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91. 发明授权

US6027711A Structurally determined metallo-constructs and applications 失效
标题翻译：结构确定的金属构造和应用
公开(公告)号：US6027711A
公开(公告)日：2000-02-22
申请号：US660697
申请日：1996-06-05
申请人： Shubh D. Sharma
发明人： Shubh D. Sharma
IPC分类号： A61K38/00 , A61K49/00 , A61K51/00 , A61K51/04 , A61K51/08 , A61P35/00 , A61P37/04 , A61P43/00 , C07K5/11 , C07K7/06 , A61M36/14
CPC分类号： C40B30/04 , A61K51/0497 , A61K51/08 , A61K51/082 , A61K51/083 , A61K51/086 , A61K51/088 , C40B40/16 , C40B50/06 , C40B50/14 , A61K2121/00 , A61K2123/00
摘要： A metallo-construct, which may be a peptide, is provided for use as a biological, therapeutic, diagnostic imaging, or radiotherapeutic agent, and for use in library or combinatorial chemistry methods. The construct has a conformationally constrained global secondary structure obtained upon complexing with a metal ion. The peptide constructs are of the general formula:R.sub.1 --X--R.sub.2where X is a plurality of amino acids and includes a complexing backbone for complexing metal ions, so that substantially all of the valences of the metal ion are satisfied upon complexation of the metal ion with X, resulting in a specific regional secondary structure forming a part of the global secondary structure; and where R.sub.1 and R.sub.2 each include from 0 to about 20 amino acids, the amino acids being selected so that upon complexing the metal ion with X at least a portion of either R.sub.1 or R.sub.2 or both have a structure forming the balance of the conformationally constrained global secondary structure. All or a portion of the global secondary structure, which may be sychnologic or rhegnylogic, may form a ligand or mimic a known biological-function domain. The construct has substantially higher affinity for its target upon labeling with a metal ion.
摘要翻译：提供可以是肽的金属构建体用作生物，治疗，诊断成像或放射治疗剂，并用于文库或组合化学方法。该构型具有在与金属离子络合时获得的构象约束的全局二级结构。肽构建体具有以下通式：R1-X-R2其中X是多个氨基酸，并且包括用于络合金属离子的络合骨架，使得当金属离子络合时，金属离子的几乎所有价态都得到满足与X，导致特定的区域二级结构构成全球二级结构的一部分; 并且其中R 1和R 2各自包含0至约20个氨基酸，所述氨基酸被选择为使得当金属离子与X配合时，R 1或R 2或两者的至少一部分具有形成构象约束的平衡的结构全球二级结构。全部或部分全球二级结构（可能是系统的或流行的）可以形成配体或模拟已知的生物功能结构域。该构建体在用金属离子标记时对其靶具有显着更高的亲和力。

92. 发明授权

US5997845A Technetium-99M labeled peptides for imaging inflammation 失效
标题翻译：锝-99M标记的肽用于成像炎症
公开(公告)号：US5997845A
公开(公告)日：1999-12-07
申请号：US902367
申请日：1997-07-29
申请人： Richard T. Dean , John Lister-James , Edgar R. Civitello
发明人： Richard T. Dean , John Lister-James , Edgar R. Civitello
IPC分类号： A61K51/04 , A61K51/08 , C07D211/22 , C07K5/02 , C07K5/103 , C07K7/06 , A61K51/00 , A61M36/14
CPC分类号： A61K51/0478 , A61K51/08 , A61K51/082 , A61K51/088 , C07D211/22 , C07K5/0215 , C07K5/1008 , C07K7/06 , A61K2123/00
摘要： This invention relates to radiolabeled scintigraphic imaging agents, and methods and reagents for producing such agents. Specifically, the invention relates to specific binding compounds, including peptides, that bind to a platelet receptor that is the platelet GPIIb/IIIa receptor, methods and kits for making such compounds, and methods for using such compounds labeled with technetium-99m via a covalently-linked radiolabel-binding moiety to image thrombi in a mammalian body.
摘要翻译：本发明涉及放射性标记的闪烁照相成像剂，以及用于制备这种试剂的方法和试剂。具体地，本发明涉及结合血小板GPIIb / IIIa受体的血小板受体的特异性结合化合物，包括肽，用于制备这些化合物的方法和试剂盒，以及通过共价方法使用锝-99m标记的化合物的方法连接的放射性标记结合部分以在哺乳动物体内成像血栓。

