公开(公告)号：US20080213175A1

公开(公告)日：2008-09-04

申请号：US11901704

申请日：2007-09-17

Applicant: Hartmuth C. Kolb ,  Kai Chen ,  Joseph C. Walsh ,  Umesh Gangadharmath ,  Dhanalakshmi Kasi ,  Bing Wang ,  Brian Duclos ,  Qianwa Liang ,  Henry Clifton Padgett ,  Farhad Karimi

Inventor： Hartmuth C. Kolb ,  Kai Chen ,  Joseph C. Walsh ,  Umesh Gangadharmath ,  Dhanalakshmi Kasi ,  Bing Wang ,  Brian Duclos ,  Qianwa Liang ,  Henry Clifton Padgett ,  Farhad Karimi

IPC: A61K51/08 ,  C07K5/12 ,  A61K38/12 ,  A61K38/14

CPC classification number: C07K7/56

Abstract: The present application is directed to radiolabeled cyclic peptidomimetics, pharmaceutical compositions comprising radiolabeled cyclic peptidomimetics, and methods of using the radiolabeled cyclic peptidomimetics. Such peptidomimetics can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Abstract translation: 本申请涉及放射性标记的环肽模拟物，包含放射性标记的环肽模拟物的药物组合物，以及使用放射性标记的环肽模拟物的方法。 这种肽模拟物可用于成像研究，例如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。

公开(公告)号：US10011632B2

公开(公告)日：2018-07-03

申请号：US14917127

申请日：2012-08-21

Applicant: Eric Wang ,  Hartmuth C. Kolb ,  Anna Katrin Szardenings ,  Changhui Liu ,  Joseph C. Walsh ,  Gang Chen ,  Anjana Sinha ,  Dhanalakshmi Kasi ,  Chul Yu ,  Umesh B. Gangadharmath ,  Wei Zhang ,  Tieming Zhao ,  Vani P. Mocharla

Inventor： Eric Wang ,  Hartmuth C. Kolb ,  Anna Katrin Szardenings ,  Changhui Liu ,  Joseph C. Walsh ,  Gang Chen ,  Anjana Sinha ,  Dhanalakshmi Kasi ,  Chul Yu ,  Umesh B. Gangadharmath ,  Wei Zhang ,  Tieming Zhao ,  Vani P. Mocharla

IPC: C07K5/02 ,  A61K51/04 ,  C07D249/06 ,  C07D249/04 ,  A61K51/08 ,  C07K5/062 ,  C07K5/072 ,  C07D403/12 ,  C07D213/81 ,  C07D213/82 ,  C07D233/78 ,  C07D233/96 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D239/60 ,  C07D251/30 ,  C07D263/34 ,  C07D207/16 ,  C07D277/56 ,  C07D209/48 ,  A61K38/00

CPC classification number: C07K5/0215 ,  A61K38/00 ,  A61K51/0402 ,  A61K51/0453 ,  A61K51/0497 ,  A61K51/088 ,  C07D207/16 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D233/78 ,  C07D233/96 ,  C07D239/60 ,  C07D249/04 ,  C07D249/06 ,  C07D251/30 ,  C07D263/34 ,  C07D277/56 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07K5/06026 ,  C07K5/06113

Abstract: Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

公开(公告)号：US09005577B2

公开(公告)日：2015-04-14

申请号：US12433211

申请日：2009-04-30

Applicant: Hartmuth C. Kolb ,  Joseph C. Walsh ,  Kai Chen ,  Umesh B. Gangadharmath ,  Gang Chen ,  Vani P. Mocharla ,  Dhanalakshmi Kasi ,  Peter J. H. Scott ,  Qianwa Liang

Inventor： Hartmuth C. Kolb ,  Joseph C. Walsh ,  Kai Chen ,  Umesh B. Gangadharmath ,  Gang Chen ,  Vani P. Mocharla ,  Dhanalakshmi Kasi ,  Peter J. H. Scott ,  Qianwa Liang

