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    Isoxazole Compounds As Inhibitors Of Heat Shock Proteins
    2.
    发明申请
    Isoxazole Compounds As Inhibitors Of Heat Shock Proteins 有权
    异恶唑化合物作为热休克蛋白的抑制剂

    公开(公告)号：US20130289026A1

    公开(公告)日：2013-10-31

    申请号：US13929098

    申请日：2013-06-27

    Applicant: Vernalis (R&D) Limited ,  The Institute of Cancer Research ,  Cancer Research Technology Limited

    Inventor： Martin James Drysdale ,  Brian William Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen Elizabeth James ,  Kwai Ming Cheung ,  Thomas Peter Matthews

    IPC: C07D261/08 ,  C07D413/10

    CPC classification number: A61K31/541 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D261/08 ,  C07D261/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D495/04

    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, —SO.sub.2-, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.

    Abstract translation: 式（A）或（B）的异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症：其中R1是式（IA）的基团：-Ar1-（Alk1）对（Z）r - （Alk2）sQ，其中在任何相容的组合中，Ar 1是任选取代的芳基或杂芳基，Alk1和Alk2是任选取代的二价C 1 -C 6亚烷基或C 2 -C 6亚烯基，p，r和s独立地为0或1， Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ，-SO 2 - ， - C（= O） - ， - C（= S）NRA，-SO 2 NRRA - ， - NRAC（= O） - ，-NRASO 2 - 或-NRA-，其中RA是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或 杂环基; R2是（i）上述式（IA）的基团或（ii）甲酰胺基团; 或（iii）非芳族碳环或杂环，其中环碳任选被取代，和/或环氮任选被式 - （Alk1）对（Z）r-（Alk2）sQ基团取代，其中Q ，Alk1，Alk2，Z，p，r和s如上文关于组（IA）所定义; 并且R 3是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C 6烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团。

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