FREYNE, EDDY JEAN EDGARD,费 艾迪,費 艾迪,VAN EMELEN, KRISTOF,范继道,范繼道,BUIJNSTERS, PETER JACOBUS JOHANNES ANTONIUS,布 彼德,布 彼德,EMBRECHTS, WERNER CONSTANT JOHAN,艾 维纳,艾 維納,PERERA, TIMOTHY PIETRO SUREN,贝 提姆,貝 提姆
申请号：
TW100107837
公开号：
TWI389890B
申请日:
2004.12.17
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
The present invention concerns the compounds of formulatheN-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH Y represents-C3-9alkyl-, -C1-5alkyl-NR12-C1-5alkyl-, -C1-6alkyl-NH-CO- or -CO-NH -C1-6alkyl- X1represents -O- X2represents a direct bond, -NR11-C1-2alkyl-, -NR11-CH2-,-C1-2alkyl-,-O-C1-2alkyl, -O- or-O-CH2- R1represents hydrogen or halo R2represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl-or Ar5 R3represents hydrogen hydroxy, C1-4alkyloxy-, Ar4-C1-4alkyloxy or R3represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2- R10represents hydrogen R11represents hydrogen,-C1-4alkyl- or C1-4alkyl-oxy-carbonyl- R12represents Het14-C1-4alkyl,in particular morpholinyl-C1-4alkyl Het2represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl Het14represents morpholinyl Het16represents a heterocycle selected from morpholinyl or pyrrolidinyl Ar4represents phenyl Ar5represents phenyl optionally substituted with cyano.本發明有關下式之化合物,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Z係表示NH;Y係表示-C3-9烷基-、-C1-5烷基-NR12-C1-5烷基-、-C1-6烷基-NH-CO-或-CO-NH-C1-6烷基-;X1係表示-O-;X2係表示直接鍵結、-NR11-C1-2烷基-、-NR11-CH2-、-C1-2烷基-、-O-C1-2烷基-、-O-或-O-CH2-;R1係表示氫或鹵基;R2係表示氫、氰基、鹵基、羥基羰基-、C1-4烷基氧基羰基-、Het16-羰基或Ar5;R3係表示氫、羥基、C1-4烷基氧基-、Ar4-C1-4烷基氧基或R3係表示經一或可能二或多個選自C1-4烷基氧基-或Het2-之取代基所取代的C1-4烷基氧基;R10係表示氫;R11係表示氫、C1-4烷基-或C1-4烷基-氧基-羰基-;R12係表示Het14-C1-4烷基,尤其是嗎啉基-C1-4烷基;Het2係表示選自視情況經C1-4烷基-(以甲基為佳)所取代之嗎啉基或哌啶基的雜環;Het14係表示嗎啉基;Het16係表示選自嗎啉基或吡咯烷基之雜環;Ar4係表示苯基;Ar5係表示視情況經氰基所取代之苯基。
