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    Phenyl substituted triazoles and their use as selective inhibitors of akl5 kinase
    6.
    发明申请
    Phenyl substituted triazoles and their use as selective inhibitors of akl5 kinase 审中-公开
    苯基取代的三唑及其作为akl5激酶的选择性抑制剂的用途

    公开(公告)号：US20050014938A1

    公开(公告)日：2005-01-20

    申请号：US10495414

    申请日：2002-11-14

    申请人： Laramie Gaster ,  John Harling ,  Jag Heer ,  Thomas Heightman ,  Andrew Payne

    发明人： Laramie Gaster ,  John Harling ,  Jag Heer ,  Thomas Heightman ,  Andrew Payne

    IPC分类号： A61K31/4192 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/538 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P3/12 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P43/00 ,  C07D249/06 ,  C07D265/36 ,  C07D285/14 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D417/02 ,  C07D413/02 ,  C07

    CPC分类号： C07D285/14 ,  C07D249/06 ,  C07D265/36 ,  C07D471/04

    摘要： Phenyl substituted triazoles of formula (I) wherein R1 is naphthyl or phenyl optionally substituted with one or more substituents selected from halo, —O—C1-6alkyl, —S—C1-6alkyl, C1-6alkyl, C1-6haloalkyl, —O—(CH2)n-Ph, —S—(CH2)n-Ph, cyano, phenyl, and CO2R, wherein R is hydrogen or C1-6alkyl, and n is 0, 1, 2 or 3; or R1 is phenyl or pyridyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C1-6 alkyl, and wherein the cyclic ring may be optionally substituted by ═O; R2 and R3 are independently selected from H, C1-6alkyl, C1-6alkoxy, phenyl, NH(CH2)n-Ph, NH—C1-6alkyl, halo, alkoxy, CN, NO2, CONHR and SO2NHR; two of X1, X2 and X3 are N and the other is NR4 wherein R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl, —(CH2)p—CN, —(CH2)p—CO2H, —(CH2)p—CONHR5R6, —(CH2)pCOR5, —(CH2)q(CR7)2, —(CH2)pOR5, (CH2)qCH═CH—CN, —(CH2)q—CH═CH—CO2H, —(CH2)p—CH═CH—CONHR5R6, —(CH2)pNHCOR8 or —(CH2)pNR9R10; R5 and R6 are independently hydrogen or C1-6alkyl; R7 is C1-6alkyl; R8 is C1-7alkyl, or optionally substituted aryl, heteroaryl, arylC1-6alkyl or heteroaryl C1-6alkyl; R9 and R10 are independently selected from hydrogen, C1-6alkyl, aryl and arylC1-6alkyl; p is 0-4; and q is 1-4 and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.

    摘要翻译： 式（I）的苯基取代的三唑，其中R 1是萘基或任选被一个或多个选自卤素，-OC 1-6烷基，-S-C 1-6烷基，C 1-6烷基，C 1-6卤代烷基，-O- （CH 2）n-Ph，-S-（CH 2）n-Ph，氰基，苯基和CO 2 R，其中R是氢或C 1-6烷基，n是0,1,2或3; 或R 1是与5-7个成员的芳族或非芳族环的稠合的苯基或吡啶基，其中所述环任选地含有至多三个独立地选自N，O和S的杂原子，并且N可以进一步任选地被C1 -6烷基，并且其中所述环状环可以任选地被= O取代; R2和R3独立地选自H，C1-6烷基，C1-6烷氧基，苯基，NH（CH2）n-Ph，NH-C1-6烷基，卤素，烷氧基，CN，NO2，CONHR和SO2NHR; X1，X2和X3中的两个是N，另一个是NR4，其中R4是氢，C1-6烷基，C3-7环烷基， - （CH2）p-CN， - （CH2）p-CO2H， - （CH2）p-CONHR5R6 ， - （CH2）pCOR5， - （CH2）q（CR7）2， - （CH2）pOR5，（CH2）qCH = CH-CN， - （CH2）q-CH = CH-CO2H， - （CH2） CH = CH-CONHR5R6， - （CH2）pNHCOR8或 - （CH2）p