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1. 发明公开

EP3303349A2 NOVEL HETEROAROMATIC SILICON-FLUORIDE-ACCEPTORS USEFUL FOR 18F LABELING OF MOLECULES AND BIOMOLECULES, AND METHODS OF PREPARING SAME 有权转让
标题翻译：用于18 F标记分子和生物分子的新型异质硅 - 氟化物 - 接受体及其制备方法
公开(公告)号：EP3303349A2
公开(公告)日：2018-04-11
申请号：EP16800638.5
申请日：2016-05-24
申请人： The Regents of the University of California
发明人： WALDMANN, Christopher, Martin , TOUTOV, Anton, A. , MURPHY, Jennifer, Marie , GRUBBS, Robert, H.
IPC分类号： C07F7/08 , C07F13/00 , C07F19/00 , A61K51/04
CPC分类号： C07F7/12 , A61K51/1027 , A61K51/1072 , C07B59/004 , C07B2200/05
摘要： The present invention includes novel compounds and compositions including heteroaromatic Silicon-Fluoride-Acceptors, which are useful for PET scanning. The present invention further includes a novel method of 18F imaging for PET scanning, the method comprising the preparation of conjugates and bioconjugates of biological ligands of interest with heteroaromatic SiFAs. In one embodiment the invention is practiced in the form of a kit.

2. 发明公开

EP3288952A1 ORGANOTRIFLUOROBORATE MIMICS OF AMINO ACIDS AND USES THEREOF 审中-公开
标题翻译：氨基酸的有机三氟硼酸盐模拟物及其用途
公开(公告)号：EP3288952A1
公开(公告)日：2018-03-07
申请号：EP16787230.8
申请日：2016-04-29
申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services
发明人： LIU, Zhibo , CHEN, Xiaoyuan
IPC分类号： C07F5/02 , A61B5/00 , C07B59/00
CPC分类号： C07F5/02 , A61B5/4839 , A61B5/4842 , C07B59/004 , C07F5/025
摘要： Disclosed are boron mimics of amino acids which are compounds, salts, solvates, or stereoisomers of the Formula (I): wherein A, R.1, R2, and R3 are defined herein, and processes for the preparation of the compounds, salts, solvates, or stereoisomers. The compounds, salts, solvates, or stereoisomers of Formula (I) may be used in boron neutron capture therapy. The compounds, salts, solvates, or stereoisomers of Formula (I) with at least one fluorine being, 18F are useful for imaging tumors using positron emission tomography and for evaluating the treatment potential of anti-cancer drugs.

3. 发明公开

EP2392012A4 COMPOSITIONS FOR RADIOLABELING DIETHYLENETRIAMINEPENTAACETIC ACID (DTPA)-DEXTRAN 有权转让
标题翻译：组合物RADIOKATIVEN打标二乙葡聚糖
公开(公告)号：EP2392012A4
公开(公告)日：2012-11-14
申请号：EP10736135
申请日：2010-01-28
申请人： NEOPROBE CORP
发明人： MAGNESON GERALD ROSS , ORAHOOD RICHARD CUSHMAN
IPC分类号： A61K51/06 , G01N33/534 , G01N33/60
CPC分类号： C07B59/005 , A61K51/0491 , A61K51/065 , C07B59/001 , C07B59/004 , C07B63/04 , C07B2200/05 , G01N33/534 , G01N33/60
摘要： The subject invention relates to the compositions for radiolabeling Diethylenetriaminepentaacetic Acid (DTPA)-dextran with Technetium-99m and for stabilizing the DTPA-dextran Cold Kit. The composition contains Stannous Chloride ions to reduce 99mTc-pertechnetate, Ascorbic Acid to reduce stannic ions to stannous ions to maintain a reducing environment, α,α-Trehalose to add bulk and to stabilize the lyophilized composition without interfering with the radiochemical yield, and Glycine to transchelate Technetium-99m under highly acidic conditions to facilitate radiolabeling DTPA-dextran with high radiochemical purity. In addition, the invention pertains to methods for making and using the compositions. The reconstitution of the lyophilized composition by 99mTc-pertechnetate, resulting in radiolabeled 99mTc-DTPA-dextran in a composition between pH 3 to 4. This invention contains a Diluent vial, which when used will shift the pH to a moderately acidic pH, which would provide less pain on injection and ease-of-use to clinical practioners for adjusting its potency.

