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公开(公告)号：US08815214B2
公开(公告)日：2014-08-26
申请号：US12355777
申请日：2009-01-17
Applicant: Milind Rajopadhye , Kevin Groves , Dorin V. Preda
Inventor： Milind Rajopadhye , Kevin Groves , Dorin V. Preda
IPC: A61B5/00 , A61B8/00 , A61B10/00 , A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , A61K38/00 , A61K38/04
CPC classification number: A61K49/0032 , A61K47/65 , A61K49/0056 , C07K5/1019 , C07K7/06 , C07K7/64 , C09B23/0008 , C09B23/083 , C09B23/086
Abstract: 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.
Abstract translation: 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。
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2.发明授权Integrin targeting agents and in-vivo and in-vitro imaging methods using the same 有权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
Applicant: Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
Inventor： Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
IPC: A61K49/00
CPC classification number: 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
Abstract: 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.
Abstract translation: 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。
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3.发明申请INTEGRIN TARGETING AGENTS AND IN-VIVO AND IN-VITRO IMAGING METHODS USING THE SAME 有权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
Applicant: Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
Inventor： Milind Rajopadhye , Guojie Ho , Bohumil Bednar , Le T. Duong , Paul J. Coleman
CPC classification number: 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
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20080267883A1
公开(公告)日：2008-10-30
申请号：US12065391
申请日：2006-09-01
Applicant: Milind Rajopadhye , Nara Narayanan , Jeffrey D. Peterson
Inventor： Milind Rajopadhye , Nara Narayanan , Jeffrey D. Peterson
IPC: C07D401/14 , C07D417/14 , A61K49/04 , A61K49/00
CPC classification number: A61K49/0032 , A61K49/0021 , C07D401/06 , C07D401/14 , C07D417/06 , C09B23/0008 , C09B23/083
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US07332149B1
公开(公告)日：2008-02-19
申请号：US09599890
申请日：2000-06-21
Applicant: Milind Rajopadhye , John A. Barrett , Alan P. Carpenter, Jr. , Edward H. Cheesman , Thomas D. Harris
Inventor： Milind Rajopadhye , John A. Barrett , Alan P. Carpenter, Jr. , Edward H. Cheesman , Thomas D. Harris
IPC: A61K51/00 , A61K51/04 , A61K51/06 , A61M36/00 , A61P35/00 , C07D231/54 , C07D259/00 , C07D403/14 , 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.
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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Patent Agency Ranking
公开(公告)号：US20050047999A1
公开(公告)日：2005-03-03
申请号：US10645272
申请日：2003-08-21
Applicant: Alan Carpenter , Milind Rajopadhye
Inventor： Alan Carpenter , Milind Rajopadhye
IPC: A61K38/00 , A61K47/48 , A61K49/00 , A61K49/04 , A61K49/08 , A61K51/00 , A61K51/04 , C07F5/00 , C07F9/6527 , C07K5/06 , C07K5/065
CPC classification number: A61K49/00 , A61K38/00 , A61K49/0002 , A61K49/085 , A61K49/10 , A61K49/223 , A61K51/0497 , C07F9/6527 , C07K5/06026 , C07K5/06078 , C07K5/06191
Abstract: Thus the present invention describes diagnostic agents comprising a diagnostic metal and a compound, wherein the compound comprises: 1-10 targeting moieties;a chelator; and 0-1 linking groups between the targeting moiety and chelator;wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to the diagnostic metal. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in diagnosis of diseases associated with MMPs.
Abstract translation: 因此，本发明描述了包含诊断金属和化合物的诊断剂，其中所述化合物包含：1-10个靶向部分;螯合剂; 和靶向部分和螯合剂之间的0-1个连接基团;其中靶向部分是基质金属蛋白酶抑制剂; 并且其中螯合剂能够与诊断金属共轭。 本发明还提供本发明化合物，试剂盒及其在诊断与MMP相关的疾病中的用途的新组合物。
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公开(公告)号：US06800273B2
公开(公告)日：2004-10-05
申请号：US10342081
申请日：2003-01-14
Applicant: Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
Inventor： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
IPC: A61K5100
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：可用于癌症的诊断和治疗，对患者肿瘤成像的方法，以及治疗患者癌症的方法。 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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公开(公告)号：US06794518B1
公开(公告)日：2004-09-21
申请号：US09466588
申请日：1999-12-17
Applicant: Milind Rajopadhye , Thomas D. Harris , Edward H. Cheesman
Inventor： Milind Rajopadhye , Thomas D. Harris , Edward H. Cheesman
IPC: C07D23154
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.
Abstract translation: 本发明描述了新的下式化合物：可用于癌症的诊断和治疗，对患者肿瘤成像的方法，以及治疗患者癌症的方法。 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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公开(公告)号：US06537520B1
公开(公告)日：2003-03-25
申请号：US09599295
申请日：2000-06-21
Applicant: Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
Inventor： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
IPC: A61K5100
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：可用于癌症的诊断和治疗，对患者肿瘤成像的方法，以及治疗患者癌症的方法。 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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公开(公告)号：US06322770B1
公开(公告)日：2001-11-27
申请号：US09281207
申请日：1999-03-30
Applicant: Milind Rajopadhye , Thomas David Harris
Inventor： Milind Rajopadhye , Thomas David Harris
IPC: A61K5100
CPC classification number: A61K49/0002 , A61K49/227 , A61K51/082 , A61K51/088 , C07D401/12 , C07D401/14
Abstract: 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.
Abstract translation: 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。
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