93. 发明授权

US5965107A Technetium-99m labeled peptides for imaging 失效
标题翻译：锝-99m标记肽成像
公开(公告)号：US5965107A
公开(公告)日：1999-10-12
申请号：US871282
申请日：1992-04-20
申请人： Richard T. Dean , Scott Buttram , William McBride , John Lister-James , Edgar R. Civitello
发明人： Richard T. Dean , Scott Buttram , William McBride , John Lister-James , Edgar R. Civitello
IPC分类号： A61K51/00 , A61K51/08 , C07F13/00 , C07K1/113 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/47 , C07K14/745 , C07K14/75 , A61M36/14
CPC分类号： A61K51/088 , A61K51/08 , A61K51/082 , A61K2121/00 , A61K2123/00
摘要： This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via a radiolabel-binding moiety which forms a neutral complex with Tc-99m.
摘要翻译：本发明涉及放射性标记的肽及其生产方法。具体地说，本发明涉及用于制备这些肽的肽，方法和试剂盒，以及使用这些肽以经锝-99m（Tc-99m）标记的哺乳动物体内的位点，通过形成中性复合物的放射性标记结合部分与Tc-99m。

94. 发明授权

US5879659A Ternary radiopharmaceutical complexes 失效
标题翻译：三元放射性药物复合物
公开(公告)号：US5879659A
公开(公告)日：1999-03-09
申请号：US808699
申请日：1997-02-28
申请人： David Scott Edwards , Shuang Liu
发明人： David Scott Edwards , Shuang Liu
IPC分类号： A61B20060101 , A61K20060101 , A61K51/08 , A61M20060101 , A61N20060101 , A61K51/00 , A61K38/12 , A61M36/14 , C07F5/00
CPC分类号： A61K51/088 , A61K51/082 , A61K2123/00
摘要： This invention relates to novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer, and to kits useful for their preparation. The radiopharmaceuticals of this invention are comprised of a transition metal radionuclide, a transition metal chelator, a biologically active group connected to said chelator, a first ancillary ligand, a second ancillary ligand capable of stabilizing the radiopharmaceutical, optionally having a linking group between said chelator and said biologically active group. Preferred radiopharmaceuticals of this invention have the formula:�(Q).sub.d' L.sub.n --C.sub.h' !.sub.x --M.sub.t (A.sub.L1).sub.y (A.sub.L2).sub.z,wherein the shown variables are as defined herein.
摘要翻译：本发明涉及可用作诊断心血管疾病，感染性疾病和癌症的成像剂的新型放射性药物，以及可用于其制备的试剂盒。本发明的放射性药物包括过渡金属放射性核素，过渡金属螯合剂，与所述螯合剂连接的生物活性基团，第一辅助配体，能稳定放射性药物的第二辅助配体，任选地在所述螯合剂之间具有连接基团并表示生物活性组。本发明优选的放射性药物具有下式：[（Q）d'Ln-Ch'] x-Mt（AL1）y（AL2）z，其中所示变量如本文所定义。

95. 发明授权

US5814297A Technetium-99m labeled peptides for imaging having a single thiol containing moiety 失效
标题翻译：用于成像具有单一含硫醇部分的锝-99m标记的肽
公开(公告)号：US5814297A
公开(公告)日：1998-09-29
申请号：US471741
申请日：1995-06-06
申请人： Richard T. Dean , William McBride , Scott Buttram
发明人： Richard T. Dean , William McBride , Scott Buttram
IPC分类号： A61K51/00 , A61K38/00 , A61K51/08 , C07B59/00 , C07F13/00 , C07K5/10 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/775 , A61M36/14
CPC分类号： C07K7/06 , A61K51/08 , A61K51/082 , A61K51/088 , C07B59/008 , C07K14/775 , A61K2121/00 , A61K2123/00 , A61K38/00 , Y10S930/28
摘要： The invention relates to radiolabeled imaging of a mammalian body. The invention in particular provides for reagents labeled with technetium-99m for such imaging. The invention provides peptides which bind Tc-99m and which can be targeted to specific sites within a mammalian body.
摘要翻译：本发明涉及哺乳动物体的放射性标记成像。本发明特别提供了用于这种成像的用锝-99m标记的试剂。本发明提供结合Tc-99m并可靶向哺乳动物体内特定位点的肽。

96. 发明授权

US5776428A Technetium-99m labeled peptides for imaging 失效
公开(公告)号：US5776428A
公开(公告)日：1998-07-07
申请号：US468975
申请日：1995-06-06
申请人： Richard T. Dean , Scott Buttram , William McBride , John Lister-James , Edgar R. Civitello
发明人： Richard T. Dean , Scott Buttram , William McBride , John Lister-James , Edgar R. Civitello
IPC分类号： A61K51/00 , A61K51/08 , C07F13/00 , C07K1/113 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/47 , C07K14/745 , C07K14/75 , A61M36/14
CPC分类号： A61K51/088 , A61K51/08 , A61K51/082 , A61K2121/00 , A61K2123/00
摘要： This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via a radiolabel-binding moiety which forms a neutral complex with Tc-99m.

