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1. 发明授权

US06479032B1 Calcitonin receptor binding reagents 失效
标题翻译：降钙素受体结合试剂
公开(公告)号：US06479032B1
公开(公告)日：2002-11-12
申请号：US09553493
申请日：2000-04-20
申请人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
发明人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
IPC分类号： A61K5100
CPC分类号： C07K14/585 , A61K38/00
摘要： This invention relates to calcitonin receptor binding reagents comprising compounds which are covalently linked to a radiometal chelator. The invention is embodied as calcitonin receptor binding peptide derivatives and analogues of calcitonin which may be radiolabeled with a suitable isotope and used as radiodiagnostic or radiotherapeutic agents. Methods and kits for making, radiolabeling and using such reagents diagnostically and therapeutically in a mammalian body are also provided.
摘要翻译：本发明涉及包含与放射性金属螯合剂共价连接的化合物的降钙素受体结合试剂。本发明体现为降钙素受体结合肽衍生物和降钙素类似物，其可以用合适的同位素放射标记并用作放射诊断或放射治疗剂。还提供了用于在哺乳动物身体中诊断和治疗地制备，放射性标记和使用这些试剂的方法和试剂盒。

2. 发明授权

US6086850A Calcitonin receptor binding reagents 失效
公开(公告)号：US6086850A
公开(公告)日：2000-07-11
申请号：US71090
申请日：1998-05-01
申请人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
发明人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
IPC分类号： A61K51/00 , A61K38/00 , A61K38/23 , A61K49/00 , A61K51/08 , A61P35/00 , C07B59/00 , C07K14/585 , A61M36/14
CPC分类号： C07K14/585 , A61K38/00
摘要： This invention relates to calcitonin receptor binding reagents comprising compounds which are covalently linked to a radiometal chelator. The invention is embodied as calcitonin receptor binding peptide derivatives and analogues of calcitonin which may be radiolabeled with a suitable isotope and used as radiodiagnostic or radiotherapeutic agents. Methods and kits for making, radiolabeling and using such reagents diagnostically and therapeutically in a mammalian body are also provided.

3. 发明授权

US06509001B1 Calcitonin receptor binding reagents 失效
标题翻译：降钙素受体结合试剂
公开(公告)号：US06509001B1
公开(公告)日：2003-01-21
申请号：US09553494
申请日：2000-04-20
申请人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
发明人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
IPC分类号： A61K5100
CPC分类号： C07K14/585 , A61K38/00
摘要： This invention relates to calcitonin receptor binding reagents Comprising Compounds which are Covalently linked to a radiometal chelator. The invention is embodied as calcitonin receptor binding peptide derivatives and analogues of calcitonin which may be radiolabeled with a suitable isotope and used as radiodiagnostic or radiotherapeutic agents. Methods and kits for making, radiolabeling and using such reagents diagnostically and therapeutically in a mammalian body are also provided.
摘要翻译：本发明涉及包含与放射性金属螯合剂共价连接的化合物的降钙素受体结合试剂。本发明体现为降钙素受体结合肽衍生物和降钙素类似物，其可以用合适的同位素放射标记并用作放射诊断或放射治疗剂。还提供了用于在哺乳动物身体中诊断和治疗地制备，放射性标记和使用这些试剂的方法和试剂盒。

4. 发明授权

US6083480A Calcitonin receptor binding reagents 失效
标题翻译：降钙素受体结合试剂
公开(公告)号：US6083480A
公开(公告)日：2000-07-04
申请号：US847007
申请日：1997-05-01
申请人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
发明人： Richard T. Dean , Larry R. Bush , Daniel A. Pearson , John Lister-James
IPC分类号： A61K51/00 , A61K38/00 , A61K38/23 , A61K49/00 , A61K51/08 , A61P35/00 , C07B59/00 , C07K14/585 , A61M36/14
CPC分类号： C07K14/585 , A61K38/00
摘要： This invention relates to radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to calcitonin receptor binding compounds, preferably peptides, derivatives and analogues of calcitonin, and embodiments of such compounds radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such compounds, particularly peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to calcitonin receptor binding peptide derivatives and analogues of calcitonin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to calcitonin receptor binding peptide derivatives and analogues of calcitonin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re) for use as radiotherapeutic agents. Methods and kits for making, radiolabeling and using such peptides diagnostically and therapeutically in a mammalian body are also provided.
摘要翻译：本发明涉及放射治疗试剂和肽，放射诊断试剂和肽，以及用于产生标记的放射诊断和放射治疗剂的方法。具体地，本发明涉及降钙素受体结合化合物，优选降钙素的肽，衍生物和类似物，以及用放射性同位素放射性标记的这种化合物的实施方案，以及用于制备，放射性标记和使用这些化合物的方法和试剂盒，特别是用于放射诊断和放射治疗目的。本发明具体涉及降钙素受体结合肽衍生物和用锝-99m放射性标记的降钙素的类似物及其用作闪烁照相成像剂。本发明还具体涉及降钙素受体结合肽衍生物和放射性标记的细胞毒性放射性同位素如铼-186（186Re）和铼-188（188Re）用作放射治疗剂的降钙素的类似物。还提供了用于在哺乳动物体内制造，放射性标记和诊断和治疗上使用这些肽的方法和试剂盒。

