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公开(公告)号：US06511648B2
公开(公告)日：2003-01-28
申请号：US09465300
申请日：1999-12-17
Applicant: Thomas D. Harris , Milind Rajopadhye
Inventor： Thomas D. Harris , Milind Rajopadhye
IPC: A61K5100
CPC classification number: C07D401/14 , A61K49/0002 , A61K49/04 , A61K49/085 , A61K49/10 , A61K49/223 , A61K51/0497 , C07D401/12
Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
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公开(公告)号：US20120328514A1
公开(公告)日：2012-12-27
申请号：US13382689
申请日：2010-07-08
Applicant: Richard R. Cesati , Thomas D. Harris , Simon P. Robinson , Richard J. Looby , Edward H. Cheesman , Padmaja Yalamanchili , David S. Casebier
Inventor： Richard R. Cesati , Thomas D. Harris , Simon P. Robinson , Richard J. Looby , Edward H. Cheesman , Padmaja Yalamanchili , David S. Casebier
IPC: A61K49/00 , A61K51/04 , C07D209/20 , C07D213/56 , C07C229/36 , C07D257/02
CPC classification number: A61K51/0497 , A61K49/085 , A61K49/10 , A61K51/0406 , C07C259/06 , C07C271/22 , C07D257/02
Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.
Abstract translation: 本公开涉及化合物，诊断剂和相关方法。 在某些情况下，提供了治疗患者的方法。 更具体地，本公开提供了用于检测和/或成像和/或监测富含弹性蛋白的组织的化合物，诊断剂和试剂盒。 此外，本公开提供了检测和/或成像和/或监测冠状动脉斑块，颈动脉斑块，髂骨/股骨斑块，主动脉斑块，肾动脉斑块，任何动脉血管的斑块，动脉瘤，血管炎，其他疾病的存在的方法 的动脉壁，和/或韧带，子宫，肺或皮肤的损伤或结构变化，如总血管壁面积，内腔大小和外动脉周长的变化所示。
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公开(公告)号：US20100221182A1
公开(公告)日：2010-09-02
申请号：US12448575
申请日：2007-12-21
Applicant: Ajay Purohit , Thomas D, Harris , Heike S. Radeke , Simon P. Robinson , Ming Yu , David S. Casebier , Michael T. Azure
Inventor： Ajay Purohit , Thomas D, Harris , Heike S. Radeke , Simon P. Robinson , Ming Yu , David S. Casebier , Michael T. Azure
IPC: A61K51/04 , C07D233/88 , C07C279/08 , C07C215/30 , C07D295/14
CPC classification number: A61K51/04 , A61K51/0453 , A61K51/0459 , C07B59/001 , C07B2200/05 , C07C215/60 , C07C217/70 , C07C279/06 , C07C279/08
Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
Abstract translation: 公开了用于心脏神经支配成像的核医学应用（PET成像）中用作成像剂的新型化合物。 这些基于PET的放射性示踪剂可能表现出增加的稳定性，减少NE释放（从而减少副作用），改进的定量数据，和/或对先前的放射性示踪剂对VMAT的高亲和力。 还提供了使用化合物成像心脏神经支配的方法。 在某些情况下，化合物通过在各种位置上衍生化某些化合物而形成：芳基，烷基，酮基，苄基，β-烷基醚，γ-丙基烷基醚和β-丙基烷基醚。 或者或另外，将甲基a加入到胺中，和/或儿茶酚官能团被消除或掩蔽，作为使这些化合物更稳定的方式。
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14.发明申请Preparation of Paramagnetic Nanoparticles Conjugated to Leukotriene B4 (LTB4) Receptor Antagonists, and Their Use as MRI Contrast Agents for the Detection of Infection and Inflammation 审中-公开与白三烯B4（LTB4）受体拮抗剂共轭的顺磁性纳米颗粒的制备及其作为检测感染和炎症的MRI对比剂公开(公告)号：US20080213181A1
公开(公告)日：2008-09-04
申请号：US11959569
申请日：2007-12-19
Applicant: Thomas D. Harris
Inventor： Thomas D. Harris
IPC: A61K49/00 , C07D401/06
CPC classification number: A61K49/1839 , A61K49/085 , A61K49/10 , A61K49/1806 , A61K49/186 , A61K49/1869 , B82Y5/00
Abstract: Nanoparticle-based compositions and emulsions that are specifically targeted to leukotriene B4 (LTB4) receptors, and employing LTB4 receptor antagonist targeting agents, are set forth. In addition, there is provided the use of non-antibody based compositions for such targeting. The compositions of the invention are useful as imaging agents in diagnostic and therapeutic applications.
