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公开(公告)号：US06664367B1
公开(公告)日：2003-12-16
申请号：US08278437
申请日：1994-07-21
IPC分类号： C07K1600
CPC分类号： C07K14/655 , C07K1/006 , C07K7/16 , C07K14/52 , C07K14/6555 , C07K14/70 , Y10S930/28
摘要： Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c) thioketal expansion, or (d) alkylation expansion. In sulfide contraction the disulfide bond (—S—S—) is replaced with a monosulfide bond (—S—) in which a bifunctional effector molecule, such as a ligand or chemotoxic agent, is bound to the new peptide linkage. In isosteric substitution, one sulfur atom is replaced with a carbon atom and at least one of the carbon atoms at the modified site is a bifunctional effector molecule. In thioketal expansion, an alkylidene unit (—CR1C2—) is inserted between the two sulfur atoms. In alkylation expansion, an alkyl moiety of from C2 to C3, is inserted between the two sulfur atoms.
摘要翻译： 公开了含有二硫键的环肽的稳定类似物。 二硫键通过四种方法之一进行改性：（a）硫化物收缩，（b）等排取代，（c）硫代缩酮扩展或（d）烷基化扩展。 在硫化物收缩中，二硫键（-S-S-）用单硫键（-S-）代替，其中双功能效应分子如配体或化学毒性剂与新的肽键结合。 在等排取代中，一个硫原子被碳原子取代，并且在修饰位点处的至少一个碳原子是双功能效应子分子。 在硫缩酮扩展中，在两个硫原子之间插入亚烷基单元（-CR1C2-）。 在烷基化扩展中，C2至C3的烷基部分插入在两个硫原子之间。
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公开(公告)号：US5804157A
公开(公告)日：1998-09-08
申请号：US989434
申请日：1997-12-12
IPC分类号： A61K51/00 , A61K51/08 , A61P35/00 , C07K14/655 , A61M36/14
CPC分类号： C07K14/6555 , A61K51/083 , A61K51/088
摘要： This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified carboxy terminal amino acid. The radiopharmaceutical composition may be used for targeting a selected biological site. The radiolabeled peptide is characterized by having its carboxy terminal amino acid in its carboxylic acid form and the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent. The radiopharmaceutical composition preferably comprises a radiolabeled peptide selected from the group consisting of somatostatin, an analog of somatostatin, a derivative of somatostatin and peptides capable of binding to the somatostatin receptor, where the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent has its carboxy terminal amino acid in its carboxylic acid form.
摘要翻译： 本发明涉及用于放射性药物用途的放射性标记肽组合物，更具体地，涉及具有未修饰的羧基末端氨基酸的用于诊断或治疗用途的放射性标记肽。 放射性药物组合物可以用于靶向选定的生物部位。 放射性标记的肽的特征在于其羧基末端氨基酸为羧酸形式，肽通过螯合剂偶联至诊断或治疗放射性核素。 放射性药物组合物优选包含选自生长抑素，生长抑素类似物，生长抑素衍生物和能够结合生长抑素受体的肽的放射性标记的肽，其中肽通过螯合剂偶联至诊断或治疗放射性核素 其羧基末端氨基酸呈羧酸形式。
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43.发明授权Method of radiolabeling chelating compounds comprising sulfur atoms with metal radionuclides 失效包含硫原子的螯合化合物与金属放射性核素放射性标记的方法
公开(公告)号：US5021556A
公开(公告)日：1991-06-04
申请号：US212688
申请日：1988-07-01
IPC分类号： A61K51/04 , C07C323/60 , C07C327/24 , C07D285/00 , C07D309/08 , C07F13/00 , C07H15/14
CPC分类号： C07D285/00 , A61K51/0478 , A61K51/0491 , C07C323/60 , C07C327/24 , C07D309/08 , C07F13/005 , C07H15/14 , A61K2123/00 , Y02P20/55
摘要： Chelating compounds which comprise one or more sulfur atoms and are to be radiolabeled with metal radionuclides to form the corresponding chelates are disclosed. The chelating compounds comprise thioacetal or hemithioacetal sulfur protecting groups which are displaced during the radiolabeling reaction, which is conducted at acidic pH, such that bonds form between said sulfur atoms and said radionuclide. The resulting metal radionuclide chelates have diagnostic and therapeutic medical uses.