5. 发明授权

US5849261A Radiolabeled vasoactive intestinal peptides for diagnosis and therapy 失效
标题翻译：放射性标记的血管活性肠肽用于诊断和治疗
公开(公告)号：US5849261A
公开(公告)日：1998-12-15
申请号：US414424
申请日：1995-03-31
申请人： Richard T. Dean , Daniel A. Pearson , John Lister-James , Edgar R. Civitello
发明人： Richard T. Dean , Daniel A. Pearson , John Lister-James , Edgar R. Civitello
IPC分类号： A61K51/00 , A61K51/08 , A61P35/00 , A61P43/00 , C07B59/00 , C07K7/06 , C07K14/575 , C07K14/775 , A61M36/14
CPC分类号： C07B59/008 , A61K51/08 , A61K51/088 , C07K14/775 , C07K7/06 , A61K2121/00 , A61K2123/00
摘要： This invention relates to radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to VIP receptor binding peptides, derivatives and analogues of VIP, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to VIP receptor binding peptide derivatives and analogues of VIP radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to VIP receptor binding peptide derivatives and analogues of VIP radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re) for use as radiotherapeutic agents. Methods and kits for making, radiolabeling and using such peptides diagnostically and therapeutically in a mammalian body are also provided.
摘要翻译：本发明涉及放射治疗试剂和肽，放射诊断试剂和肽，以及用于产生标记的放射诊断和放射治疗剂的方法。具体地，本发明涉及VIP受体结合肽，VIP的衍生物和类似物，以及用放射性同位素放射性标记的这种肽的实施方案，以及用于制造，放射性标记和使用这些肽用于放射诊断和放射治疗目的的方法和试剂盒。本发明具体涉及VIP受体结合肽衍生物和用锝-99m放射标记的VIP的类似物及其用作闪烁照相成像剂。本发明还具体涉及VIP受体结合肽衍生物和用细胞毒性放射性同位素如铼-186（186Re）和铼-188（188Re）放射性标记的VIP作为放射治疗剂的类似物。还提供了用于在哺乳动物体内制造，放射性标记和诊断和治疗上使用这些肽的方法和试剂盒。

6. 发明授权

US06358491B1 Somatostatin analogs 失效
标题翻译：生长抑素类似物
公开(公告)号：US06358491B1
公开(公告)日：2002-03-19
申请号：US09397792
申请日：1999-09-16
申请人： John Lister-James , Richard T. Dean , Daniel A. Pearson , David M. Wilson
发明人： John Lister-James , Richard T. Dean , Daniel A. Pearson , David M. Wilson
IPC分类号： A61K5100
CPC分类号： C07K14/6555 , A61K38/00 , A61K51/08 , A61K51/083 , A61K51/088
摘要： The invention provides novel peptide-based pharmacophores and compounds which bind somatostatin receptors with high affinity and which exhibit improved pharmacokinetic properties over known somatostatin analogs. The pharmacophores and compounds of the invention may be used in labeled or unlabeled form for diagnosing and/or treating somatostatin responsive diseases. The invention also provides radiopharmaceuticals and kits comprising these compounds, as well as methods for diagnosing and/or treating somatostatin receptor mediated diseases.
摘要翻译：本发明提供了新颖的基于肽的药效学和与高亲和力结合生长抑素受体的化合物，并且与已知的生长抑素类似物相比表现出改进的药代动力学性质。本发明的药效团和化合物可以以标记或未标记的形式用于诊断和/或治疗生长抑素反应性疾病。本发明还提供包含这些化合物的放射性药物和试剂盒，以及用于诊断和/或治疗生长抑素受体介导的疾病的方法。