Abstract translation: 阐述了特异性靶向白细胞三烯B4（LTB4）受体的纳米颗粒组合物和乳剂，并采用LTB4受体拮抗剂靶向剂。 此外，提供了用于这种靶向的基于非抗体的组合物的用途。 本发明的组合物可用作诊断和治疗应用中的成像剂。
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公开(公告)号：US07018611B2
公开(公告)日：2006-03-28
申请号：US10281015
申请日：2002-10-26
Applicant: Thomas D. Harris , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye
Inventor： Thomas D. Harris , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye
CPC classification number: A61K49/0002 , A61K49/04 , A61K49/085 , A61K49/10 , A61K49/223 , A61K51/0455 , A61K51/0459 , A61K51/0497 , C07D401/12 , C07D401/14
Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
Abstract translation: 本发明描述了新的下式化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？>（Q） 对于癌症的诊断和治疗有用的<？in-line-formula description =“在线公式”end =“tail”？>，肿瘤成像方法 患者，以及在患者中治疗癌症的方法。 本发明还提供了可用于监测治疗性血管生成治疗和破坏新的血管生成脉管系统的新型化合物。 本发明还提供可用于成像动脉粥样硬化，再狭窄，心脏缺血和心肌再灌注损伤的新型化合物。 本发明还提供了可用于治疗类风湿性关节炎的新化合物。 药物由与血管发生期间上调的受体结合的靶向部分，任选的连接基团和治疗有效的放射性同位素或诊断上有效的可成像部分组成。 可成像部分是伽马射线或正电子发射放射性同位素，磁共振成像造影剂，X射线造影剂或超声造影剂。
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Patent Agency Ranking
公开(公告)号：US06416733B1
公开(公告)日：2002-07-09
申请号：US08943659
申请日：1997-10-03
Applicant: John A. Barrett , Edward H. Cheesman , Thomas D. Harris , Shuang Liu , Milind Rajopadhye , Michael Sworin
Inventor： John A. Barrett , Edward H. Cheesman , Thomas D. Harris , Shuang Liu , Milind Rajopadhye , Michael Sworin
IPC: A61K5100
CPC classification number: A61K51/0497 , A61K51/0455 , A61K51/0478 , C07C59/90 , C07D213/64 , C07D213/71 , C07D213/77 , C07D213/82 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07F13/005
Abstract: The present invention provides novel radiopharmaceuticals useful for the diagnosis of infection and inflammation, reagents and kits useful for preparing the radiopharmaceuticals, methods of imaging sites of infection and/or inflammation in a patient, and methods of diagnosing diseases associated with infection or inflammation in patients in need of such diagnosis. The radiopharmaceuticals bind in vivo to the leukotriene B4 (LTB4) receptor on the surface of leukocytes which accumulate at the site of infection and inflammation. The reagents provided by this invention are also useful for the treatment of diseases associated with infection and inflammation.
Abstract translation: 本发明提供了可用于诊断感染和炎症的新型放射性药物，可用于制备放射性药物的试剂和试剂盒，成像患者感染和/或炎症部位成像方法以及诊断患者感染或炎症相关疾病的方法 需要这样的诊断。 放射性药物在体内结合白细胞表面的白细胞三烯B4（LTB4）受体，其在感染和炎症部位积聚。 本发明提供的试剂也可用于治疗与感染和炎症相关的疾病。
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17.发明授权
公开(公告)号：US5397902A
公开(公告)日：1995-03-14
申请号：US167685
申请日：1993-12-15
Applicant: James F. Castner , Bobby E. Corry , Thomas D. Harris , Richard J. Looby
Inventor： James F. Castner , Bobby E. Corry , Thomas D. Harris , Richard J. Looby
CPC classification number: G21F5/015
Abstract: Apparatus and method for producing a radiopharmaceutical formulation utilize a radiation-shielding container for receiving a vial having the non-radioactive components necessary to form a radiopharmaceutical formulation therein. A mixture of such non-radioactive components and a radioactive liquid added thereto is both heated and cooled using a thermoelectric element. The container comprises a hollow outer shielding member formed from a radiation shielding material and a vial holder formed from a highly heat conductive material received therewithin. The vial holder includes a skirt portion that defines a socket. The socket is sized to receive in an intimate heat transmissive relationship a mounting projection that is itself connected in thermally conductive contact with the thermoelectric element. Using the thermoelectric heating and cooling element, heat is both applied to and removed from the radioactive liquid and the non-radioactive components within the vial while the vial is held within the vial holder within the radiation shielding container, thereby to produce a radiopharmaceutical formulation within the vial.
