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    Phenyl substituted triazoles and their use as selective inhibitors of akl5 kinase
    1.
    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

    Chemical compounds
    2.
    发明申请
    Chemical compounds 失效
    化合物

    公开(公告)号：US20060074111A1

    公开(公告)日：2006-04-06

    申请号：US10518778

    申请日：2003-06-18

    申请人： Paul Beswick ,  John Harling ,  Savvas Kleanthous ,  Millard Lambert ,  Vipulkumar Patel ,  Juliet Simpson

    发明人： Paul Beswick ,  John Harling ,  Savvas Kleanthous ,  Millard Lambert ,  Vipulkumar Patel ,  Juliet Simpson

    IPC分类号： C07D213/55 ,  A61K31/44 ,  A61K31/195

    CPC分类号： C07D213/74 ,  C07C217/58 ,  C07C217/80 ,  C07C233/18 ,  C07C255/58 ,  C07C311/08 ,  C07C311/29 ,  C07C323/25 ,  C07C2601/02 ,  C07D239/42 ,  C07D241/20

    摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, Wherein: R1 and R2 are independently hydrogen or C1-3 alkyl; X represents a bond, CH2 or O; R3 and R4 are independently hydrogen, C1-6 alkyl, OCH3, CF3, allyl or halogen; X1 is CH2, SO2, or CO; R5 is —C1-6 alkyl (optionally substituted by C1-6alkoxy or C1-6alkylthio), —C2-6 alkenyl, —C0-6 alkyl phenyl (wherein the phenyl is optionally substituted by one or more CF3, halogen, C1-3 alkyl, C1-3 alkoxy), —COC1-6 alkyl, SO2C1-6 alkyl; R6 is phenyl or a 6 membered heteroaryl group containing 1, 2 or 3 N atoms wherein the phenyl or heteroaryl group is optionally substituted with 1, 2 or 3 moieties selected from the group consisting of C1-6 alkyl, halogen, —OC1-6 alkyl, —SO2C1-3 alkyl, phenyl (optionally substituted by one or more groups selected from halogen, CF3, C1-3 alkyl, OC1-3 alkyl, acetyl, CN).

    摘要翻译： 式（I）化合物或其药学上可接受的盐，溶剂化物或可水解的酯，其中R 1和R 2独立地是氢或C 1 -3 烷基; X表示键，CH 2或O; R 3和R 4独立地是氢，C 1-6烷基，OCH 3，CF 3， 3，烯丙基或卤素; X 1是CH 2，SO 2，或CO; R 5是-C 1-6 - 烷基（任选被C 1-6烷氧基或C 1-6 - 烷基取代） 烷硫基），-C 2-6亚烯基，-C 0-6烷基苯基（其中苯基任选被一个或多个CF 3取代） 卤素，C 1-3烷基，C 1-3烷氧基），-COC 1-6烷基，SO 3 - 2个C 1-6烷基; R 6是苯基或含有1,2或3个N原子的6元杂芳基，其中苯基或杂芳基任选被1,2或3个选自C