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    • 113. 发明申请
    • CYCLIC ANILINO - PYRIDINOTRIAZINES
    • CYCLIC ANILINO - PYRIDINOTRIAZINES
    • WO2007003525A2
    • 2007-01-11
    • PCT/EP2006/063555
    • 2006-06-26
    • JANSSEN PHARMACEUTICA N.V.ROMBOUTS, Frederik, Jan, RitaLOVE, Christopher, JohnVAN EMELEN, KristofVAN BRANDT, Sven, Franciscus, AnnaWU, Tongfei
    • ROMBOUTS, Frederik, Jan, RitaLOVE, Christopher, JohnVAN EMELEN, KristofVAN BRANDT, Sven, Franciscus, AnnaWU, Tongfei
    • C07D487/18C07D251/16C07D401/04C07D471/18C07D471/22C07D487/08
    • The present invention concerns the compounds of formula (I), the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; -X 1 - represents C 1-4 alkyl, in particular methyl; -X 2 - represents -C 1-4 alkyl- or -C 1-4 alkyl-NR 7 -, in particular propyl, -ethyl-NR 7 - or -propyl-NR 7 -; -Y- represents-NR 2 -C 1-6 alkyl-CO-NR 4 -, -Het 1 -C 1-6 alkyl-CO-NR 5 - or -Het 2 -CO-NR 6 - and wherein the -C 1-6 alkyl- linker of -NR 2 -C 1-6 alkyl-CO-NR 4 - or -Het 1 -C 1-6 alkyl-CO-NR 5 - is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R 1 represents hydrogen, chloro, fluoro or bromo; R 2 represents -C 1-4 alkyl-, in particular ethyl or methyl; R 7 represents hydrogen; R 8 represents hydrogen; R 4 , R 5 and R 6 represent hydrogen; Het 1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het 2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.
    • 本发明涉及式(I)化合物,N-氧化物形式,其药学上可接受的加成盐和立体化学异构形式,其中m表示1,n表示1,Z表示N或C,特别是N; -X 1表示C 1-4烷基,特别是甲基; -X 2 - 表示-C 1-4烷基 - 或-C 1-4 - 烷基-NR 7 - - ,特别是丙基, - 乙基-NR 7 - 或 - 丙基-NR 7 - ; -Y-表示-NR 2 -C 1-6烷基-CO-NR 4 - ,-Het 1 SUP / > -C 1-6烷基-CO-NR 5 - 或-Het 2 -CO-NR 6 - - 并且其中-NR 2 -C 1-6烷基-CO-NR的-C 1-6烷基 - 连接基团, 4 - 或-Het 1 -C 1-6烷基-CO-NR 5 - 任选被一个或多个 可能的两个或更多个选自羟基,卤素和苯基的取代基; R 1表示氢,氯,氟或溴; R 2表示-C 1-4 - 烷基 - ,特别是乙基或甲基; R 7表示氢; R 8表示氢; R 4,R 5和R 6表示氢; Het 1选自哌嗪基或哌啶基,特别是哌嗪基; Het 2选自吡咯烷基或哌啶基,特别是吡咯烷基,其中所述吡咯烷基任选被羟基取代。