Abstract translation: 用于制备放射性药物制剂的装置和方法利用辐射屏蔽容器来接收具有在其中形成放射性药物制剂所必需的非放射性成分的小瓶。 使用热电元件将这种非放射性组分和加入其中的放射性液体的混合物加热和冷却。 容器包括由辐射屏蔽材料形成的中空外屏蔽构件和由其中容纳的高导热材料形成的小瓶支架。 瓶保持器包括限定插座的裙部。 插座的尺寸被设计成以紧密的热传导关系接收安装突起，该安装突起本身与热电元件的导热接触连接。 使用热电加热和冷却元件，当将小瓶保持在辐射屏蔽容器内的小瓶保持器内时，热量被施加到放射性液体和小瓶内的非放射性组分中并从其中移除，由此产生放射性药物制剂 小瓶。
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公开(公告)号：US08361438B2
公开(公告)日：2013-01-29
申请号：US12350628
申请日：2009-01-08
Applicant: Richard R. Cesati , Thomas D. Harris , Simon P. Robinson , Richard J. Looby , Edward H. Cheesman , Padmaja Yalamanchili , David S. Casebier
Inventor： Richard R. Cesati , Thomas D. Harris , Simon P. Robinson , Richard J. Looby , Edward H. Cheesman , Padmaja Yalamanchili , David S. Casebier
CPC classification number: C07D257/02 , A61K49/103 , A61K49/106 , A61K51/04 , C07C53/18 , C07C259/06 , C07C259/14 , C07C271/22 , C07C2601/14 , C07D209/20 , C07D213/56 , C07D403/12
Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.
Abstract translation: 本公开涉及化合物，诊断剂和相关方法。 在某些情况下，提供了治疗患者的方法。 更具体地，本公开提供了用于检测和/或成像和/或监测富含弹性蛋白的组织的化合物，诊断剂和试剂盒。 此外，本公开提供了检测和/或成像和/或监测冠状动脉斑块，颈动脉斑块，髂骨/股骨斑块，主动脉斑块，肾动脉斑块，任何动脉血管的斑块，动脉瘤，血管炎，其他疾病的存在的方法 的动脉壁，和/或韧带，子宫，肺或皮肤的损伤或结构变化，如总血管壁面积，内腔大小和外动脉周长的变化所示。
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公开(公告)号：US07321045B2
公开(公告)日：2008-01-22
申请号：US10770380
申请日：2004-02-02
Applicant: Milind Rajopadhye , Thomas D. Harris , Edward H. Cheesman
Inventor： Milind Rajopadhye , Thomas D. Harris , Edward H. Cheesman
IPC: C07D231/54 , C07D259/00 , A61K51/00 , A61K31/416 , A61K31/33
CPC classification number: C07D401/14 , A61K49/0002 , C07D401/12 , C07K5/0205 , C07K5/0215 , C07K5/06139 , C07K5/06191
Abstract: The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
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公开(公告)号：US07052673B2
公开(公告)日：2006-05-30
申请号：US10622246
申请日：2003-07-18
Applicant: Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D Harris , Stuart D Heminway , Shuang Liu , Singh R Prahlad
Inventor： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D Harris , Stuart D Heminway , Shuang Liu , Singh R Prahlad
CPC classification number: C07D401/14 , A61K38/00 , A61K45/06 , A61K49/0002 , A61K49/227 , A61K51/082 , A61K51/088 , C07D401/12 , C07K7/06 , C07K7/08 , C07K7/64
Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
Abstract translation: 本发明描述了新的下式化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？>（Q） 对于癌症的诊断和治疗有用的<？in-line-formula description =“在线公式”end =“tail”？>，肿瘤成像方法 患者，以及在患者中治疗癌症的方法。 本发明还提供了可用于监测治疗性血管生成治疗和破坏新的血管生成脉管系统的新型化合物。 药物由与血管发生期间上调的受体结合的靶向部分，任选的连接基团和治疗有效的放射性同位素或诊断上有效的可成像部分组成。 可成像部分是伽马射线或正电子发射放射性同位素，磁共振成像造影剂，X射线造影剂或超声造影剂。
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