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    PYRAZINE DERIVATIVES FOR OPTICAL IMAGING AND THERAPY
    3.
    发明申请
    PYRAZINE DERIVATIVES FOR OPTICAL IMAGING AND THERAPY 审中-公开
    用于光学成像和治疗的吡嗪衍生物

    公开(公告)号：WO2010121003A1

    公开(公告)日：2010-10-21

    申请号：PCT/US2010/031203

    申请日：2010-04-15

    Applicant: MALLINCKRODT INC. ,  NEUMANN, William, L. ,  FRESKOS, John, N. ,  DORSHOW, Richard, B.

    Inventor： NEUMANN, William, L. ,  FRESKOS, John, N. ,  DORSHOW, Richard, B.

    IPC: C07D241/26 ,  C07D241/28 ,  A61B5/00 ,  A61K49/00

    CPC classification number: C07D241/26 ,  A61K31/444 ,  A61K31/497 ,  C07D241/28

    Abstract: The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.

    Abstract translation: 本发明提供化合物，包括组合物，制剂和制剂，以及使用和制备这些化合物的方法。 本发明的化合物包括具有吡嗪核和多个取代基的吡嗪衍生物。 在一些实施方案中，本发明的吡嗪衍生物是具有一个或多个给电子基团和一个或多个吸电子基团的吡嗪核心化合物，其任选被官能化以提供有用的光学，生物学，药代动力学和/或物理性质。

    INTEGRATED PHOTOACTIVE SMALL MOLECULES AND USES THEREOF
    4.
    发明申请
    INTEGRATED PHOTOACTIVE SMALL MOLECULES AND USES THEREOF 审中-公开
    综合光敏小分子及其用途

    公开(公告)号：WO2008108944A3

    公开(公告)日：2008-11-27

    申请号：PCT/US2008002521

    申请日：2008-02-26

    Applicant: MALLINCKRODT INC ,  NEUMANN WILLIAM L ,  RAJAGOPALAN RAGHAVAN ,  MOORE DENNIS A ,  DORSHOW RICHARD B

    Inventor： NEUMANN WILLIAM L ,  RAJAGOPALAN RAGHAVAN ,  MOORE DENNIS A ,  DORSHOW RICHARD B

    IPC: A61K41/00 ,  A61K49/00 ,  C07D241/26

    CPC classification number: A61K49/001 ,  A61K41/0019 ,  A61K47/60 ,  A61K49/0021 ,  A61K49/0052

    Abstract: This invention is directed to the general method of transforming non-photoactive bioactive small molecule compounds of known structure and function into photoactive analogs of the small molecules which exhibit both photoactivity and the original biological targeting activity. The general method for the design of the photoactive analogs of the small molecules includes: (a) selecting a desired bioactive molecule; (b) identifying the region of the molecule that contains an aromatic or a heteroaromatic motif; and (c) either replacing said motif with a photoactive functional group of similar size, or modifying said motif to make it photoactive. Other aspects include photoactive analog compounds and photodiagnostic and phototherapeutic uses thereof.

    Abstract translation: 本发明涉及将具有已知结构和功能的非光活性生物活性小分子化合物转化为具有光活性和原始生物靶向活性的小分子的光活性类似物的一般方法。 设计小分子的光活性类似物的一般方法包括：（a）选择所需的生物活性分子; （b）鉴定含有芳族或杂芳族基序的分子的区域; 和（c）用相似尺寸的光活性官能团取代所述基序，或修饰所述基序以使其具有光活性。 其他方面包括光敏类似物化合物及其光诊断和光治疗用途。

    INTEGRATED PHOTOACTIVE SMALL MOLECULES AND USES THEREOF
    5.
    发明申请
    INTEGRATED PHOTOACTIVE SMALL MOLECULES AND USES THEREOF 审中-公开
    集成的光敏小分子及其用途

    公开(公告)号：WO2008108944A2

    公开(公告)日：2008-09-12

    申请号：PCT/US2008/002521

    申请日：2008-02-26

    Applicant: MALLINCKRODT INC. ,  NEUMANN, William, L. ,  RAJAGOPALAN, Raghavan ,  MOORE, Dennis, A. ,  DORSHOW, Richard, B.