摘要翻译： 公开了包含一个或多个硫原子并且与金属放射性核素进行放射性标记以形成相应螯合物的螯合化合物。 螯合化合物包括在酸性pH下进行的放射性标记反应期间被置换的硫代缩醛或半硫缩醛硫保护基，使得在所述硫原子和所述放射性核素之间形成键。 所得金属放射性核素螯合物具有诊断和治疗用途。
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44.发明授权Radiolabeled peptides for the diagnosis and treatment of breast and prostate tumors and metastases of such tumors 失效放射性标记的肽用于诊断和治疗乳腺和前列腺肿瘤以及这种肿瘤的转移公开(公告)号：US06866837B2
公开(公告)日：2005-03-15
申请号：US10248668
申请日：2003-02-06
摘要： Compounds and methods for the diagnosis and treatment of tumors, including breast and prostate tumors and metastases thereof using radiolabelled peptides that bind to GRP receptors. The peptides are Bombesin analogs wherein the first and optionally the third amino acid are modified.
摘要翻译： 使用与GRP受体结合的放射性标记肽来诊断和治疗肿瘤的化合物和方法，包括乳腺和前列腺肿瘤及其转移。 所述肽是Bombesin类似物，其中第一个和任选的第三个氨基酸被修饰。
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45.发明授权
公开(公告)号：US6132697A
公开(公告)日：2000-10-17
申请号：US870042
申请日：1997-06-05
申请人： Ananthachari Srinivasan , Larry P. Feigen , Daniel Lee Flynn , Jeffery Alan Zablocki , Philip Needleman , Michelle A. Schmidt
发明人： Ananthachari Srinivasan , Larry P. Feigen , Daniel Lee Flynn , Jeffery Alan Zablocki , Philip Needleman , Michelle A. Schmidt
CPC分类号： C07K5/06113 , A61K51/088 , A61K2121/00 , A61K2123/00
摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.
摘要翻译： 提供了能够在哺乳动物体内含有活化血小板的血栓位点定位的放射性药物，其中放射性药物包含能够特异性结合血栓中血小板的GPIIb / IIIa整联蛋白受体的线性拟肽含量配体和共价结合的放射性核素 含有拟肽的配体。 提供本发明的配体组合物与所选择的金属放射性核素复合以形成诊断或治疗性放射性药物，以分别对血栓位点成像或向血栓部位提供放射治疗。 通过施用诊断上有效量的本发明的放射性药物组合物与选定的诊断性金属放射性核素复合而在哺乳动物体内成像血栓位点的方法和通过施用治疗有效的方法向哺乳动物体内的血栓位点提供治疗 还提供了与选定的治疗性金属放射性核素复合的本发明的放射性药物组合物的量以及用于制备这种放射性药物组合物的试剂盒。
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公开(公告)号：US5830431A
公开(公告)日：1998-11-03
申请号：US480373
申请日：1995-06-07
IPC分类号： A61K51/00 , A61K51/08 , A61P35/00 , C07K14/655 , A61M36/14
CPC分类号： C07K14/6555 , A61K51/083 , A61K51/088
摘要： This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified carboxy terminal amino acid. The radiopharmaceutical composition may be used for targeting a selected biological site. The radiolabeled peptide is characterized by having its carboxy terminal amino acid in its carboxylic acid form and the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent. The radiopharmaceutical composition preferably comprises a radiolabeled peptide selected from the group consisting of somatostatin, an analog of somatostatin, a derivative of somatostatin and peptides capable of binding to the somatostatin receptor, where the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent has its carboxy terminal amino acid in its carboxylic acid form.
