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24 条记录 (耗时 0.024 秒)

    Triazolopyrimidines and related analogs as HSP90-inhibitors
    22.
    发明授权
    Triazolopyrimidines and related analogs as HSP90-inhibitors 有权
    三唑并嘧啶和相关类似物作为HSP90-抑制剂

    公开(公告)号：US07129244B2

    公开(公告)日：2006-10-31

    申请号：US10946628

    申请日：2004-09-20

    申请人： Srinivas Rao Kasibhatla ,  Kevin D. Hong ,  Marcus F. Boehm

    发明人： Srinivas Rao Kasibhatla ,  Kevin D. Hong ,  Marcus F. Boehm

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

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

    摘要： A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, diastereomer, pharmaceutically acceptable salt or prodrug thereof, Wherein R1 is halogen, —OR11, —SR11 or lower alkyl; R2 is —NHR8; R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —S2—; and R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 4 to 5 substituents, the heteroaryl group is substituted with 3 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, and 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，对映体，非对映异构体，药学上可接受的盐或前药，其中R 1是卤素，-OR 11， -SR 11或低级烷基; R 2是-NHR 8; R 4是-CHR 12 - ， - C（O） - ， - C（S） - ， - S（O） - 或-S < / SUB> - ; R 5是芳基，杂芳基，脂环族或杂环基，其中芳基被4〜5个取代基取代，杂芳基被3〜5个取代基取代，脂环基被3个 至5个取代基，并且杂环基团被3至5个取代基取代。

    Purine inhibitors of fructose 1,6-bisphosphatase
    24.
    发明授权
    Purine inhibitors of fructose 1,6-bisphosphatase 失效
    果糖1,6-二磷酸酶的嘌呤抑制剂

    公开(公告)号：US06284748B1

    公开(公告)日：2001-09-04

    申请号：US09036327

    申请日：1998-03-06

    申请人： Qun Dang ,  Mark D. Erion ,  M. Rami Reddy ,  Edward D. Robinson ,  Srinivas Rao Kasibhatla ,  K. Raja Reddy

    发明人： Qun Dang ,  Mark D. Erion ,  M. Rami Reddy ,  Edward D. Robinson ,  Srinivas Rao Kasibhatla ,  K. Raja Reddy

    IPC分类号： C07F96561

    CPC分类号： C07F9/65616 ,  C07F9/657181

    摘要： Novel purine compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described. wherein A is selected from the group consisting of —NR82, —NHSO2R3, —OR5, —SR5, halo, lower alkyl, —CON(R4)2, guanidino, amidino, —H, and perhaloalkyl; E is selected from the group consisting of —H, halo, lower alkylthio, lower perhaloalkyl, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, —CN, and —NR72; X is selected from the group consisting of -alk-NR—, alkylene, alkenylene, alkynylene, arylene, heteroarylene, -alk-NR-alk-, -alk-O-alk-, -alk-S-alk-, -alk-S—, alicyclicene, heteroalicyclicene, 1,1-dihaloalkylene, —C(O)-alk-, —NR—C(O)—NR′—, -alk-NR—C(O)—, -alk-C(O)—NR—, —Ar-alk-, and -alk-Ar—, all optionally substituted, wherein each R and R′ is independently selected from —H and lower alkyl, and wherein each “alk” and “Ar” is an independently selected alkylene or arylene, respectively; Y is selected from the group consisting of —H, alkyl, alkenyl, alkynyl, aryl, alicyclic, heteroalicyclic, aralkyl, aryloxyalkyl, alkoxyalkyl, —C(O)R3, —S(O)2R3, —C(O)—OR3, —CONHR3, —NR22, and —OR3, all except H are optionally substituted; and pharmaceutically acceptable prodrugs and salts thereof.

    摘要翻译： 描述了以下结构的新型嘌呤化合物及其作为果糖-1,6-二磷酸酶抑制剂的用途，其中A选自-NR82，-NHSO2R3，-OR5，-SR5，卤素，低级烷基，-CON（ R 4）2，胍基，脒基，-H和全卤代烷基; E选自-H，卤素，低级烷硫基，低级全卤代烷基，低级烷基，低级烯基，低级炔基，低级烷氧基，-CN和 - NR72; X选自-alk-NR-，亚烷基，亚烯基，亚炔基，亚芳基，亚杂芳基，-alk-NR-烷基， - 烷基-O-烷基， - 烷基-S-烷基， （O）-NR' - ，-NR-C（O） - ， - 烷基，（C 1 -C 6） - 烷基亚磺酰基， 其中每个R和R'独立地选自-H和低级烷基，并且其中每个“烷基”和“烷氧基” Ar“分别是独立选择的亚烷基或亚芳基; Y选自-H，烷基，烯基，炔基，芳基， 脂环，杂脂环，芳烷基，芳氧基烷基，烷氧基烷基，-C（O）R 3，-S（O）2 R 3，-C（O）-OR 3，-CONHR 3，-NR 22和-OR 3， 和药学上可接受的前药及其盐。