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    Pyrazolopyrimidines and related analogs as HSP90-inhibitors
    6.
    发明授权
    Pyrazolopyrimidines and related analogs as HSP90-inhibitors 有权
    吡唑并嘧啶类和相关类似物作为HSP90-抑制剂

    公开(公告)号：US07148228B2

    公开(公告)日：2006-12-12

    申请号：US10946637

    申请日：2004-09-20

    申请人： Srinivas Rao Kasibhatla ,  Marco A. Biamonte ,  Kevin D. Hong ,  David Hurst ,  Marcus F. Boehm

    发明人： Srinivas Rao Kasibhatla ,  Marco A. Biamonte ,  Kevin D. Hong ,  David Hurst ,  Marcus F. Boehm

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P37/06 ,  A61P29/00

    CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D473/00

    摘要： A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R1 is halogen, —OR1, —SR11 or lower alkyl; R2 is —NHR8; R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8, —CN, —C(O)R9, —CO2H, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R4 is —CHR12—, —C(O), —C(S), —S(O)—, or —SO2—; R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents.

    摘要翻译： 由式I表示的化合物或其多晶型物，酯，互变异构体，对映异构体，药学上可接受的盐或前体药物：其中：R 1是卤素，-OR 1， - 或低级烷基; R 2是-NHR 8; R 3选自氢，卤素，-SR 8，-OR 8，-CN，-C（O） R 9，-CO 2 H，-NO 2，-NR 8 R 10，低级烷基，低级链烯基 ，低级炔基，低级全卤代烷基，芳基，杂芳基，脂环族和杂环基，全部是任选取代的，其中：芳基，杂芳基，脂环族和杂环基团任选是单，双或三环的R 4 > - > - ， - C（O）， - （S），-S（O） - 或-SO 2 - 。 R 5是芳基，杂芳基，脂环族或杂环基，其中芳基被3〜5个取代基取代，杂芳基被2〜5个取代基取代，脂环基被3〜 5个取代基，杂环基团被3至5个取代基取代。