IPC: A61K51/00 ,  A61M36/14 ,  A61K51/08

CPC classification number: A61K51/088 ,  G01N33/60 ,  G01N2333/96466

Abstract: The present application is directed to radiolabeled imaging agents comprising a radiolabel, and a substrate, pharmaceutical compositions comprising radiolabeled imaging agents, and methods of using the radiolabeled imaging agents. The present application is further directed to methods of preparing the radiolabeled imaging agent. Such imaging agents can used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Abstract translation: 本申请涉及包含放射性标记和底物，包含放射性标记的成像剂的药物组合物的放射性标记的成像剂，以及使用放射性标记的成像剂的方法。 本申请进一步涉及制备放射性标记的成像剂的方法。 这些成像剂可用于成像研究，例如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。

公开(公告)号：US08435454B2

公开(公告)日：2013-05-07

申请号：US12986323

申请日：2011-01-07

Applicant: Arkadij M. Elizarov ,  Carroll Edward Ball ,  Jianzhong Zhang ,  Hartmuth C. Kolb ,  Reza Miraghaie ,  Todd L. Graves ,  Artem Lebedev ,  Keith E. Schleiffer

Inventor： Arkadij M. Elizarov ,  Carroll Edward Ball ,  Jianzhong Zhang ,  Hartmuth C. Kolb ,  Reza Miraghaie ,  Todd L. Graves ,  Artem Lebedev ,  Keith E. Schleiffer

IPC: G21C1/00 ,  B01J19/00

CPC classification number: B01J19/0093 ,  B01J2219/0081 ,  B01J2219/00826 ,  B01J2219/00831 ,  B01J2219/00833 ,  B01J2219/0086 ,  B01J2219/00871 ,  B01J2219/00873 ,  B01J2219/00889 ,  B01J2219/00905 ,  B01J2219/00936

Abstract: Macro- and microfluidic devices and related technologies, and chemical processes using such devices. More specifically, the devices may be used for a fully automated synthesis of radioactive compounds for imaging, such as by positron emission tomography (PET), in an efficient, compact and safe to the operator manner. In particular, embodiments of the present invention relate to an automated, multi-run, microfluidic instrument for the multi-step synthesis of radiopharmaceuticals, such as PET probes, comprising a remote shielded mini-cell containing radiation-handing components.

Abstract translation: 宏观和微流体装置及相关技术以及使用这种装置的化学过程。 更具体地，这些装置可以用于以有效，紧凑和安全的操作者方式全面自动化合成用于成像的放射性化合物，例如通过正电子发射断层摄影（PET）。 特别地，本发明的实施例涉及一种用于多步合成放射性药物的自动化，多运行微流控仪器，例如PET探针，其包括含有辐射递送部件的远程屏蔽微型电池。

公开(公告)号：US20120302755A1

公开(公告)日：2012-11-29

申请号：US13477095

申请日：2012-05-22

Applicant: Anna Katrin Szardenings ,  Hartmuth C. Kolb ,  Joseph C. Walsh ,  Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Changhui Liu ,  Anjana Sinha ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Kai Chen ,  Vani P. Mocharla ,  Peter J.H. Scott

Inventor： Anna Katrin Szardenings ,  Hartmuth C. Kolb ,  Joseph C. Walsh ,  Gang Chen ,  Umesh B. Gangadharmath ,  Dhanalakshmi Kasi ,  Changhui Liu ,  Anjana Sinha ,  Eric Wang ,  Chul Yu ,  Wei Zhang ,  Kai Chen ,  Vani P. Mocharla ,  Peter J.H. Scott

IPC: C07D471/04 ,  C07D471/14

CPC classification number: A61K51/0455 ,  A61K51/0446 ,  C07B59/002 ,  C07D471/04 ,  C07D471/14

Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

Abstract translation: 本文公开了在哺乳动物中诊断阿尔茨海默病或倾向于其的化合物和方法，所述方法包括向哺乳动物施用诊断有效量的放射性标记的化合物，其中所述化合物选自放射性标记的咔唑及其衍生物，以及 三唑衍生物，允许化合物分布到脑组织中并对脑组织进行成像，其中与正常对照水平的结合相比，化合物与脑组织的结合增加表明哺乳动物患有或处于危险中 发展为阿尔茨海默病。

