利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

30 条记录 (耗时 0.058 秒)

    Pharmaceutical Compounds
    16.
    发明申请
    Pharmaceutical Compounds 审中-公开
    药物化合物

    公开(公告)号：US20080167309A1

    公开(公告)日：2008-07-10

    申请号：US11572305

    申请日：2005-07-22

    申请人： Valerio Berdini ,  Theresa Rachael Early ,  Michael Alistair O'Brien ,  Andrew James Woodhead ,  Paul Graham Wyatt

    发明人： Valerio Berdini ,  Theresa Rachael Early ,  Michael Alistair O'Brien ,  Andrew James Woodhead ,  Paul Graham Wyatt

    IPC分类号： A61K31/535 ,  A61K31/445 ,  A61K31/497 ,  A61K31/425 ,  A61K31/44

    CPC分类号： C07D275/03 ,  C07D277/56 ,  C07D417/12 ,  C07D417/14

    摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): and salts, tautomers, N-oxides or solvates thereof, wherein A is a bond, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; Q is S or CR2; J is S or CH; provided that one of Q and J is S, and the other of Q and J is not S; when Q is S, there is a double bond between the ring carbon atoms “a” and “b” and a double bond between the ring nitrogen N and J; and when J is S, there is a double bond between Q and the ring carbon atom “a” and a double bond between the ring nitrogen N and the ring carbon atom “b”; and R1 to R4 are as defined in the claims.

    摘要翻译： 本发明提供一种用于预防或治疗由细胞周期蛋白依赖性激酶介导的疾病状态或病症的化合物，具有式（I）的化合物及其盐，互变异构体，N-氧化物或溶剂合物，其中A为 键，CO，NR（CO）或O（CO），其中R为氢或任选被羟基取代的C 1-4烃基 或C 1-4烷氧基; Y是长度为1,2或3个碳原子的键或亚烷基链; Q是S或CR <2>; J为S或CH; 假设Q和J中的一个是S，Q和J中的另一个不是S; 当Q是S时，环碳原子“a”和“b”之间有双键，环氮N与J之间有双键; 当J为S时，Q与环碳原子“a”之间存在双键，环氮N与环碳原子“b”之间具有双键。 和R 1至R 4如权利要求中所定义。

    Pharmaceutical compounds
    17.
    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。