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1. 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。

2. 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.

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

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。

5. 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。

6. 发明授权

US06524553B2 Quinolone vitronectin receptor antagonist pharmaceuticals 有权
标题翻译：喹诺酮玻连蛋白受体拮抗剂药物
公开(公告)号：US06524553B2
公开(公告)日：2003-02-25
申请号：US09281209
申请日：1999-03-30
申请人： Thomas David Harris
发明人： Thomas David Harris
IPC分类号： A61B5055
CPC分类号： C07K5/06191 , A61K49/0002 , A61K49/04 , A61K49/085 , A61K49/10 , A61K49/223 , A61K51/0455 , A61K51/0459 , A61K51/0497 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07K5/0205 , C07K5/0207 , C07K5/0215 , C07K5/06139 , 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 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。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。

7. 发明授权

US5688485A Radiolabelled complexes of ester-substituted diaminethiols 失效
标题翻译：酯取代的二氨基硫醇的放射性标记复合物
公开(公告)号：US5688485A
公开(公告)日：1997-11-18
申请号：US999705
申请日：1992-12-31
申请人： Thomas David Harris
发明人： Thomas David Harris
IPC分类号： A61K51/04 , C07C323/58 , C07F13/00 , C07C321/00
CPC分类号： C07F13/005 , A61K51/0478 , C07C323/58
摘要： This invention relates to compounds and methods for use in determining renal function by means of scintigraphic urography. More specifically, this invention relates to radionuclide complexes of ester-substituted diaminethiols, radiopharmaceutical compositions comprising said complexes, kits for the preparation of said compositions, and a method of using said compositions for examining renal function. Compounds of this invention have the formula: ##STR1## wherein the various groups are as defined herein.
摘要翻译：本发明涉及通过闪烁照相术确定肾功能的化合物和方法。更具体地，本发明涉及酯取代的二氨基硫醇的放射性核素配合物，包含所述复合物的放射性药物组合物，用于制备所述组合物的试剂盒，以及使用所述组合物检查肾功能的方法。本发明的化合物具有下列通式：本文所述。

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