利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

5 条记录 (耗时 0.022 秒)

    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