdash (b), &mdash(CR8R9)m- (c) and &mdashCR10&boxH (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR13R14 or C1-4alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR15R16 R6 represents hydrogen R11 and R12 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl- R13 and R14 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl- R15 and R16 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl- R17 and R18 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-.本發明係有關一種式(I)化合物其N-氧化物型、醫藥上可接受之加成鹽類與立體化學異構型,其中n為1、2、3或4;Z代表O、S、NR6、SO或SO2;R1代表氫、氰基、羥基或C1-4烷基,其可視需要經鹵基取代,或在R3與R2共同結合形成式-CR10=之三價基團之情況時,R1代表一鍵結;R2代表氫、C1-4烷基或C1-4烷基氧-;R3代表氫、C1-4烷基、C1-4烷基氧-或R3與R2共同結合形成選自下列所組成群中之二價或三價基團:-O-CH2-(a)、-NR7-CH2-(b)、-(CR8R9)m-(c)與-CR10=(d),其中m代表1或2,R7、R8、R9與R10分別獨立選自:氫或C1-4烷基;R4代表氫、鹵基、羥基、氰基、胺基、NR11R12、C1-4烷基氧-,其可視需要經一個或若可能時,經二個或三個選自羥基與鹵基之取代基取代,或R4代表C1-4烷基,其可視需要經一個或若可能時,經二個或三個選自羥基與鹵基之取代基取代;R5代表氫、鹵基、氰基、胺基、苯基、羥基、C1-4烷基氧羰基、羥基羰基、N
