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1. 发明授权

US06322770B1 Indazole vitronectin receptor antagonist pharmaceuticals 失效
标题翻译：吲唑玻连蛋白受体拮抗剂药物
公开(公告)号：US06322770B1
公开(公告)日：2001-11-27
申请号：US09281207
申请日：1999-03-30
申请人： Milind Rajopadhye , Thomas David Harris
发明人： Milind Rajopadhye , Thomas David Harris
IPC分类号： A61K5100
CPC分类号： A61K49/0002 , A61K49/227 , A61K51/082 , A61K51/088 , C07D401/12 , C07D401/14
摘要： The present invention d ribs 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.
摘要翻译：本发明d排除下式的新型化合物：可用于癌症的诊断和治疗，对患者的肿瘤成像的方法，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。

2. 发明授权

US5750088A Stable hydrazones linked to a peptide moiety as reagents for the preparation of radiopharmaceuticals 失效
标题翻译：连接到肽部分的稳定腙作为制备放射性药物的试剂
公开(公告)号：US5750088A
公开(公告)日：1998-05-12
申请号：US476296
申请日：1995-06-07
申请人： Michael Sworin , Milind Rajopadhye , Thomas David Harris , David Scott Edwards , Edward Hollister Cheesman , Shuang Liu
发明人： Michael Sworin , Milind Rajopadhye , Thomas David Harris , David Scott Edwards , Edward Hollister Cheesman , Shuang Liu
IPC分类号： A61K31/00 , A61K38/12 , A61K49/04 , A61K51/00 , A61K51/04 , A61K51/08 , C07B59/00 , C07D213/82 , C07D257/00 , C07D259/00 , C07D277/60 , C07D401/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07K5/10 , C07K5/103 , C07K7/64 , C07K14/75 , C07K17/02 , A61K38/00
CPC分类号： C07D213/82 , A61K51/04 , A61K51/082 , A61K51/088 , C07B59/008 , C07D401/12 , C07D401/14 , C07K14/75 , A61K2123/00
摘要： This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.
摘要翻译：本发明提供用于制备用作诊断心血管疾病，感染，炎症和癌症的成像剂的放射性药物的新型试剂，包含所述试剂的诊断试剂和可用于制备所述试剂的中间体化合物。试剂由稳定的腙修饰的生物活性分子组成，其与γ发射放射性同位素反应形成放射性药物，其选择性地定位在疾病部位，从而允许使用γ闪烁扫描获得基因座的图像。

3. 发明授权

US6015904A Stable reagents for the preparation of radio pharmaceuticals 失效
标题翻译：用于制备放射性药物的稳定试剂
公开(公告)号：US6015904A
公开(公告)日：2000-01-18
申请号：US956313
申请日：1997-10-23
申请人： Michael Sworin , Milind Rajopadhye , Thomas David Harris , David Scott Edwards , Edward Hollister Cheesman , Shuang Liu
发明人： Michael Sworin , Milind Rajopadhye , Thomas David Harris , David Scott Edwards , Edward Hollister Cheesman , Shuang Liu
IPC分类号： A61K31/00 , A61K38/12 , A61K49/04 , A61K51/00 , A61K51/04 , A61K51/08 , C07B59/00 , C07D213/82 , C07D257/00 , C07D259/00 , C07D277/60 , C07D401/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07K5/10 , C07K5/103 , C07K7/64 , C07K14/75 , C07K17/02
CPC分类号： C07D213/82 , A61K51/04 , A61K51/082 , A61K51/088 , C07B59/008 , C07D401/12 , C07D401/14 , C07K14/75 , A61K2123/00
摘要： This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.
摘要翻译：本发明提供用于制备用作诊断心血管疾病，感染，炎症和癌症的成像剂的放射性药物的新型试剂，包含所述试剂的诊断试剂和可用于制备所述试剂的中间体化合物。试剂由稳定的腙修饰的生物活性分子组成，其与γ发射放射性同位素反应形成放射性药物，其选择性地定位在疾病部位，从而允许使用γ闪烁扫描获得基因座的图像。

