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    CYCLIC ANILINO - PYRIDINOTRIAZINES
    1.
    发明申请
    CYCLIC ANILINO - PYRIDINOTRIAZINES 有权
    CYCLIC ANILINO - PYRIDINOTRIAZINES

    公开(公告)号：US20100222574A1

    公开(公告)日：2010-09-02

    申请号：US11993237

    申请日：2006-06-26

    申请人： Frederik Jan Rita Rombouts ,  Christopher John Love ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Tongfei Wu

    发明人： Frederik Jan Rita Rombouts ,  Christopher John Love ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Tongfei Wu

    IPC分类号： C07D471/14

    CPC分类号： C07D487/18 ,  C07D251/16 ,  C07D401/04 ,  C07D471/18 ,  C07D471/22 ,  C07D487/08

    摘要： 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.

    摘要翻译： 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。

    Cyclic anilino—pyridinotriazines
    2.
    发明授权
    Cyclic anilino—pyridinotriazines 有权
    环状苯胺基 - 吡啶并三嗪

    公开(公告)号：US08778919B2

    公开(公告)日：2014-07-15

    申请号：US11993237

    申请日：2006-06-26

    申请人： Frederik Jan Rita Rombouts ,  Christopher John Love ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Tongfei Wu

    发明人： Frederik Jan Rita Rombouts ,  Christopher John Love ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Tongfei Wu

    IPC分类号： A61K31/33 ,  C07D487/00 ,  C07D255/02

    CPC分类号： C07D487/18 ,  C07D251/16 ,  C07D401/04 ,  C07D471/18 ,  C07D471/22 ,  C07D487/08

    摘要： 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.

    摘要翻译： 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。

    2,4 (4,6) PYRIMIDINE DERIVATIVES
    3.
    发明申请
    2,4 (4,6) PYRIMIDINE DERIVATIVES 有权

    公开(公告)号：US20100160310A1

    公开(公告)日：2010-06-24

    申请号：US11720681

    申请日：2005-12-08

    申请人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Frederik Jan Rita Rombouts

    发明人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Frederik Jan Rita Rombouts

    IPC分类号： A61K31/5377 ,  C07D471/22 ,  C07D498/22 ,  C07D413/14 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/33 ,  A61P3/10

    CPC分类号： C07D487/18 ,  C07D487/08 ,  C07D487/22 ,  C07D498/08 ,  C07D498/18

    摘要： 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 Z1 and Z2 represent NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C1-5alkyl-NR6—C1-5alkyl-, —C1-5alkyl-NR7—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-2alkyl-CO-Het10-CO—, —C1-3alkyl-NH—CO-Het3-, -Het4-C1-3alkyl-CO—NH—C1-3alkyl-, —C1-2alkyl-NH—CO-L1-NH—, —NH—CO-L2-NH—, —C1-2alkyl-CO—NH-L3-CO—, —C1-2alkyl-NH—CO-L1-NH—CO—C1-3alkyl-, —C1-2alkyl-CO—NH-L3-CO—NH—C1-3alkyl-, —C1-2alkyl-NR11—CH2—CO—NH—C1-3alkyl-, Het5-CO—C1-2alkyl-, (C1-5alkyl-CO—NH—C1-3alkyl-CO—NH, —C1-5alkyl-NR13—CO—C1-3alkyl-NH—, —C1-3alkyl-NH—CO-Het27-CO—, or —C1-3alkyl-CO-Het28-CO—NH—; X1 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR16—C1-2alkyl-, —CO—NR17—, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR18—C1-2alkyl-, —CO—NR19—, Het24—C1-2alkyl- or C1-2alkyl; R1 and R5 each independently represent hydrogen, halo, C1-6alkyloxy- or C1-6alkyloxy- substituted with Het1 or C1-4alkyloxy-; R2 and R4 each independently represent hydrogen or halo; R3 represents hydrogen or cyano; R6, R7, R13, R17 and R19 represent hydrogen; R11 represents hydrogen or C1-4alkyl; R16 and R18 represent hydrogen, C1-4alkyl or Het17-C1-4alkyl-; L1, L2 and L3 each independently represents C1-8alkyl optionally substituted with one or where possible two or more substituents selected from phenyl, methylsulfide, cyano, polyhaloC1-4alkyl-phenyl-, C1-4alkyloxy, pyridinyl, mono- or di(C1-4alkyl)-amino- or C3-6cycloalkyl; Het1, Het2, Het17 each independently represent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het3, Het4, Het5 each independently represent morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl; Het10 represents piperazinyl, piperidinyl, pyrrolidinyl or azetidinyl; Het22 represents morpholinyl, oxazolyl, isoxazolyl or piperazinyl wherein said Het22 is optionally substituted with C1-4alkyl; Het23 and Het24 each independently represent a heterocycle selected from pyrrolidinyl, piperazinyl or piperidinyl wherein said Het23 or Het24 are optionally substituted with Het22-carbonyl; Het27 and Het28 each independently represent a heterocycle selected from morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl.

