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1. 发明申请

WO2010129258A3 TISSUE SEALANT COMPOSITIONS, VASCULAR CLOSURE DEVICES, AND USES THEREOF 审中-公开
标题翻译：组织密封组合物，血管闭合装置及其用途
公开(公告)号：WO2010129258A3
公开(公告)日：2011-06-30
申请号：PCT/US2010032519
申请日：2010-04-27
申请人： MALLINCKRODT INC , BASORE JR BOB O , NEUMANN WILLIAM L , DORSHOW RICHARD B , RAJAGOPALAN RAGHAVAN
发明人： BASORE JR BOB O , NEUMANN WILLIAM L , DORSHOW RICHARD B , RAJAGOPALAN RAGHAVAN
IPC分类号： A61L24/04
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，其用于组织密封和/或凝块形成的光学检测。本发明的组合物和装置包括随着组合物和/或装置结合到组织密封和/或凝块中而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脉管系统封闭装置可用于在例如在外科手术期间或之后，导管移除等之后可视化密封和/或凝块形成。本发明还提供用于组织密封件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件或脉管系统穿刺闭合件的形成和光学检测的医疗套件。

2. 发明申请

WO2009061473A3 PHOTONIC SHELL-CORE CROSS LINKED AND FUNCTIONALIZED NANOSTRUCTURES FOR BIOLOGICAL APPLICATIONS 审中-公开
标题翻译：光子壳体生物应用的交联和功能化纳米结构
公开(公告)号：WO2009061473A3
公开(公告)日：2009-11-05
申请号：PCT/US2008012575
申请日：2008-11-07
申请人： MALLINCKRODT INC , UNIV WASHINGTON , NEUMANN WILLIAM L , RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B , FRESKOS JOHN N , SHIEH JENG JONG , WOOLEY KAREN L , SEUNG LEE NAM
发明人： NEUMANN WILLIAM L , RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B , FRESKOS JOHN N , SHIEH JENG JONG , WOOLEY KAREN L , SEUNG LEE NAM
IPC分类号： A61K47/48 , C08F8/12 , C08F8/32
CPC分类号： C08F8/00 , A61K47/6907 , C08F2800/10 , C08F2800/20
摘要： The present invention provides optical agents comprising optically functional cross linked supramolecular structures and assemblies useful for a range of imaging, diagnostic, and therapeutic applications. Supramolecular structures and assemblies of the present invention include optically functional shell-cross linked micelles wherein optical functionality is achieved via incorporation of one or more linking groups that include one or more photoactive moieties. The present invention further includes imaging, sensing and therapeutic methods using one or more optical agents of the present invention including optically functional shell cross-linked micelles. The present invention includes in situ monitoring methods, for example, wherein physical and/or structural changes in an optically functional shell-cross linked micelle generated in response to changes in chemical environment or physiological conditions causes a measurable change in the wavelengths or intensities of emission from the micelle.
摘要翻译：本发明提供包含光学功能交联的超分子结构和用于一系列成像，诊断和治疗应用的组件的光学剂。本发明的超分子结构和组件包括光学功能的壳交联胶束，其中通过引入一个或多个包含一个或多个光活性部分的连接基团来实现光学官能团。本发明还包括使用包括光学功能的壳交联胶束的本发明的一种或多种光学剂的成像，感测和治疗方法。本发明包括原位监测方法，例如，其中响应于化学环境或生理条件变化产生的光学功能的壳交联胶束的物理和/或结构变化导致发射波长或强度的可测量的变化从胶束。

3. 发明申请

WO2010037069A3 DITHIENOPYRROLE DYES FOR IMAGING AND THERAPY 审中-公开
标题翻译：二噻吩并吡喃染料成像与治疗
公开(公告)号：WO2010037069A3
公开(公告)日：2010-06-10
申请号：PCT/US2009058680
申请日：2009-09-29
申请人： MALLINCKRODT INC , RAJAGOPALAN RAGHAVAN , NEUMANN WILLIAM L , POREDDY AMRUTA , FRESKOS JOHN N , DORSHOW RICHARD B
发明人： RAJAGOPALAN RAGHAVAN , NEUMANN WILLIAM L , POREDDY AMRUTA , FRESKOS JOHN N , DORSHOW RICHARD B
IPC分类号： C09B57/00 , G01N33/533 , G01N33/58
CPC分类号： C09B57/00 , A61K41/0057 , A61K49/0021 , G01N2458/00
摘要： The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienopyrrole core. In some embodiments, dyes of the present invention are dithienopyrrole dyes having a dithienopyrrole core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.
摘要翻译：本发明提供了光学试剂，包括组合物，制剂和制剂，以及使用和制造光学试剂的方法。本发明的光学剂包括具有含二噻吩并吡喃核心的稠环骨架结构的染料及其衍生物。在一些实施方案中，本发明的染料是二噻吩并吡咯染料，其具有任选官能化的二噻吩并吡咯核以提供有用的光学，生物学，药代动力学和/或物理性质。