公开(公告)号：US08318132B2

公开(公告)日：2012-11-27

申请号：US12372717

申请日：2009-02-17

Applicant: Hartmuth C. Kolb ,  Joseph C. Walsh ,  Wei Zhang ,  Peter J. H. Scott ,  Kai Chen ,  Vani P. Mocharla ,  Dhanalakshmi Kasi ,  Gang Chen ,  Eric Wang ,  Anjana Sinha

Inventor： Hartmuth C. Kolb ,  Joseph C. Walsh ,  Wei Zhang ,  Peter J. H. Scott ,  Kai Chen ,  Vani P. Mocharla ,  Dhanalakshmi Kasi ,  Gang Chen ,  Eric Wang ,  Anjana Sinha

IPC: A61K51/00 ,  A61M36/14

CPC classification number: C07B59/002

Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

Abstract translation: 本文公开了在哺乳动物中诊断阿尔茨海默病或其倾向的化合物和方法，所述方法包括向哺乳动物施用诊断有效量的放射性标记的化合物，其中所述化合物选自放射性标记的黄酮，香豆素，咔唑 ，喹啉酮，色烯酮，咪唑和三唑衍生物，使化合物分布到脑组织中，并使脑组织成像，其中与正常对照结合水平相比，化合物与脑组织的结合增加指示哺乳动物 患有或有发生阿尔茨海默病的风险。

公开(公告)号：US20120282180A1

公开(公告)日：2012-11-08

申请号：US13155558

申请日：2011-06-08

Applicant: Hartmuth C. Kolb ,  Guenter Haufe ,  Malte Behrends ,  Klaus Kopka ,  Stefan Wagner ,  Verena Hugenberg ,  Hans-Joerg Breyholz ,  Sven Hermann ,  Michael Schaefers

Inventor： Hartmuth C. Kolb ,  Guenter Haufe ,  Malte Behrends ,  Klaus Kopka ,  Stefan Wagner ,  Verena Hugenberg ,  Hans-Joerg Breyholz ,  Sven Hermann ,  Michael Schaefers

IPC: A61K51/04 ,  A61K31/216 ,  C07D213/55 ,  A61K31/44 ,  A61P35/00 ,  A61K31/18 ,  C07D309/10 ,  A61K31/351 ,  A61P9/00 ,  A61P29/00 ,  C07C311/16 ,  A61K31/195

CPC classification number: C07C311/29 ,  C07D213/42 ,  C07D309/12

Abstract: The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.

Abstract translation: 本发明涉及治疗和诊断剂领域，更具体地涉及作为基质金属蛋白酶抑制剂（MMP）的式（I）化合物，可用于治疗与其相关的疾病如心血管疾病，炎性疾病和 恶性疾病。 本发明的一个实施方案是用具有适合于诊断成像的基质金属蛋白酶抑制活性的18-氟原子标记的式（I）化合物。 本发明还公开了一种药物组合物，其包含本发明的基质金属蛋白酶抑制剂（MMPs）或适用于哺乳动物给药形式的本发明诊断显像剂的相应标记化合物。 本发明还公开了合成本发明的基质金属蛋白酶抑制剂（MMPs）和本发明的诊断显像剂以及用于制备本发明的药物组合物的试剂盒的中间体。

公开(公告)号：US08273300B2

公开(公告)日：2012-09-25

申请号：US12803862

申请日：2010-07-08

Applicant: Arkadij M. Elizarov ,  Carroll Edward Ball ,  Jianzhong Zhang ,  Hartmuth C. Kolb ,  Reza Miraghaie ,  Todd Graves ,  Artem Lebedev

Inventor： Arkadij M. Elizarov ,  Carroll Edward Ball ,  Jianzhong Zhang ,  Hartmuth C. Kolb ,  Reza Miraghaie ,  Todd Graves ,  Artem Lebedev

