FREYNE, EDDY JEAN EDGARD,费 艾迪,費 艾迪,WILLEMS, MARC,魏 玛可,魏 瑪可,TEN HOLTE, PETER,贺 彼得,賀 彼得,PAPANIKOS, ALEXANDRA,艾 利亚,艾 利亞,EMBRECHTS, WERNER CONSTANT JOHAN,尹 温尔,尹 溫爾,STORCK, PIERRE HENRI,史 皮尔,史 皮爾,PONCELET,
申请号：
TW102141302
公开号：
TWI511970B
申请日:
2005.12.07
申请国别(地区):
TW
年份:
2015
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-NR13-C1-5alkyl-, -C1-5alkyl-NR14-CO-C1-5alkyl-, -C1-2alkyl-NR21-H2-CO-NH-C1-3alkyl- or -C1-2alkyl-NR23-CO-CR16R17-NH- X1represents O or -O-C1-2alkyl- X2represents a direct bond, C1-2alkyl, -CO-C1-2alkyl or NR12-C1-2alkyl R1represents hydrogen or halo R2represents halo, acetylene or Het1R3represents hydrogen or cyano R4represents Ar4-C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy- R7represents hydrogen or C1-4alkyl R8represents C1-4alkyl substituted with NR25R26or C1-4alkylsulfonyl R12represents hydrogen or C1-4alkyl- R13represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl R16and R17represents hydrogen, C1-4alkyl or R16and R17taken together with the carbon atom to which they are attached from a C3-6cycloalkyl R23represents C1-4alkyl and R23represents hydrogen when R16and R17taken together with the carbon atom to which they are attached from a C3-6cycloalkyl R25, R26, R27and R28each independently represent hydrogen or C1-4alkylcarbonyl Het1represents 2-bora-1,3-dioxolanyl Het2represents piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl or 1,1-dioxothiomotpholinyl wherein said Het2is optionally substituted with C1-4alkyloxycarbonyl or NR27R28-C1-4alkyl Ar4and Ar5represents phenyl Ar6represents phenyl optionally substituted with nitro.本發明係關於下式之化合物其N-氧化物形式、藥學上可接受的加成鹽及立體化學異構物形式,其中Z代表NH;Y代表-C3-9烷基-、-C1-5烷基-NR13-C1-5烷基-、-C1-5烷基-NR14-CO-C1-5烷基-、-C1-2烷基-NR21-H2-CO-NH-C1-3烷基-或-C1-2烷基-NR23-CO-CR16R17-NH-;X1代表O或-O-C1-2烷基-;X2代表直接鍵、C1-2烷基、-CO-C1-2烷基或NR12-C1-2烷基;R1代表氫或鹵基;R2代表鹵基、乙炔基或Het1;R3代表氫或氰基;R4代表Ar4-C1-4烷氧基-、C1-4烷氧基-或經一或兩個或多個選自Het2、NR7R8、羥基及C1-4烷氧基-C1-4烷氧基-之取代基取代之C1-4烷氧基;R7代表氫或C1-4烷基;R8代表經NR25R
