首页> 外国专利> 2-ANILINO, 4-PYRIDINO s-TRIAZINE BRIDGED COMPOUNDS, INTERMEDIATES FOR THEIR PREPARTION AND THEIR USE AS GSK-3 INHIBITORS

2-ANILINO, 4-PYRIDINO s-TRIAZINE BRIDGED COMPOUNDS, INTERMEDIATES FOR THEIR PREPARTION AND THEIR USE AS GSK-3 INHIBITORS

机译:2-苯胺基,4-吡啶基-s-三嗪桥联化合物的中间体,用作其制备和用作GSK-3抑制剂

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.
机译:本发明涉及式(I)的化合物,其N-氧化物形式,其药学上可接受的加成盐及其立体化学异构形式,其中m代表1,n代表1,Z代表N或C,特别是N; -X1-代表C1-4烷基,特别是甲基; -X2-代表-C1-4烷基-或-C1-4烷基-NR7-,特别是丙基,-乙基-NR7-或-丙基-NR7-; -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-的-C1-6烷基-接头6烷基-CO-NR4-或-Het1-C1-6烷基-CO-NR5-任选地被一个或在可能的情况下两个或多个选自羟基,卤素和苯基的取代基取代; R1代表氢,氯,氟或溴; R 2代表-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;选自吡咯烷基或哌啶基的Het 2,特别是吡咯烷基,其中所述吡咯烷基任选地被羟基取代。

著录项

  • 公开/公告号IL188453B

    专利类型

  • 公开/公告日2012-06-28

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号IL188453

  • 发明设计人

    申请日2007-12-27

  • 分类号C07Dnull/null;

  • 国家 IL

  • 入库时间 2022-08-21 17:24:45

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