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    Pharmaceutical combinations
    2.
    发明授权
    Pharmaceutical combinations 有权
    药物组合

    公开(公告)号：US08916552B2

    公开(公告)日：2014-12-23

    申请号：US12445180

    申请日：2007-10-12

    Applicant: Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    Inventor： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    IPC: A61K31/535 ,  A61K31/497 ,  A01N43/40 ,  A61K31/435 ,  A61K31/445 ,  A01N43/56 ,  A61K31/415 ,  A01N43/38 ,  A61K31/40 ,  C07D209/44 ,  A61K45/06 ,  A61K31/4035 ,  A61K31/403

    CPC classification number: A61K31/403 ,  A61K31/4035 ,  A61K45/06 ,  A61K2300/00

    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound 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 combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase inhibitors.

    Abstract translation: 本发明提供包含（或基本上由）一种或多种辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2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; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任意取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 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。 这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶抑制剂的活性。

    Pharmaceutical compounds
    5.
    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

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

    Inventor： 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: C07D403/06 ,  A61K31/497

    CPC classification number: 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

    Abstract: 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.

    Abstract translation: 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。

    Non-contact pressure sensing using laser-induced dielectric breakdown
    8.
    发明授权
    Non-contact pressure sensing using laser-induced dielectric breakdown 失效
    使用激光诱导电介质击穿的非接触式压力感测

    公开(公告)号：US08240215B2

    公开(公告)日：2012-08-14

    申请号：US12781262

    申请日：2010-05-17

    Applicant: Ray Glynn Holt ,  Todd William Murray ,  Jonathan Robert Sukovich

    Inventor： Ray Glynn Holt ,  Todd William Murray ,  Jonathan Robert Sukovich

    IPC: G01L9/00

    CPC classification number: G01L11/02

    Abstract: A technique for measuring pressure of a material directs one or more laser beams at the material (e.g., a pressurized fluid) to create a distribution of electromagnetic field intensity which varies over an intensity range and induces dielectric breakdown in the material. An emission pattern of broadband light from the dielectric breakdown is detected, and a value of a characteristic of the emission pattern (e.g., location of a threshold intensity or of a peak intensity) is processed (e.g., by a computer or similar electronic processor) to generate a pressure measurement signal representing a pressure of the material. Processing typically employs a pre-established calibration function which associates a set of stored values of the characteristic with corresponding known pressures of the material, obtained for example by preceding similar measurements of the same material under conditions of known pressures.

    Abstract translation: 用于测量材料压力的技术将材料（例如，加压流体）上的一个或多个激光束引导以产生在强度范围内变化的电磁场强度的分布并且诱导材料中的电介质击穿。 检测来自电介质击穿的宽带光的发射图案，并且处理发射图案的特性值（例如，阈值强度或峰值强度的位置）（例如，通过计算机或类似的电子处理器） 以产生表示材料的压力的压力测量信号。 处理通常使用预先建立的校准功能，其将特征的一组存储值与材料的相应已知压力相关联，例如通过在已知压力的条件下通过相同材料的先前相似测量而获得。

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