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    Hydroxybenzamide Derivatives And Their Use As Inhibitors Of HSP90
    6.
    发明申请
    Hydroxybenzamide Derivatives And Their Use As Inhibitors Of HSP90 有权
    羟基苯甲酰胺衍生物及其作为HSP90抑制剂的用途

    公开(公告)号：US20070276026A1

    公开(公告)日：2007-11-29

    申请号：US11680805

    申请日：2007-03-01

    申请人： Gianni Chessari ,  Miles Congreve ,  Martyn Frederickson ,  Christopher Murray ,  Eva Navarro ,  Alison Woolford

    发明人： Gianni Chessari ,  Miles Congreve ,  Martyn Frederickson ,  Christopher Murray ,  Eva Navarro ,  Alison Woolford

    IPC分类号： A61K31/40 ,  C07D209/00

    CPC分类号： C07D401/12 ,  C07C65/21 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10

    摘要： The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof, wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.

    摘要翻译： 本发明提供式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物，其中R 1是羟基或氢; R 2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R 3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5 - 烃氧基; R 4选自氢; 其中n为0或1且R 7为任选取代的无环C 1 - （O）N - ， - -5个烃基或具有3〜7个环成员的单环碳环或杂环基; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。 该化合物具有作为Hsp90抑制剂的活性。