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公开(公告)号：US06887854B2
公开(公告)日：2005-05-03
申请号：US10436759
申请日：2003-05-13
申请人： Samuel Achilefu , Hermo N. Jimenez , Raghavan Rajagopalan , Richard B. Dorshow , Joseph E. Bugai
发明人： Samuel Achilefu , Hermo N. Jimenez , Raghavan Rajagopalan , Richard B. Dorshow , Joseph E. Bugai
IPC分类号： C07H15/26 , A61K49/00 , C07D209/08 , C07D209/12 , C07D209/60 , C07D405/14 , A01N43/04 , A61K31/70 , C07D277/04 , C07H15/00
CPC分类号： C07D405/14 , C07D209/08 , C07D209/12 , C07D209/60
摘要： Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
摘要翻译： 公开了在可见光区域吸收和发出荧光的高度亲水的吲哚和苯并吲哚衍生物。 这些化合物可用于生理和器官功能监测。 特别地，本发明的分子可用于肾脏和心脏疾病的光学诊断以及体内血液体积估计。
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公开(公告)号：US08722685B2
公开(公告)日：2014-05-13
申请号：US13343231
申请日：2012-01-04
IPC分类号： A61K31/4965 , C07D241/02
CPC分类号： A61K31/4965 , A61K31/5377 , A61K49/0021 , A61K49/0052 , A61K49/0054 , C07D241/26
摘要： The present invention relates to pyrazine derivatives such as those represented by Formulas I and II below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
摘要翻译： 本发明涉及吡嗪衍生物，例如由下式I和II表示的衍生物。 式I和II化合物的X 1至X 4可以表征为吸电子基团。 相反，式I和II化合物的Y1至Y4可以表征为给电子基团。 本发明的吡嗪衍生物可用于评估肾功能。 特别地，有效量的本发明的吡嗪衍生物可以施用于患者体内。 身体中的吡嗪衍生物可能暴露于可见光和/或红外光，导致光谱能量从吡嗪衍生物中发出。 这种发出的光谱能量可以被检测并用于确定患者的肾功能。
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公开(公告)号：US08664392B2
公开(公告)日：2014-03-04
申请号：US13344930
申请日：2012-01-06
IPC分类号： C07D241/02 , A61K31/497 , A61K31/4965
CPC分类号： A61K41/0057 , A61K47/64 , A61K49/0021 , A61K49/0056 , C07D241/26 , C07D403/12
摘要： Provided are compounds and compositions of general Formula IX: E1-L-Ar—X-PA, that may be utilized in bioconjugation procedures, where Ar is a chromophore and PA is a functional group capable of being attached to any bioactive molecule of interest. The present invention provides Formulas I-III that are capable of being attached to a bioactive vector for the selective delivery of said photoactive pyrazine derivatives to a desired biological target.
摘要翻译： 提供通式IX的化合物和组合物：E1-L-Ar-X-PA，其可用于生物缀合方法，其中Ar是发色团，PA是能够连接到任何目的生物活性分子的官能团。 本发明提供能够连接到生物活性载体上的式I-III，用于将所述光活性吡嗪衍生物选择性递送到期望的生物靶。
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74.发明申请Fluorescent Pyrazine Derivatives and Methods of Using the Same in Assessing Renal Function 有权荧光吡嗪衍生物及其在肾功能评估中的应用方法公开(公告)号：US20140039191A1
公开(公告)日：2014-02-06
申请号：US14047733
申请日：2013-10-07
IPC分类号： C07D241/28 , C07D241/20
CPC分类号： C07D241/28 , A61K31/4965 , A61K49/0004 , A61K49/0021 , A61K49/0052 , C07D241/20 , C07D241/26
摘要： The present invention relates to pyrazine derivatives such as those represented by Formulas I and II. X1 to X4 of Formulas I and II may be characterized as electron withdrawing groups, while Y1 to Y4 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 400 nm (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.
摘要翻译： 本发明涉及吡嗪衍生物，例如由式I和II表示的衍生物。 式I和II的X 1至X 4可以表征为吸电子基团，而式I和II的Y1至Y4可以表征为给电子基团。 本发明的吡嗪衍生物可用于评估器官（例如肾）功能。 在具体实例中，有效量的能够被再次清除的吡嗪衍生物可以被施用到患者体内。 吡嗪衍生物可以具有一个或两个吸收和发射至少约400nm的光谱能量（例如可见光和/或红外光）。 身体中的至少一些衍生物可能暴露于光谱能量，反过来，光谱能量可能来自衍生物。 这种发出的光谱能量可以被检测并用于确定患者的肾功能。
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公开(公告)号：US08313729B2
公开(公告)日：2012-11-20
申请号：US12528630
申请日：2008-02-26
CPC分类号： A61K49/001 , A61K41/0019 , A61K47/60 , A61K49/0021 , A61K49/0052
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20120100078A1
公开(公告)日：2012-04-26
申请号：US13343231
申请日：2012-01-04
IPC分类号： A61K49/00 , C07D413/04 , C08B37/00 , C07D241/28
CPC分类号： A61K31/4965 , A61K31/5377 , A61K49/0021 , A61K49/0052 , A61K49/0054 , C07D241/26
摘要： The present invention relates to pyrazine derivatives such as those represented by Formulas I and II below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
摘要翻译： 本发明涉及吡嗪衍生物，例如由下式I和II表示的衍生物。 式I和II化合物的X 1至X 4可以表征为吸电子基团。 相反，式I和II化合物的Y1至Y4可以表征为给电子基团。 本发明的吡嗪衍生物可用于评估肾功能。 特别地，有效量的本发明的吡嗪衍生物可以施用于患者体内。 身体中的吡嗪衍生物可能暴露于可见光和/或红外光，导致光谱能量从吡嗪衍生物中发出。 这种发出的光谱能量可以被检测并用于确定患者的肾功能。
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77.发明申请公开(公告)号：US20120041479A1
公开(公告)日：2012-02-16
申请号：US13266161
申请日：2010-04-27
IPC分类号： A61B17/03
CPC分类号： A61L24/102 , A61L24/001 , A61L24/0015 , A61L24/0042 , A61L24/046 , A61L24/106 , A61L24/108 , A61L2300/418 , A61L2300/442 , A61L2300/604 , A61L2400/04 , A61L2430/20 , A61L2430/34
摘要： The present invention provides tissue sealant compositions and vasculature closure devices useful for the optical detection of tissue seal and/or clot formation. Compositions and devices of the present invention comprise optical dyes which undergo an observable change as the compositions and/or devices are incorporated into a tissue seal and/or clot, for example a change in fluorescence quantum yield and/or a change in visual color including a change in emission and/or absorption wavelength. Tissue sealants and vasculature closure devices of the present invention are useful for visualizing seal and/or clot formation, for example, during or after surgical procedures, after catheter removal, etc. The present invention further provides methods for formation and optical detection of tissue seals or vasculature puncture closures as well as medical kits useful for the formation and optical detection of tissue seals or vasculature puncture closures.