97. 发明授权

US09957293B2 Conjugates of RGD peptides and porphyrin or (bacterio)chlorophyll photosynthesizers and their uses 有权
公开(公告)号：US09957293B2
公开(公告)日：2018-05-01
申请号：US13447825
申请日：2012-04-16
申请人： Avigdor Scherz , Yoram Salomon , Efrat Rubinstein , Alexander Brandis , Doron Eren , Karin Neimann
发明人： Avigdor Scherz , Yoram Salomon , Efrat Rubinstein , Alexander Brandis , Doron Eren , Karin Neimann
IPC分类号： C07K5/12 , C07K5/09 , C07K5/10 , C07K7/06 , C07K7/64 , A61K41/00 , A61K51/08 , G01N33/574 , A61K47/64 , A61K51/00 , A61M36/14
CPC分类号： C07K5/123 , A61K41/00 , A61K41/0071 , A61K47/64 , A61K51/082 , A61K51/088 , C07K5/0817 , C07K5/10 , C07K5/126 , C07K7/06 , C07K7/64 , G01N33/57426 , G01N2333/96411
摘要： Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and nonneoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.

98. 发明授权

US09896480B2 Integrin receptor antagonists and their methods of use 有权
公开(公告)号：US09896480B2
公开(公告)日：2018-02-20
申请号：US13467995
申请日：2012-05-09
申请人： Michael John Mackel , John Y. Park , Hampar L. Karageozian , Vicken H. Karageozian
发明人： Michael John Mackel , John Y. Park , Hampar L. Karageozian , Vicken H. Karageozian
IPC分类号： A61K38/06 , C07K5/09 , A61K51/08 , C07K7/06 , C07K7/64 , A61K9/08 , A61K38/08 , A61K38/12 , A61K38/17 , A61K39/395 , A61K51/06 , A61L26/00 , A61L27/00 , A61L27/22 , A61L31/04 , G01N1/00 , A61K47/64 , A61K9/06
CPC分类号： C07K5/0817 , A61K9/06 , A61K9/08 , A61K38/06 , A61K38/08 , A61K38/12 , A61K38/1709 , A61K39/3955 , A61K47/64 , A61K51/065 , A61K51/082 , A61K51/088 , A61L26/00 , A61L27/00 , A61L27/227 , A61L31/043 , A61L2300/252 , C07K7/06 , C07K7/64 , G01N1/00
摘要： Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH2—SO3H)COOH or Arg-Gly-NH—CH(CH2—SO3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting integrins including but not necessarily limited to α5β1-Integrin, αvβ3-Integrin and αvβ5-Integrin, inhibiting cellular adhesion to RGD binding sites, preventing or treating viral or other microbial infections, inhibiting angiogenesis in tumors, retinal tissue or other tissues or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

99. 发明申请

US20170267698A1 NITROGEN-CONTAINING MACROCYCLIC CONJUGATES AS RADIOPHARMACEUTICALS 审中-公开
公开(公告)号：US20170267698A1
公开(公告)日：2017-09-21
申请号：US15612009
申请日：2017-06-02
申请人： THE UNIVERSITY OF MELBOURNE
发明人： Paul Stephen DONNELLY , Michelle Therese Ma , Denis Bernard Scanlon
IPC分类号： C07D521/00 , A61K51/04 , A61K51/08
CPC分类号： C07D521/00 , A61K49/06 , A61K49/08 , A61K49/10 , A61K49/101 , A61K51/00 , A61K51/02 , A61K51/04 , A61K51/0482 , A61K51/082 , A61K51/088
摘要： The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

100. 发明申请

US20170174723A1 BI-TERMINAL PEGYLATED INTEGRIN-BINDING PEPTIDES AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20170174723A1
公开(公告)日：2017-06-22
申请号：US15292564
申请日：2016-10-13
申请人： The Regents of the University of California
发明人： Sven H. Hausner , Julie L. Sutcliffe
IPC分类号： C07K7/06 , A61K31/337 , A61K51/08
CPC分类号： C07K7/06 , A61K31/337 , A61K38/00 , A61K47/60 , A61K47/64 , A61K51/082 , C07K14/70546 , C12N2770/32122
摘要： The present invention provides bi-terminal PEGylated peptide conjugates that target an integrin such as αvβ6 integrin. In particular embodiments, the peptide conjugates of the present invention further comprise a biological agent such as an imaging agent or a therapeutic agent, e.g., covalently attached to one of the PEG moieties. The peptide conjugates of the present invention are particularly useful for imaging a tumor, organ, or tissue and for treating integrin-mediated diseases and disorders such as cancer, inflammatory diseases, autoimmune diseases, chronic fibrosis, chronic obstructive pulmonary disease (COPD), lung emphysema, and chronic wounding skin disease. Compositions and kits containing the peptide conjugates of the present invention find utility in a wide range of applications including, e.g., in vivo imaging and immunotherapy.

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