4. 发明申请

WO2008108941A3 INTEGRATED PHOTOACTIVE PEPTIDES AND USES THEREOF 审中-公开
标题翻译：整合的光敏肽及其用途
公开(公告)号：WO2008108941A3
公开(公告)日：2008-12-31
申请号：PCT/US2008002463
申请日：2008-02-26
申请人： MALLINCKRODT INC , RAJAGOPALAN RAGHAVAN , NEUMANN WILLIAM L , DORSHOW RICHARD B
发明人： RAJAGOPALAN RAGHAVAN , NEUMANN WILLIAM L , DORSHOW RICHARD B
IPC分类号： A61K41/00 , A61K49/00 , A61P35/00 , C07K1/00 , C07K7/06 , C07K7/08
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：本发明涉及将已知结构和功能的生物活性化合物转化成光活性分子从而保持原始生物活性的一般方法。将光活性和生物功能的两个基本性质整合到单个分子实体中产生的分子在下文中一般称为“整合光活性类似物”或“整合光活性肽或假肽”。设计整合光敏类似物的一般方法主要涉及：（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区域;和（c）用具有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敏性。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。

5. 发明申请

WO2010037068A3 DITHIENOFURAN DYES FOR IMAGING AND THERAPY 审中-公开
标题翻译： DITHIENOFURAN染料成像和治疗
公开(公告)号：WO2010037068A3
公开(公告)日：2010-11-18
申请号：PCT/US2009058679
申请日：2009-09-29
申请人： MALLINCKRODT INC , RAJAGOPALAN RAGHAVAN , NEUMANN WILLIAM L , POREDDY AMRUTA , FRESKOS JOHN N , DORSHOW RICHARD B
发明人： RAJAGOPALAN RAGHAVAN , NEUMANN WILLIAM L , POREDDY AMRUTA , FRESKOS JOHN N , DORSHOW RICHARD B
IPC分类号： C09B57/00
CPC分类号： C07D497/14 , A61K41/0057 , A61K49/0021 , A61K49/005 , A61K49/0054 , A61K49/0056 , C09B57/00
摘要： The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienofuran core. In some embodiments, dyes of the present invention are dithienofuran dyes having a dithienofuran core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.
摘要翻译：本发明提供了光学试剂，包括组合物，制剂和制剂，以及使用和制造光学试剂的方法。本发明的光学剂包括具有含二噻吩并呋喃核心的稠环骨架结构的染料及其衍生物。在一些实施方案中，本发明的染料为二噻吩并呋喃染料，其具有任选官能化的二噻吩并呋喃核心以提供有用的光学，生物学，药代动力学和/或物理性质。

6. 发明申请

WO2008108944A3 INTEGRATED PHOTOACTIVE SMALL MOLECULES AND USES THEREOF 审中-公开
标题翻译：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
申请人： MALLINCKRODT INC , NEUMANN WILLIAM L , RAJAGOPALAN RAGHAVAN , MOORE DENNIS A , DORSHOW RICHARD B
发明人： NEUMANN WILLIAM L , RAJAGOPALAN RAGHAVAN , MOORE DENNIS A , DORSHOW RICHARD B
IPC分类号： A61K41/00 , A61K49/00 , C07D241/26
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。

7. 发明申请

WO2007149478A2 PYRAZINE DERIVATIVES WITH EXTENDED CONJUGATION AND USES THEREOF 审中-公开
标题翻译：具有扩展性结合的吡嗪衍生物及其用途
公开(公告)号：WO2007149478A2
公开(公告)日：2007-12-27
申请号：PCT/US2007014369
申请日：2007-06-20
申请人： MALLINCKRODT INC , NEUMANN WILLIAM L , RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B
发明人： NEUMANN WILLIAM L , RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B
IPC分类号： C07D241/20 , C07D241/24 , C07D241/28 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/04 , C07D417/04
CPC分类号： C07D405/04 , A61K49/0021 , C07D241/12 , C07D241/20 , C07D241/24 , C07D241/26 , C07D241/28 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/04 , C07D417/04 , C07D473/18 , C07D473/34
摘要： The present invention relates to pyrazine derivatives capable of absorbing and emanating spectral energy in the visible and/or near infrared spectrum. Pyrazine derivatives of the invention may be administered to a patient in the form of a pharmaceutically acceptable composition and utilized in medical (e.g., diagnostic imaging) procedures.
摘要翻译：本发明涉及能够吸收和发出可见光和/或近红外光谱中的光谱能量的吡嗪衍生物。本发明的吡嗪衍生物可以以药学上可接受的组合物的形式施用于患者，并用于医学（例如，诊断成像）程序中。