摘要翻译： 本发明提供组织密封剂组合物和脉管系统闭合装置，其可用于光学检测组织密封和/或凝块形成。 本发明的组合物和装置包括当组合物和/或装置结合到组织密封和/或凝块中时经历可观察到的变化的光学染料，例如荧光量子产率的变化和/或视觉颜色的变化，包括 发射和/或吸收波长的变化。 本发明的组织密封剂和血管闭合装置可用于可视化密封和/或血块形成，例如，在外科手术期间或之后，导管移除之后等。本发明还提供用于组织密封的形成和光学检测的方法 或脉管系统穿刺闭合件以及可用于组织密封或脉管系统穿刺闭合件的形成和光学检测的医疗套件。
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公开(公告)号：US08115000B2
公开(公告)日：2012-02-14
申请号：US11995223
申请日：2007-06-20
IPC分类号： C07D241/02
CPC分类号： A61K31/4965 , A61K31/5377 , A61K49/0021 , A61K49/0052 , A61K49/0054 , C07D241/26
摘要： The present invention relates to pyrazine derivatives such as those represented by Formulas (I) and (II) below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
摘要翻译： 本发明涉及吡嗪衍生物，例如由下式（I）和（II）表示的衍生物。 式I和II化合物的X 1至X 4可以表征为吸电子基团。 相反，式I和II化合物的Y1至Y4可以表征为给电子基团。 本发明的吡嗪衍生物可用于评估肾功能。 特别地，有效量的本发明的吡嗪衍生物可以施用于患者体内。 身体中的吡嗪衍生物可能暴露于可见光和/或红外光，导致光谱能量从吡嗪衍生物中发出。 这种发出的光谱能量可以被检测并用于确定患者的肾功能。
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公开(公告)号：US20100222547A1
公开(公告)日：2010-09-02
申请号：US12528631
申请日：2008-02-26
CPC分类号： A61K41/0042 , A61K49/0021 , A61K49/0056 , C07K1/13 , C07K7/06 , C07K7/08
摘要： This invention is directed to the general method of transforming bioactive compounds of known structure and function into photoactive molecules such that the original biological activity is retained. The molecules resulting from the integration of two fundamental properties of photoactivity and biological function into a single molecular entity are hereinafter generally referred to as ‘integrated photoactive analogs’ or ‘integrated photoactive peptides or pseudopeptides.” The general method for the design of integrated photoactive analogs principally involves: (a) selecting a desired bioactive peptide or pseudopeptide; (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 render it photoactive. Other aspects include photoactive analog compounds and photodiagnostic and phototherapeutic uses thereof.
摘要翻译： 本发明涉及将具有已知结构和功能的生物活性化合物转化为光活性分子的一般方法，使得保留原始生物活性。 由光活性和生物功能的两个基本性质整合到单一分子实体中产生的分子在下文中通常被称为“整合的光活性类似物”或“整合的光活性肽或假肽”。用于设计综合光敏类似物的通用方法 主要涉及：（a）选择所需的生物活性肽或假肽; （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。
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公开(公告)号：US20100113756A1
公开(公告)日：2010-05-06
申请号：US12683851
申请日：2010-01-07
IPC分类号： C07F5/00
CPC分类号： C09K11/06 , A61K49/0013 , C07C237/02 , C07C237/12 , C09K2211/188
摘要： Some embodiments of the present invention may be said to be directed to metal complexes of Formula I wherein at least one of X1, X2, X3, R1, R2, R3, R4 or R5 is what may be characterized as an antenna capable of providing (e.g., absorbing and/or emitting) an appropriate electromagnetic signal. Some embodiments of the present invention are directed to ligands corresponding to metal complexes of Formula I. Some embodiments of the invention are directed to methods of determining renal function using at least one metal complex of Formula I.
摘要翻译： 可以说本发明的一些实施方案涉及式I的金属络合物，其中X 1，X 2，X 3，R 1，R 2，R 3，R 4或R 5中的至少一个可被表征为能够提供（ 例如吸收和/或发射）适当的电磁信号。 本发明的一些实施方案涉及对应于式I的金属配合物的配体。本发明的一些实施方案涉及使用至少一种式I的金属络合物测定肾功能的方法。
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