摘要翻译： 本发明涉及用于放射性药物用途的放射性标记肽组合物，更具体地，涉及具有未修饰的羧基末端氨基酸的用于诊断或治疗用途的放射性标记肽。 放射性药物组合物可以用于靶向选定的生物部位。 放射性标记的肽的特征在于其羧基末端氨基酸为羧酸形式，肽通过螯合剂偶联至诊断或治疗放射性核素。 放射性药物组合物优选包含选自生长抑素，生长抑素类似物，生长抑素衍生物和能够结合生长抑素受体的肽的放射性标记的肽，其中肽通过螯合剂偶联至诊断或治疗放射性核素 其羧基末端氨基酸呈羧酸形式。
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公开(公告)号：US5656253A
公开(公告)日：1997-08-12
申请号：US255148
申请日：1994-06-07
IPC分类号： A61K51/04 , A61K51/08 , C07B59/00 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/00 , C07K14/655 , C07K14/815 , A61K51/00 , A61K7/32 , C07D211/70 , C07D401/02
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/088 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555 , A61K2121/00 , A61K2123/00
摘要： The present invention relates particularly to novel pyridine based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, novel aminothiol ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, and amide-thiolate ligands having improved metal chelate formation kinetics. The amide-thiolate ligands include an amine which converts to a vinylogous amide upon complexation, thereby providing rapid complexation and thermodynamic stability. The ligands may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.
摘要翻译： 本发明特别涉及适用于与放射性核素络合的新型吡啶类氮硫配体，并且可用作诊断目的的一般成像剂，适于与放射性核素络合的新型氨基硫醇配体，并且可用作一般 用于诊断目的的成像剂和具有改善的金属螯合物形成动力学的酰胺 - 硫醇酸配体。 酰胺 - 硫醇酸酯配体包括在络合时转化为戊烯酰胺的胺，从而提供快速的络合和热力学稳定性。 配体可用于生物物质的后期标记用于诊断和治疗领域。
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48.发明授权
公开(公告)号：US5653958A
公开(公告)日：1997-08-05
申请号：US419319
申请日：1995-04-10
IPC分类号： C07D233/64 , A61K51/00 , A61K51/04 , C07D233/54 , C07D233/91 , C07D405/12 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0478 , C07D233/64 , C07D405/12 , A61K2123/00
摘要： The present invention relates particularly to novel imidazole based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
摘要翻译： 本发明特别涉及适用于与放射性核素络合的新型咪唑基氮硫配体，并且可用作用于诊断目的的一般成像剂。
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公开(公告)号：US5310536A
公开(公告)日：1994-05-10
申请号：US832149
申请日：1992-02-06
IPC分类号： A61K51/04 , A61K51/08 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/00 , A61K49/02 , A61K43/00
CPC分类号： C07F13/005 , A61K51/0478 , A61K51/088 , C07D213/40 , C07D213/64 , C07D213/68 , A61K2121/00 , A61K2123/00
摘要： Amide-thiolate ligands having improved metal chelate formation kinetics are disclosed. The ligands include a tertiary amine strategically located to facilitate rapid formation of an amine-amide-thiolate intermediate complex, followed by transfer of the metal to a thermodynamically stable amide-thiolate complex. The amide-thiolate ligands of the present invention may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.
摘要翻译： 公开了具有改进的金属螯合物形成动力学的酰胺 - 硫醇盐配体。 配体包括策略性定位以促进胺 - 酰胺 - 硫醇盐中间体复合物的快速形成，然后将金属转移到热力学稳定的酰胺 - 硫醇盐络合物的叔胺。 本发明的酰胺 - 硫醇酸酯配体可用于在诊断和治疗领域中用于生物物质的后成形标记。
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公开(公告)号：US5112954A
公开(公告)日：1992-05-12
申请号：US176851
申请日：1988-04-04
IPC分类号： C07D233/91 , A61K39/395 , A61K45/00 , A61K47/48 , A61K51/00 , A61P35/00 , C07D207/452 , C07K14/00 , C07K14/705 , C07K14/715 , C07K16/00
CPC分类号： A61K47/48715
摘要： The activity of cytotoxic agents on target cells is enhanced through administration of a sensitizing agent to a patient prior to or simultaneously with administration of the cytotoxic agent. One or both of the two types of agents are attached to antibodies specific for the desired target cells, thereby enhancing the cytotoxic effect on target cells compared to non-target cells. The sensitizer and/or the cytotoxic agent may be attached to monoclonal antibodies specific for cancer cells to selectively eradicate the cancer cells while minimizing toxicity toward normal tissues.
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