8. 发明申请

WO2006071759A3 FLUORESCENT PYRAZINE DERIVATIVES AND METHODS OF USING THE SAME IN ASSESSING RENAL FUNCTION 审中-公开
标题翻译：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
申请人： MALLINCKRODT INC , RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B , NEUMANN WILLIAM L , MOORE DENNIS A
发明人： RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B , NEUMANN WILLIAM L , MOORE DENNIS A
IPC分类号： C07D241/26 , A61K31/4965
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. 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.
摘要翻译：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。

9. 发明申请

WO2011031955A3 OPTICAL MONITORING OF LEUKEMIA 审中-公开
标题翻译：光学监测
公开(公告)号：WO2011031955A3
公开(公告)日：2011-06-23
申请号：PCT/US2010048409
申请日：2010-09-10
申请人： MALLINCKRODT INC , RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B
发明人： RAJAGOPALAN RAGHAVAN , DORSHOW RICHARD B
IPC分类号： A61K41/00 , A61K49/00 , A61P35/02
CPC分类号： A61K41/0057 , A61B5/0071 , A61B5/4842
摘要： The invention relates to compounds, methods and devices for targeting of optical agents to leukemia affected cells or tissues in a subject. Compounds of the invention include conjugates and bioconjugates comprising a targeting moiety and an optical agent. In an aspect of the invention, the targeting moiety is an amino acid sequence which preferentially binds to leukemia cells. In another aspect of the invention, the optical agent is an imaging agent derived from a pyrazine, azulene, or azaazulene dye. In a further aspect of the invention, the optical agent may comprise a photosensitizer. Some methods of the invention relate to administration, activation, and/or monitoring of compounds of the invention. In an aspect, a compound of the invention is administered to a subject, allowed time to target a leukemia affected cell or tissue in the subject, and the fluorescence intensity of the compound in the subject is measured. Some devices of the invention include means for activation, detection and monitoring of compounds of the invention. In an aspect of the invention, a device includes an electromagnetic radiation source, collector, and detector.
摘要翻译：本发明涉及用于将光学剂靶向受试者中受影响的白血病细胞或组织的化合物，方法和装置。本发明的化合物包括缀合物和包含靶向部分和光学剂的生物缀合物。在本发明的一个方面，靶向部分是优先与白血病细胞结合的氨基酸序列。在本发明的另一方面，光学剂是衍生自吡嗪，薁或氮杂薁染料的成像剂。在本发明的另一方面，光学剂可以包含光敏剂。本发明的一些方法涉及本发明化合物的给药，活化和/或监测。一方面，将本发明的化合物给予受试者，允许对受试者的白血病受影响的细胞或组织的时间，并测量受试者中化合物的荧光强度。本发明的一些装置包括用于激活，检测和监测本发明化合物的装置。在本发明的一个方面，一种装置包括电磁辐射源，收集器和检测器。

10. 发明申请

WO2007103250A3 THIADIAZOLE COMPOUNDS AND THEIR USE IN PHOTOTHERAPY 审中-公开
标题翻译：噻吗化合物及其在光合作用中的应用
公开(公告)号：WO2007103250A3
公开(公告)日：2008-03-20
申请号：PCT/US2007005491
申请日：2007-03-02
申请人： MALLINCKRODT INC , RAJAGOPALAN RAGHAVAN , JACOBS FREDERICK G , DORSHOW RICHARD B
发明人： RAJAGOPALAN RAGHAVAN , JACOBS FREDERICK G , DORSHOW RICHARD B
IPC分类号： C07D513/14 , A61K31/00
CPC分类号： C07D513/04
摘要： The current application discloses thidiazole derivatives of Formula (1), compositions thereof and their use for targeting and photoactivation at target sites.
摘要翻译：目前的应用公开了式（1）的噻二唑衍生物，其组合物及其在靶位点靶向和光活化的用途。

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