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公开(公告)号：US06511649B1
公开(公告)日：2003-01-28
申请号：US09599364
申请日：2000-06-21
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
IPC: A61K5100
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：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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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：US09913917B2
公开(公告)日：2018-03-13
申请号：US11645111
申请日：2006-12-22
Applicant: Kevin Groves , Milind Rajopadhye
Inventor： Kevin Groves , Milind Rajopadhye
CPC classification number: A61K49/1866 , A61K49/0002 , A61K49/0032 , A61K49/0056 , A61K49/0093 , A61K49/1833 , A61K49/186 , B82Y5/00
Abstract: The invention relates to highly fluorescent metal oxide nanoparticles to which biomolecules and other compounds can be chemically linked to form biocompatible, stable optical imaging agents for in vitro and in vivo applications. The fluorescent metal oxide nanoparticles may also be used for magnetic resonance imaging (MRI), thus providing a multi modality imaging agent.
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公开(公告)号：US20090220430A1
公开(公告)日：2009-09-03
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
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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公开(公告)号：US20080317676A1
公开(公告)日：2008-12-25
申请号：US12065385
申请日：2006-09-01
Applicant: Milind Rajopadhye , Kevin Groves
Inventor： Milind Rajopadhye , Kevin Groves
IPC: C07D401/14 , C07D401/02 , C07D413/14 , A61K49/00 , A61K49/04
CPC classification number: G01N33/582 , A61K49/0032 , A61K49/0052 , C09B23/0008 , C09B23/0066 , C09B23/083 , C09B23/086 , G01N33/533
Abstract: This invention relates to new fluorescent chemical entities that are designed to attach to biocompatible molecules to form in vivo optical imaging agents.
Abstract translation: 本发明涉及被设计成附着于生物相容性分子以形成体内光学成像剂的新荧光化学实体。
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Patent Agency Ranking
公开(公告)号：US20080226562A1
公开(公告)日：2008-09-18
申请号：US11645111
申请日：2006-12-22
Applicant: Kevin Groves , Milind Rajopadhye
Inventor： Kevin Groves , Milind Rajopadhye
CPC classification number: A61K49/1866 , A61K49/0002 , A61K49/0032 , A61K49/0056 , A61K49/0093 , A61K49/1833 , A61K49/186 , B82Y5/00
Abstract: The invention relates to highly fluorescent metal oxide nanoparticles to which biomolecules and other compounds can be chemically linked to form biocompatible, stable optical imaging agents for in vitro and in vivo applications. The fluorescent metal oxide nanoparticles may also be used for magnetic resonance imaging (MRI), thus providing a multi modality imaging agent.
Abstract translation: 本发明涉及高度荧光的金属氧化物纳米颗粒，生物分子和其它化合物可以化学连接以形成用于体外和体内应用的生物相容性，稳定的光学成像剂。 荧光金属氧化物纳米颗粒也可用于磁共振成像（MRI），从而提供多模态成像剂。
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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：US07060248B2
公开(公告)日：2006-06-13
申请号：US10645272
申请日：2003-08-21
Applicant: Alan P. Carpenter, Jr. , Milind Rajopadhye
Inventor： Alan P. Carpenter, Jr. , Milind Rajopadhye
IPC: A61K49/00
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：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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公开(公告)号：US06743412B2
公开(公告)日：2004-06-01
申请号：US09947783
申请日：2001-09-07
Applicant: Thomas D. Harris , Milind Rajopadhye
Inventor： Thomas D. Harris , Milind Rajopadhye
IPC: A61K4900
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.
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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