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1. 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。

2. 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。

3. 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。

4. 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.

5. 发明授权

US06416733B1 Radiopharmaceuticals for imaging infection and inflammation 失效
标题翻译：用于成像感染和炎症的放射性药物
公开(公告)号：US06416733B1
公开(公告)日：2002-07-09
申请号：US08943659
申请日：1997-10-03
申请人： John A. Barrett , Edward H. Cheesman , Thomas D. Harris , Shuang Liu , Milind Rajopadhye , Michael Sworin
发明人： John A. Barrett , Edward H. Cheesman , Thomas D. Harris , Shuang Liu , Milind Rajopadhye , Michael Sworin
IPC分类号： A61K5100
CPC分类号： 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
摘要： 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.
摘要翻译：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。

6. 发明授权

US06558649B1 Vitronectin receptor antagonist pharmaceuticals 失效
公开(公告)号：US06558649B1
公开(公告)日：2003-05-06
申请号：US09466582
申请日：1999-12-17
申请人： Edward H. Cheesman , Michael Sworin , Milind Rajopadhye
发明人： Edward H. Cheesman , Michael Sworin , Milind Rajopadhye
IPC分类号： A61K5100
CPC分类号： C07K9/003 , A61K49/0002 , A61K51/0497 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0207 , C07K5/0806 , C07K5/0821 , C07K5/1008 , C07K5/1024 , C07K7/02 , C07K7/06 , C07K7/64
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 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.

7. 发明授权

US07090828B2 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US07090828B2
公开(公告)日：2006-08-15
申请号：US10348268
申请日：2003-01-21
申请人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
发明人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
IPC分类号： A61K5/00 , A61M36/14
CPC分类号： A61K49/0002 , A61K51/0497 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0207 , C07K5/0806 , C07K5/0821 , C07K5/1008 , C07K5/1024 , C07K7/02 , C07K7/06 , C07K7/64 , C07K9/003
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 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.
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。

8. 发明授权

US06818201B2 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US06818201B2
公开(公告)日：2004-11-16
申请号：US10306244
申请日：2002-11-26
申请人： Edward H. Cheesman , Michael Sworin , Milind Rajopadhye
发明人： Edward H. Cheesman , Michael Sworin , Milind Rajopadhye
IPC分类号： A61K4900
CPC分类号： C07K9/003 , A61K49/0002 , A61K51/0497 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0207 , C07K5/0806 , C07K5/0821 , C07K5/1008 , C07K5/1024 , C07K7/02 , C07K7/06 , C07K7/64
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 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.
摘要翻译：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。

9. 发明授权

US06569402B1 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US06569402B1
公开(公告)日：2003-05-27
申请号：US09599365
申请日：2000-06-21
申请人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
发明人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
IPC分类号： A61K500
CPC分类号： A61K49/0002 , A61K51/0497 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0207 , C07K5/0806 , C07K5/0821 , C07K5/1008 , C07K5/1024 , C07K7/02 , C07K7/06 , C07K7/64 , C07K9/003
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 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.
摘要翻译：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。

10. 发明授权

US06524554B1 Radiopharmaceuticals for imaging infection and inflammation and for imaging and treatment of cancer 失效
标题翻译：用于成像感染和炎症以及成像和治疗癌症的放射性药物
公开(公告)号：US06524554B1
公开(公告)日：2003-02-25
申请号：US09285280
申请日：1999-04-02
申请人： David Scott Edwards , Milind Rajopadhye
发明人： David Scott Edwards , Milind Rajopadhye
IPC分类号： A61K4904
CPC分类号： C07K7/06 , A61K51/088
摘要： The present invention provides novel radiopharmaceuticals comprising one to three pentapeptides, X1X2X3X4X5, independently attached to a metal chelator or bonding moiety, Ch, to which is attached a Tc-99m, Re-186, or Re-188, optionally further comprising a linking group, Ln, between-the peptides and the chelator or bonding moiety. The pentapeptide sequence binds to the tuftsin receptor and is attached at the N-terminus to Ln or Ch. These radiopharmaceuticals are 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.
摘要翻译：本发明提供了包含一至三个五肽X1X2X3X4X5的新型放射性药物，其独立地连接到金属螯合剂或结合部分Ch上，其连接有Tc-99m，Re-186或Re-188，任选地还包含连接基团，Ln，肽与螯合剂或结合部分之间。五肽序列与簇绒蛋白受体结合，并在N末端连接至Ln或Ch。这些放射性药物可用于感染和炎症的诊断，可用于制备放射性药物的试剂和试剂盒，成像患者感染和/或炎症部位的成像方法，以及诊断与感染或炎症有关的疾病的方法这样的诊断。

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