IPC: G21C1/00 ,  B01J19/00 ,  B01J8/00

CPC classification number: B01J19/0093 ,  B01J2219/0081 ,  B01J2219/00826 ,  B01J2219/0086 ,  B01J2219/00871 ,  B01J2219/00936

Abstract: Macro- and microfluidic devices and related technologies, and chemical processes using such devices. More specifically, the devices may be used for a fully automated synthesis of radioactive compounds for imaging, such as by positron emission tomography (PET), in an efficient, compact and safe to the operator manner. In particular, embodiments of the present invention relate to an automated, multi-run, microfluidic instrument for the multi-step synthesis of radiopharmaceuticals, such as PET probes, comprising a remote shielded mini-cell containing radiation-handing components.

Abstract translation: 宏观和微流体装置及相关技术以及使用这种装置的化学过程。 更具体地，这些装置可以用于以有效，紧凑和安全的操作者方式全面自动化合成用于成像的放射性化合物，例如通过正电子发射断层摄影（PET）。 特别地，本发明的实施例涉及一种用于多步合成放射性药物的自动化多运行微流体仪器，例如PET探针，其包括含有辐射递送部件的远程屏蔽微型电池。

公开(公告)号：US08043601B2

公开(公告)日：2011-10-25

申请号：US12180444

申请日：2008-07-25

Applicant: Hartmuth C. Kolb ,  Kai Chen ,  Joseph C. Walsh ,  Dhanalakshmi Kasi ,  Vani P. Mocharla ,  Gang Chen ,  Qianwa Liang ,  Tieming Zhao

Inventor： Hartmuth C. Kolb ,  Kai Chen ,  Joseph C. Walsh ,  Dhanalakshmi Kasi ,  Vani P. Mocharla ,  Gang Chen ,  Qianwa Liang ,  Tieming Zhao

IPC: A61K51/00 ,  A61M36/14

CPC classification number: A61K51/08 ,  A61K38/00 ,  A61K47/60 ,  A61K51/082 ,  C07K5/021 ,  C07K7/54 ,  C07K7/64

Abstract: The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Abstract translation: 本申请涉及放射性标记的环状多氮杂肽，包含放射性标记的环状多氮杂肽的药物组合物，以及使用放射性标记的环状多氮杂肽的方法。 这种多分子肽可用于成像研究，如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。

公开(公告)号：US20110202177A1

公开(公告)日：2011-08-18

申请号：US13027465

申请日：2011-02-15

Applicant: Arkadij M. Elizarov ,  Carroll Edward Ball ,  Ansgar Graw ,  Hartmuth C. Kolb ,  Uttam D. Shah

Inventor： Arkadij M. Elizarov ,  Carroll Edward Ball ,  Ansgar Graw ,  Hartmuth C. Kolb ,  Uttam D. Shah

IPC: G05B21/02

CPC classification number: B01J19/0093 ,  B01J2219/0095 ,  B01J2219/00952 ,  B01J2219/00959 ,  B01J2219/00961 ,  B01J2219/00975 ,  B01J2219/00986 ,  G05B15/02 ,  G16B45/00 ,  G16C20/10 ,  G16C20/80

Abstract: An apparatus and method for chemical synthesis, the method includes accessing a recipe, the recipe including a sequence of one or more processing steps for the chemical synthesis. The processing steps including one or more steps. The recipe is executed by sorting the processing steps and executing the one or more selected steps prior to executing other steps. The chemical synthesis is monitored by providing status data, indicating a status of the execution and enabling input of control data to modify execution based on the status data or user-initiated modification. Information related to the status of the execution is displayed, typically as a graphical representation of a process action.

Abstract translation: 一种用于化学合成的装置和方法，所述方法包括访问配方，所述配方包括用于化学合成的一个或多个处理步骤的序列。 处理步骤包括一个或多个步骤。 通过在执行其他步骤之前排序处理步骤并执行一个或多个所选步骤来执行配方。 通过提供状态数据来指示化学合成，指示执行的状态，并且根据状态数据或用户发起的修改使控制数据的输入能够修改执行。 显示与执行状态相关的信息，通常作为流程操作的图形表示。