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    • 1. 发明申请
      US20100222574A1 CYCLIC ANILINO - PYRIDINOTRIAZINES 有权
    • CYCLIC ANILINO - PYRIDINOTRIAZINES
    • CYCLIC ANILINO - PYRIDINOTRIAZINES
    • US20100222574A1
    • 2010-09-02
    • US11993237
    • 2006-06-26
    • Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
    • Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
    • C07D471/14
    • C07D487/18 , C07D251/16 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 2. 发明授权
      US08778919B2 Cyclic anilino—pyridinotriazines 有权
    • Cyclic anilino—pyridinotriazines
    • 环状苯胺基 - 吡啶并三嗪
    • US08778919B2
    • 2014-07-15
    • US11993237
    • 2006-06-26
    • Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
    • Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
    • A61K31/33 , C07D487/00 , C07D255/02
    • C07D487/18 , C07D251/16 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 3. 发明申请
      US20100160310A1 2,4 (4,6) PYRIMIDINE DERIVATIVES 有权
    • 2,4 (4,6) PYRIMIDINE DERIVATIVES
    • US20100160310A1
    • 2010-06-24
    • US11720681
    • 2005-12-08
    • Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
    • Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
    • A61K31/5377 , C07D471/22 , C07D498/22 , C07D413/14 , A61K31/4985 , A61K31/519 , A61K31/33 , A61P3/10
    • C07D487/18 , C07D487/08 , C07D487/22 , C07D498/08 , C07D498/18
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 6. 发明申请
      US20120065395A1 2,4 (4,6) PYRIMIDINE DERIVATIVES 有权
    • 2,4 (4,6) PYRIMIDINE DERIVATIVES
    • US20120065395A1
    • 2012-03-15
    • US13277651
    • 2011-10-20
    • Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
    • Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
    • C07D239/48 , C07D405/12 , C07D403/12
    • C07D487/18 , C07D487/08 , C07D487/22 , C07D498/08 , C07D498/18
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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