7. 发明授权

US6007792A Radiolabeled vasoactive intestinal peptides for diagnosis and therapy 失效
标题翻译：放射性标记的血管活性肠肽用于诊断和治疗
公开(公告)号：US6007792A
公开(公告)日：1999-12-28
申请号：US930845
申请日：1998-01-21
申请人： Richard T. Dean , Daniel A. Pearson , John Lister-James , Edgar R. Civitello
发明人： Richard T. Dean , Daniel A. Pearson , John Lister-James , Edgar R. Civitello
IPC分类号： A61K51/00 , A61K51/08 , A61P35/00 , A61P43/00 , C07B59/00 , C07K7/06 , C07K14/575 , C07K14/775 , A61M36/14
CPC分类号： C07B59/008 , A61K51/08 , A61K51/088 , C07K14/775 , C07K7/06 , A61K2121/00 , A61K2123/00
摘要： This invention relates to radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to vasoactive intestinal peptide receptor binding peptides, derivatives and analogues of vasoactive intestinal peptide, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to vasoactive intestinal peptide receptor binding peptide derivatives and analogues of vasoactive intestinal peptide radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to vasoactive intestinal peptide receptor binding peptide derivatives and analogues of vasoactive intestinal peptide radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re) for use as radiotherapeutic agents. Methods and kits for making, radiolabeling and using such peptides diagnostically and therapeutically in a mammalian body are also provided.
摘要翻译： PCT No.PCT / US96 / 04308 Sec。 371日期1998年1月21日 102（e）日期1998年1月21日PCT 1996年3月29日PCT公布。 WO96 / 30055 PCT公开日期1996年10月3日本发明涉及放射治疗试剂和肽，放射诊断试剂和肽，以及用于制备标记的放射性诊断和放射治疗剂的方法。具体地，本发明涉及血管活性肠肽受体结合肽，血管活性肠肽的衍生物和类似物以及用放射性同位素放射性标记的这些肽的实施方案，以及用于制备放射性标记和使用这些肽用于放射诊断和放射治疗目的的方法和试剂盒。本发明具体涉及放射性标记有锝-99m的血管活性肠肽受体结合肽衍生物和血管活性肠肽的类似物及其用作闪烁照相成像剂。本发明还特别涉及放射性标记用细胞毒性放射性同位素如铼-186（186Re）和铼-188（188Re）用作放射治疗剂的血管活性肠肽受体结合肽衍生物和血管活性肠肽的类似物。还提供了用于在哺乳动物体内制造，放射性标记和诊断和治疗上使用这些肽的方法和试剂盒。

8. 发明授权

US5670479A .alpha.-ketoamide derivatives as inhibitors of thrombosis 失效
标题翻译： α-酮酰胺衍生物作为血栓形成的抑制剂
公开(公告)号：US5670479A
公开(公告)日：1997-09-23
申请号：US218329
申请日：1994-03-25
申请人： Matthew M. Abelman , Daniel A. Pearson , George P. Vlasuk , Thomas R. Webb
发明人： Matthew M. Abelman , Daniel A. Pearson , George P. Vlasuk , Thomas R. Webb
IPC分类号： A61K38/00 , A61K49/00 , A61K51/08 , A61P7/02 , C07K5/02 , C07K7/02 , C07K14/815 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/0202 , A61K51/088 , C07K14/815 , A61K2123/00 , A61K38/00
摘要： a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described. a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described. Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.
摘要翻译：描述了可用于预防或治疗哺乳动物特征在于血栓形成的病理状态的α-酮酰胺衍生物，其药学上可接受的盐，组合物，诊断组合物和药物组合物。还描述了可用于哺乳动物血栓体内成像的α-酮酰胺衍生物，其药学上可接受的盐，组合物和诊断组合物。还公开了在哺乳动物中预防或治疗血栓形成的特征的病理状态和哺乳动物血栓体内成像方法。

9. 发明授权

US5714580A Trypsin Inhibitors 失效
标题翻译：胰蛋白酶抑制剂
公开(公告)号：US5714580A
公开(公告)日：1998-02-03
申请号：US455974
申请日：1995-05-31
申请人： Terence K. Brunck , Michael G. Pepe , Daniel A. Pearson , Thomas R. Webb
发明人： Terence K. Brunck , Michael G. Pepe , Daniel A. Pearson , Thomas R. Webb
IPC分类号： A61K38/55 , A61P1/00 , C07C251/76 , C07C281/10 , C07K1/113 , C07K5/072 , C07K5/078 , C07K5/093 , C07K14/81 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/06139 , C07C281/10 , C07K5/06104 , C07K5/06113
摘要： Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.
摘要翻译：公开了具有抗胰蛋白酶活性的新型化合物。具体地说，具有作为哺乳动物胰腺胰蛋白酶抑制剂的实质效力和特异性的新型肽醛类似物。该化合物可用于预防和治疗与胰腺炎相关的组织损伤或破坏。

10. 发明授权

US06989138B2 Stabilization of radiopharmaceutical compositions using hydrophilic thioethers and hydrophilic 6-hydroxy chromans 失效
公开(公告)号：US06989138B2
公开(公告)日：2006-01-24
申请号：US10131546
申请日：2002-04-24
申请人： John E. Cyr , Daniel A. Pearson
发明人： John E. Cyr , Daniel A. Pearson
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/12
摘要： Radiopharmaceutical compositions which are stabilized by addition of a mixture of a hydrophilic thioether and a hydrophilic 6-hydroxy-chroman derivative.

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