4. 发明公开

EP1723161A4 RADIOLABELED COMPOUNDS AND COMPOSITIONS, THEIR PRECURSORS AND METHODS FOR THEIR PRODUCTION 审中-公开
标题翻译：放射性标记的化合物和组合物，它们的前体和方法FOR THEIR
公开(公告)号：EP1723161A4
公开(公告)日：2010-04-28
申请号：EP05706491
申请日：2005-02-14
申请人： UNIV BRITISH COLUMBIA
发明人： PERRIN DAVID M , TING RICHARD
IPC分类号： C07H21/04 , A61K51/04 , A61K51/06 , C07B59/00 , C07D475/04 , C07D495/04 , G01T1/161
CPC分类号： A61K51/04 , C07B59/004 , C07B2200/05 , C07D495/04 , C07H21/04

5. 发明授权

EP1282631B1 METHODS OF SYNTHESIS OF RADIOLABELLED PLATINUM CHEMOTHERAPEUTIC AGENTS 有权
标题翻译：用于生产RADIO MARK铂化疗药物
公开(公告)号：EP1282631B1
公开(公告)日：2008-09-03
申请号：EP01913394.1
申请日：2001-03-23
申请人： AUSTRALIAN NUCLEAR SCIENCE AND TECHNOLOGY ORGANISATION
发明人： SMITH, Suzanne, Virginia
IPC分类号： A61K51/00 , C07F15/00 , C07B59/00
CPC分类号： A61K51/02 , C07B59/004 , C07F15/0093

6. 发明公开

EP1195168A3 Ternary radiopharmaceutical complexes 失效
标题翻译：三元复合物的放射性药物
公开(公告)号：EP1195168A3
公开(公告)日：2007-05-30
申请号：EP01123928.2
申请日：1996-04-03
申请人： Bristol-Myers Squibb Pharma Company
发明人： Edwards, David S. , Liu, Shuang
IPC分类号： A61K51/08 , A61M36/14 , C07F5/00 , C07F13/00 , A61K103/10
CPC分类号： C07K14/75 , A61K51/0476 , A61K51/0497 , A61K51/082 , A61K51/088 , A61K2123/00 , C07B59/004 , C07B59/008 , C07K7/56
摘要： This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious diseases and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labelled hydrazine or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention havee the structure: [(Q) d' L n -C h' ] x -M t (A L1 ) y (A L2 ) z wherein the variables are as defined therein.

7. 发明授权

EP0538402B1 METHOD OF PREPARING A RADIOACTIVE RHENIUM COMPLEX SOLUTION 失效
标题翻译：方法用于生产放射性铼的溶液
公开(公告)号：EP0538402B1
公开(公告)日：2006-03-08
申请号：EP91915046.6
申请日：1991-07-02
申请人： MALLINCKRODT INC.
发明人： PANEK-FINDA, Helena
IPC分类号： A61K51/04 , A61K51/12 , C07B59/00
CPC分类号： C07B59/004 , A61K51/0489 , A61K51/12 , A61K2121/00 , A61K2123/00
摘要： The invention relates to a method of preparing a solution of a radioactive rhenium complex, by reacting at elevated temperature a radioactive perrhenate in a substantially aqueous solution with a ligand in the presence of a reductant and optionally an antioxidant under substantially anaerobic conditions, wherein said reaction is carried out at a pH from approx. 1.5 to approx. 5 and by heating the reaction components for at least 10 min. at a temperature of at least 100 DEG C. The invention further relates to a kit for performing said method.