    2,4 (4,6) PYRIMIDINE DERIVATIVES
    6.
    发明申请
    2,4 (4,6) PYRIMIDINE DERIVATIVES 有权

    公开(公告)号：US20120065395A1

    公开(公告)日：2012-03-15

    申请号：US13277651

    申请日：2011-10-20

    申请人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Frederik Jan Rita Rombouts

    发明人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Kristof Van Emelen ,  Sven Franciscus Anna Van Brandt ,  Frederik Jan Rita Rombouts

    IPC分类号： C07D239/48 ,  C07D405/12 ,  C07D403/12

    CPC分类号： C07D487/18 ,  C07D487/08 ,  C07D487/22 ,  C07D498/08 ,  C07D498/18

    摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z1 and Z2 represent NH; Y represents —C3-9alkyl-, —C3-9 alkenyl-, —C1-5alkyl-NR6—C1-5alkyl-, —C1-5alkyl-NR7—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-2alkyl-CO-Het10-CO—, —C1-3alkyl-NH—CO-Het3-, -Het4-C1-3alkyl-CO—NH—C1-3alkyl-, —C1-2alkyl-NH—CO-L1-NH—, —NH—CO-L2-NH—, —C1-2alkyl-CO—NH-L3-CO—, —C1-2alkyl-NH—CO-L1-NH—CO—C1-3 alkyl-, —C1-2alkyl-CO—NH-L3-CO—NH—C1-3alkyl-, —C1-2alkyl-NR11—CH2—CO—NH—C1-3alkyl-, Het5-CO—C1-2alkyl-, —C1-5alkyl-CO—NH—C1-3alkyl-CO—NH—, —C1-5alkyl-NR13—CO—C1-3alkyl-NH—, —C1-3alkyl-NH—CO-Het27-CO—, or —C1-3alkyl-CO-Het28-CO—NH—; X1 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR16—C1-2alkyl-, —CO—NR17—, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR18—C1-2alkyl-, —CO—NR19—, Het24-C1-2alkyl- or C1-2alkyl; R1 and R5 each independently represent hydrogen, halo, C1-6alkyloxy- or C1-6alkyloxy- substituted with Het1 or C1-4alkyloxy-; R2 and R4 each independently represent hydrogen or halo; R3 represents hydrogen or cyano; R6, R7, R13, R17 and R19 represent hydrogen; R11 represents hydrogen or C1-4alkyl; R16 and R18 represent hydrogen, C1-4alkyl or Het17-C1-4alkyl-; L1, L2 and L3 each independently represents C1-8alkyl optionally substituted with one or where possible two or more substituents selected from phenyl, methylsulfide, cyano, polyhaloC1-4alkyl-phenyl-, C1-4alkyloxy, pyridinyl, mono- or di(C1-4alkyl)-amino- or C3-6cycloalkyl; Het1, Het2, Het17 each independently represent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het3, Het4, Het5 each independently represent morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl; Het10 represents piperazinyl, piperidinyl, pyrrolidinyl or azetidinyl; Het22 represents morpholinyl, oxazolyl, isoxazolyl or piperazinyl wherein said Het22 is optionally substituted with C1-4alkyl; Het23 and Het24 each independently represent a heterocycle selected from pyrrolidinyl, piperazinyl or piperidinyl wherein said Het23 or Het24 are optionally substituted with Het22-carbonyl; Het27 and Het28 each independently represent a heterocycle selected from morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl.