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    Bioluminescence imaging of myeloperoxidase activity in vivo, methods, compositions and apparatuses therefor
    3.
    发明授权
    Bioluminescence imaging of myeloperoxidase activity in vivo, methods, compositions and apparatuses therefor 有权
    骨髓过氧化物酶活性的生物发光成像，其方法，组合物和装置

    公开(公告)号：US08652442B2

    公开(公告)日：2014-02-18

    申请号：US13127448

    申请日：2009-11-03

    申请人： David Piwnica-Worms ,  Shimon Gross ,  Vijay Sharma ,  Seth Gammon

    发明人： David Piwnica-Worms ,  Shimon Gross ,  Vijay Sharma ,  Seth Gammon

    IPC分类号： A61B5/00 ,  C07D237/30

    CPC分类号： C12Q1/28 ,  A61K49/0013

    摘要： Methods of imaging distribution of myeloperoxidase activity in a subject are disclosed. These methods include the use of bioluminescent substrates, including luminol and wavelength-shifted analogues of luminol. Bioluminescent myeloperoxidase substrates that emit light at longer wavelengths compared to luminol are shown to be useful for imaging myeloperoxidase activity in vivo. The disclosed methods can be used for imaging sites of inflammation and other pathological conditions associated with abnormal levels of MPO activity in vivo. Methods of synthesis of luminol analogues are also disclosed.

    摘要翻译： 公开了在受试者中成像骨髓过氧化物酶活性分布的方法。 这些方法包括使用生物发光底物，包括鲁米诺和鲁米诺的波长偏移类似物。 显示出比鲁米诺更长波长发光的生物发光髓过氧化物酶底物可用于体内髓过氧化物酶活性成像。 所公开的方法可用于与体内MPO活性异常水平相关的炎症和其他病理状况的成像部位。 还公开了鲁米诺类似物的合成方法。

    PHTHALAZINONE DERIVATIVES
    9.
    发明申请
    PHTHALAZINONE DERIVATIVES 失效
    邻苯二酚衍生物

    公开(公告)号：US20090069303A1

    公开(公告)日：2009-03-12

    申请号：US12271308

    申请日：2008-11-14

    申请人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Sylvie Gomez ,  Marc Geoffrey Hummersone ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Xiao-Ling Fan Cockcroft ,  Frank Kerrigan

    发明人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Sylvie Gomez ,  Marc Geoffrey Hummersone ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Xiao-Ling Fan Cockcroft ,  Frank Kerrigan

    IPC分类号： A61K31/551 ,  C07D237/30 ,  A61K31/502 ,  C07D253/06 ,  A61K31/53 ,  A61P9/00 ,  A61P29/00 ,  A61P3/10 ,  A61P25/00 ,  A61P35/00 ,  C07D413/14 ,  A61K31/5377 ,  C07D243/08

    CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

    摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2. RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.

    摘要翻译： 式（I）的化合物：其中：A和B一起表示任选取代的稠合芳环; D选自：（i）其中Y1选自CH和N，Y2选自CH和N，Y3选自CH，CF和N; 和（ii）其中Q为O或S; RD是：其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2，CRC3RC4和C-O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4独立地选自H，R，C（-O）OR，其中R是任选取代的C 1-10烷基，任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRC1RC2。 RC1和RC2独立地选自H，R，C（-O）OR，其中R是任选取代的C 1-10烷基，任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时，RN1和RC2可以与它们所结合的N和C原子一起形成任选被取代的C5-7杂环; 并且当X是CRC3RC4时，RC2和RC4可以一起形成附加键，使得在被RC1和RC3取代的原子之间存在双键。