    Inventor： NEUMANN, William, L. ,  RAJAGOPALAN, Raghavan ,  MOORE, Dennis, A. ,  DORSHOW, Richard, B.

    IPC: A61K41/00 ,  A61K49/00 ,  C07D241/26

    CPC classification number: A61K49/001 ,  A61K41/0019 ,  A61K47/60 ,  A61K49/0021 ,  A61K49/0052

    Abstract: This invention is directed to the general method of transforming non-photoactive bioactive small molecule compounds of known structure and function into photoactive analogs of the small molecules which exhibit both photoactivity and the original biological targeting activity. The general method for the design of the photoactive analogs of the small molecules includes: (a) selecting a desired bioactive molecule; (b) identifying the region of the molecule that contains an aromatic or a heteroaromatic motif; and (c) either replacing said motif with a photoactive functional group of similar size, or modifying said motif to make it photoactive. Other aspects include photoactive analog compounds and photodiagnostic and phototherapeutic uses thereof.

    Abstract translation: 本发明涉及将具有已知结构和功能的非光敏生物活性小分子化合物转化为同时显示光活性和原始生物靶向活性的小分子的光活性类似物的一般方法。 设计小分子的光敏类似物的一般方法包括：（a）选择所需的生物活性分子; （b）鉴定含有芳族或杂芳族基序的分子区域; 和（c）用具有相似大小的光敏官能团取代所述基序，或修饰所述基序以使其具有光敏性。 其他方面包括光敏类似物化合物以及它们的光诊断和光治疗用途。

    FLUORESCENT PYRAZINE DERIVATIVES AND METHODS OF USING THE SAME IN ASSESSING RENAL FUNCTION
    7.
    发明申请
    FLUORESCENT PYRAZINE DERIVATIVES AND METHODS OF USING THE SAME IN ASSESSING RENAL FUNCTION 审中-公开
    荧光吡嗪衍生物及其在评价肾功能中的应用方法

    公开(公告)号：WO2006071759A3

    公开(公告)日：2006-09-14

    申请号：PCT/US2005046732

    申请日：2005-12-22

    Applicant: MALLINCKRODT INC ,  RAJAGOPALAN RAGHAVAN ,  DORSHOW RICHARD B ,  NEUMANN WILLIAM L ,  MOORE DENNIS A

    Inventor： RAJAGOPALAN RAGHAVAN ,  DORSHOW RICHARD B ,  NEUMANN WILLIAM L ,  MOORE DENNIS A

    IPC: C07D241/26 ,  A61K31/4965

    CPC classification number: C07D241/28 ,  A61K31/4965 ,  A61K49/0004 ,  A61K49/0021 ,  A61K49/0052 ,  C07D241/20 ,  C07D241/26

    Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II. X 1 to X 4 of Formulas I and II may be characterized as electron withdrawing groups, while Y 1 to Y 4 of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing organ (e.g., kidney) function. In a particular example, an effective amount of a pyrazine derivative that is capable of being renally cleared may be administered into a patient's body. The pyrazine derivative may capable of one or both absorbing and emanating spectral energy of at least about 400nm (e.g., visible and/or infrared light). At least some of the derivative that is in the body may be exposed to spectral energy and, in turn, spectral energy may emanate from the derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.

    Abstract translation: 本发明涉及吡嗪衍生物，例如由式I和II表示的那些。 式I和II的X 1至X 4可以表征为吸电子基团，而Y 1至Y 4可以表示为吸电子基团， 式I和II的SUP可表征为给电子基团。 本发明的吡嗪衍生物可用于评估器官（例如肾）功能。 在一个特定的例子中，可以将有效量的能够被肾脏清除的吡嗪衍生物施用到患者体内。 吡嗪衍生物能够吸收和发出至少约400nm的光谱能量（例如可见光和/或红外光）中的一种或两种。 至少一些在体内的衍生物可能暴露于光谱能量，并且反过来，光谱能量可能从该衍生物发出。 该发出的光谱能量可被检测并用于确定患者的肾功能。

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