4. 发明授权

US6022523A Radiolabeled platelet GPIIb/IIIa receptor antagonists as imaging agents for the diagnosis of thromboembolic disorders 失效
标题翻译：放射性标记的血小板GPIIb / IIIa受体拮抗剂作为诊断血栓栓塞障碍的显像剂
公开(公告)号：US6022523A
公开(公告)日：2000-02-08
申请号：US999400
申请日：1997-12-29
申请人： William Frank DeGrado , Shaker Ahmed Mousa , Michael Sworin , John Andrew Barrett , Scott David Edwards , Thomas David Harris , Milind Rajopadhye , Shuang Liu
发明人： William Frank DeGrado , Shaker Ahmed Mousa , Michael Sworin , John Andrew Barrett , Scott David Edwards , Thomas David Harris , Milind Rajopadhye , Shuang Liu
IPC分类号： A61K38/12 , A61K49/04 , A61K51/00 , A61K51/04 , A61K51/08 , C07B59/00 , C07D213/82 , C07D257/00 , C07D259/00 , C07D277/60 , C07D401/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07K5/10 , C07K5/103 , C07K7/64 , C07K14/75 , C07K17/02
CPC分类号： C07K14/75 , A61K51/04 , A61K51/0482 , A61K51/082 , A61K51/088 , C07B59/008 , C07D213/82 , C07D401/12 , C07D401/14 , A61K2123/00
摘要： This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.
摘要翻译：本发明提供新的放射性药物，其是放射性标记的环状化合物，其含有作为血小板糖蛋白IIb / IIIa复合物拮抗剂的碳环或杂环系统; 使用所述放射性药物作为诊断动脉和静脉血栓的显像剂的方法; 用于制备所述放射性药物的新型试剂; 以及包含所述试剂的试剂盒。

5. 发明授权

US5879657A Radiolabeled platelet GPIIb/IIIa receptor antagonists as imaging agents for the diagnosis of thromboembolic disorders 失效
公开(公告)号：US5879657A
公开(公告)日：1999-03-09
申请号：US218861
申请日：1994-03-28
申请人： William Frank DeGrado , Shaker Ahmed Mousa , Michael Sworin , John Andrew Barrett , Scott David Edwards , Thomas David Harris , Milind Rajopadhye , Shuang Liu
发明人： William Frank DeGrado , Shaker Ahmed Mousa , Michael Sworin , John Andrew Barrett , Scott David Edwards , Thomas David Harris , Milind Rajopadhye , Shuang Liu
IPC分类号： A61K38/12 , A61K49/04 , A61K51/00 , A61K51/04 , A61K51/08 , C07B59/00 , C07D213/82 , C07D257/00 , C07D259/00 , C07D277/60 , C07D401/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07K5/10 , C07K5/103 , C07K7/64 , C07K14/75 , C07K17/02 , A61M36/14
CPC分类号： C07K14/75 , A61K51/04 , A61K51/0482 , A61K51/082 , A61K51/088 , C07B59/008 , C07D213/82 , C07D401/12 , C07D401/14 , A61K2123/00
摘要： This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.

6. 发明授权

US08815214B2 Fluorescent imaging agents 有权
标题翻译：荧光成像剂
公开(公告)号：US08815214B2
公开(公告)日：2014-08-26
申请号：US12355777
申请日：2009-01-17
申请人： Milind Rajopadhye , Kevin Groves , Dorin V. Preda
发明人： Milind Rajopadhye , Kevin Groves , Dorin V. Preda
IPC分类号： A61B5/00 , A61B8/00 , A61B10/00 , A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , A61K38/00 , A61K38/04
CPC分类号： A61K49/0032 , A61K47/65 , A61K49/0056 , C07K5/1019 , C07K7/06 , C07K7/64 , C09B23/0008 , C09B23/083 , C09B23/086
摘要： Provided is a family of intramolecularly quenched imaging agents for use in both in vivo and in vitro imaging that contain at least one enzymatically cleavable oligopeptide and two fluorophores or a fluorophore and a quencher. When subjected to proteolytic cleavage, at least one fluorophore is unquenched and becomes capable of producing a fluorescent signal upon excitation with light of an appropriate wavelength. Also provided are in vivo and in vitro imaging methods using such imaging agents.
摘要翻译：提供了用于体内和体外成像的分子内骤冷成像剂家族，其包含至少一种可酶促切割的寡肽和两个荧光团或荧光团和猝灭剂。当进行蛋白水解切割时，至少一个荧光团是不淬灭的，并且在用适当波长的光激发时变得能够产生荧光信号。还提供了使用这种成像剂的体内和体外成像方法。

