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    • 5. 发明授权
    • Cyclic anilino—pyridinotriazines
    • 环状苯胺基 - 吡啶并三嗪
    • US08778919B2
    • 2014-07-15
    • US11993237
    • 2006-06-26
    • Frederik Jan Rita RomboutsChristopher John LoveKristof Van EmelenSven Franciscus Anna Van BrandtTongfei Wu
    • Frederik Jan Rita RomboutsChristopher John LoveKristof Van EmelenSven Franciscus Anna Van BrandtTongfei Wu
    • A61K31/33C07D487/00C07D255/02
    • 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; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-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; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 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; -X1-表示C1-4烷基,特别是甲基; -X2-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-代表-NR2-C1-6烷基-CO-NR4-,-Het1-C1-6烷基-CO-NR5-或-Het2-CO-NR6-,其中-NR2-C1- C 1-6烷基-CO-NR 4 - 或-Het 1 -C 1-6烷基-CO-NR 5 - 任选被一个或其中可能的两个或更多个选自羟基,卤素和苯基的取代基取代; R1代表氢,氯,氟或溴; R 2表示-C 1-4烷基,特别是乙基或甲基; R7代表氢; R8代表氢; R4,R5和R6代表氢; Het1选自哌嗪基或哌啶基,特别是哌嗪基; Het2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。
    • 6. 发明申请
    • CYCLIC ANILINO - PYRIDINOTRIAZINES
    • CYCLIC ANILINO - PYRIDINOTRIAZINES
    • US20100222574A1
    • 2010-09-02
    • US11993237
    • 2006-06-26
    • Frederik Jan Rita RomboutsChristopher John LoveKristof Van EmelenSven Franciscus Anna Van BrandtTongfei Wu
    • Frederik Jan Rita RomboutsChristopher John LoveKristof Van EmelenSven Franciscus Anna Van BrandtTongfei Wu
    • C07D471/14
    • 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; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-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; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 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; -X1-表示C1-4烷基,特别是甲基; -X2-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-NR2-C1-6烷基-CO-NR4-,-Het1-C1-6烷基-CO-NR5-或-Het2-CO-NR6-,其中-NR2-C1- C 1-6烷基-CO-NR 4 - 或-Het 1 -C 1-6烷基-CO-NR 5 - 任选被一个或其中可能的两个或更多个选自羟基,卤素和苯基的取代基取代; R1代表氢,氯,氟或溴; R 2表示-C 1-4烷基,特别是乙基或甲基; R7代表氢; R8代表氢; R4,R5和R6代表氢; Het1选自哌嗪基或哌啶基,特别是哌嗪基; Het2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。