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    Pharmaceutical compounds
    1.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US08779132B2

    公开(公告)日：2014-07-15

    申请号：US12445154

    申请日：2007-10-12

    申请人： Miles Stuart Congreve ,  Lynsey Helen Fazal ,  Martyn Frederickson ,  Christopher William Murray ,  Michael Alistair O'Brien ,  Andrew James Woodhead ,  John Francis Lyons ,  Neil Thomas Thompson

    发明人： Miles Stuart Congreve ,  Lynsey Helen Fazal ,  Martyn Frederickson ,  Christopher William Murray ,  Michael Alistair O'Brien ,  Andrew James Woodhead ,  John Francis Lyons ,  Neil Thomas Thompson

    IPC分类号： C07D403/06 ,  A61K31/497

    CPC分类号： C07D403/06 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D215/14 ,  C07D217/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107 ,  C07D491/18

    摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C═O, (C═O)O, (C═O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C═O or (C═O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims. The compounds of formula (VI0) are pro-drugs of parent compounds wherein R1 and/or R2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.

    摘要翻译： 本发明提供了一种用于医药的化合物，该化合物为式（VI0）化合物或其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团：选自结构C1，C5和C6： 其中n为0,1,2或3; R1是氢，羟基或O-Rz; R2a是羟基，甲氧基或O-Rz; 条件是R1和R2a中的至少一个是O-Rz; Rz是Lp-Rp1; SO3H; 葡萄糖苷酸残基; 单，二或三肽残基; 或Lp为键，C = O，（C = O）O，（C = O）NRp1或S（O）xNRp1; x为1或2; Rp1是氢或任选取代的含有0,1或2个碳环和0,1,2,3,4,5或6个碳 - 碳多重键的C1〜25烃基，条件是当Lp为 一个键，C = O或（C = O）O; 并且还提供O-Rz不含有O-O部分; 并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，并且各自为基团Rp1; R3，R4a，R8和R10如权利要求中所定义。 式（VI0）化合物是其中R 1和/或R 2a是羟基的母体化合物的前药，其中母体化合物具有Hsp90抑制活性。