7. 发明授权

US08685370B2 Integrin targeting agents and in-vivo and in-vitro imaging methods using the same 有权
标题翻译：整合素靶向剂和使用其的体内和体外成像方法
公开(公告)号：US08685370B2
公开(公告)日：2014-04-01
申请号：US12922594
申请日：2009-03-13
申请人： Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
发明人： Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
IPC分类号： A61K49/00
CPC分类号： A61K49/04 , A61K47/65 , A61K49/0002 , A61K49/0032 , A61K49/0052 , A61K49/0056 , A61K49/0065 , A61K49/085 , A61K49/10 , A61K49/1839 , A61K51/0455 , A61K51/0459 , A61K51/0497 , B82Y5/00 , C09B23/0008 , C09B23/083 , C09B23/086 , G01N33/574
摘要： The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.
摘要翻译：本发明提供靶向整联蛋白的药物家族，其可以用作成像剂和/或治疗剂。这些药剂可用于影像受试者的血管生成，炎症或其他生理过程。

8. 发明申请

US20110165075A1 INTEGRIN TARGETING AGENTS AND IN-VIVO AND IN-VITRO IMAGING METHODS USING THE SAME 有权
标题翻译： INTEGRIN定位试剂和使用该方法的体内和体外成像方法
公开(公告)号：US20110165075A1
公开(公告)日：2011-07-07
申请号：US12922594
申请日：2009-03-13
申请人： Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
发明人： Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
IPC分类号： A61K51/00 , C07D471/04 , C07F15/02 , C07F5/00 , C07K7/06 , A61K49/00 , A61K49/04 , G01N33/53
CPC分类号： A61K49/04 , A61K47/65 , A61K49/0002 , A61K49/0032 , A61K49/0052 , A61K49/0056 , A61K49/0065 , A61K49/085 , A61K49/10 , A61K49/1839 , A61K51/0455 , A61K51/0459 , A61K51/0497 , B82Y5/00 , C09B23/0008 , C09B23/083 , C09B23/086 , G01N33/574
摘要： The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.
摘要翻译：本发明提供靶向整联蛋白的药物家族，其可以用作成像剂和/或治疗剂。这些药剂可用于影像受试者的血管生成，炎症或其他生理过程。

9. 发明申请

US20080267883A1 Nicotinic and Picolinic Acid Derived Near-Infrared Fluorophores 有权
标题翻译：烟碱衍生物近红外荧光团
公开(公告)号：US20080267883A1
公开(公告)日：2008-10-30
申请号：US12065391
申请日：2006-09-01
申请人： Milind Rajopadhye , Nara Narayanan , Jeffrey D. Peterson
发明人： Milind Rajopadhye , Nara Narayanan , Jeffrey D. Peterson
IPC分类号： C07D401/14 , C07D417/14 , A61K49/04 , A61K49/00
CPC分类号： A61K49/0032 , A61K49/0021 , C07D401/06 , C07D401/14 , C07D417/06 , C09B23/0008 , C09B23/083
摘要： This invention relates to new fluorescent chemical entities, including fluorescent molecules that comprise a carboxyl or carbonyl functionalized pyridine moiety. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.
摘要翻译：本发明涉及新的荧光化学实体，包括含有羧基或羰基官能化的吡啶部分的荧光分子。本发明还涉及这种分子的相应的反应性形式。本发明还涉及与诸如肽，蛋白质，各种生物分子，碳环和杂环化合物，糖等部分的相应缀合物及其用途。

10. 发明授权

US07332149B1 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US07332149B1
公开(公告)日：2008-02-19
申请号：US09599890
申请日：2000-06-21
申请人： Milind Rajopadhye , John A. Barrett , Alan P. Carpenter, Jr. , Edward H. Cheesman , Thomas D. Harris
发明人： Milind Rajopadhye , John A. Barrett , Alan P. Carpenter, Jr. , Edward H. Cheesman , Thomas D. Harris
IPC分类号： A61K51/00 , A61K51/04 , A61K51/06 , A61M36/00 , A61P35/00 , C07D231/54 , C07D259/00 , C07D403/14 , A61K31/416 , A61K31/33
CPC分类号： C07D401/14 , A61K49/0002 , C07D401/12 , C07K5/0205 , C07K5/0215 , C07K5/06139 , C07K5/06191
摘要： 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.
摘要翻译：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。本发明还提供了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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