8. 发明授权

EP0630264B1 LIGANDS FOR IMPROVING METAL CHELATE FORMATION KINETICS 失效
标题翻译：提高金属螯合物形成动力学的配位体
公开(公告)号：EP0630264B1
公开(公告)日：2002-11-06
申请号：EP93904905.2
申请日：1993-02-05
申请人： BioSynthema Inc.
发明人： SRINIVASAN, Ananthachari
IPC分类号： A61K49/00 , A61K45/00 , C07F13/00 , C07K5/08 , C07K5/02 , C07D213/64 , C07D405/12 , C07C323/60
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/088 , A61K2121/00 , A61K2123/00 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555
摘要： Amide-thiolate ligands having improved metal chelate formation kinetics are disclosed. The ligands include an amine to facilitate rapid formation of an amine-amide-thiolate intermediate complex, followed by transfer of the metal to or conversion of the ligand to a thermodynamically stable amide-thiolate complex. In one embodiment of the invention, the amine is a tertiary amine, or its equivalent, strategically located to facilitate complex formation. In another embodiment of the invention, the amine is part of pyridine containing a lower alkoxy substituent in the 2 or 4 ring position. O-dealkylation occurs upon complexation causing the amine to become a vinylogous amide as part of 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。配体包括胺以促进胺 - 酰胺 - 硫醇盐中间体配合物的快速形成，接着将金属转移至配体或转化为热力学稳定的酰胺 - 硫醇盐配合物。在本发明的一个实施方案中，胺是叔胺或其等价物，策略性定位以促进复合物的形成。在本发明的另一个实施方案中，胺是在2或4环位置含有低级烷氧基取代基的吡啶的一部分。络合作用发生O-脱烷基化，导致胺成为一种vinylogous酰胺，作为热力学稳定的酰胺 - 硫醇盐配合物的一部分。本发明的酰胺 - 硫醇盐配体可以用于在诊断和治疗领域中使用的生物物质的后标记标记。

9. 发明授权

EP0713513B1 TRIS(ISONITRILE)COPPER(I) SULFATES FOR PREPARING RADIONUCLIDE COMPLEXES 失效
标题翻译： TRIS（异腈）硫酸亚铜用于生产RADIONUKLEIDKOMPLEXEN
公开(公告)号：EP0713513B1
公开(公告)日：2000-10-11
申请号：EP94923912.3
申请日：1994-07-29
申请人： Dupont Pharmaceuticals Company
发明人： EDWARDS, David, Scott
IPC分类号： C07F1/08 , C07F9/00 , A61K51/00 , C07F11/00 , C07F13/00 , C07F15/02 , C07F15/04 , C07F15/06 , C07F17/00
CPC分类号： C07F13/005 , A61K51/0476 , A61K2123/00 , C07B59/004 , C07F1/005

10. 发明公开

EP1019095A1 METHOD FOR THE PREPARATION OF FACIAL METAL TRICARBONYL COMPOUNDS AND THEIR USE IN THE LABELLING OF BIOLOGICALLY ACTIVE SUBSTRATES 失效
标题翻译：用于生产金属面部三羰基化合物及应用进行标记biosubstrates
公开(公告)号：EP1019095A1
公开(公告)日：2000-07-19
申请号：EP98918501.2
申请日：1998-04-21
申请人： Mallinckrodt Inc.
发明人： ALBERTO, Roger , SCHIBLI, Roger , EGLI, André
IPC分类号： A61K51/04 , C01G45/04 , C07F13/00
CPC分类号： A61K51/0476 , A61K51/0478 , C01G45/04 , C01G99/006 , C01P2006/88 , C07B59/004 , C07F13/005
摘要： The invention relates to a method of preparing a compound of the general formula (I): fac-[M(CO)3(OH2)3]+ wherein M is Mn, ?99mTc, 186Re or 188¿Re, by reacting a metal in the permetallate form with carbon monoxide and a reducing agent, characterized in that a mixture of a base, a reducing agent soluble in water but not substantially decomposed by water, and optionally a stabilizing agent is solved in a water containing solvent system containing a solution of the metal in the permanganate, pertechnetate or perrhenate form in the presence of carbon monoxide and optionally in the presence of a halide. The invention further relates to a method of preparing a labeled compound with the aid of the compound of general formula (I), to a method of direct preparation of labeled compounds, to a method of labeling of substrates such as amino acids, peptides, proteins, sugars, small receptor binding molecules and body cells with the aid of compound of general formula (I) and to a kit for the preparation of a labeling composition and a kit for the preparation of a diagnostic of therapeutic pharmaceutical composition.

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