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1. 发明公开

EP2196222A1 Tricarbonyl complexes of rhenium and technetium comprising amino acids as bidentate ligands and their use as radiotherapeutic chemotoxic agents. 有权
标题翻译：的含有氨基酸二齿配体和它们作为化疗毒性放射治疗剂使用铼三羰基复合物。
公开(公告)号：EP2196222A1
公开(公告)日：2010-06-16
申请号：EP10154938.4
申请日：2004-10-20
申请人： Universität Zürich
发明人： Alberto, Roger , Zobi, Fabio
IPC分类号： A61K51/04 , A61K51/08 , A61P35/00
CPC分类号： A61K51/0476 , A61K33/24 , A61K51/0478
摘要： A metal tricarbonyl compound of the general formula

wherein
M is rhenium or technetium or an isotope thereof;
two of X1, X2 and X3 are part of a bidentate ligand and the other one is optionally a monodentate ligand selected from the group consisting of halogens, CO, aromatic heterocycles, thioethers and isocyanides, wherein the aromatic heterocycles are selected from the group consisting of pyridine, pyrimidine, pyrazine, imidazole, pyrazole, triazole, tetrazole, thiazole, and oxazole, wherein the bidentate ligand is an amino acid.
摘要翻译：通式worin M的金属化合物三羰是铼或锝或与其同位素; 2 X1，X2和X3的是二齿配体的一部分，而另一个为任选选自卤素，CO，芳族杂环，硫醚和异氰化物的，worin芳香族杂环的单齿配体选自下组的选择吡啶，嘧啶，吡嗪，咪唑，吡唑，三唑，四唑，噻唑和恶唑，worin双齿配体是氨基酸。

2. 发明公开

EP1846015A4 METHOD, COMPOSITIONS AND CLASSIFICATION FOR TUMOR DIAGNOSTICS AND TREATMENT 审中-公开
标题翻译：方法，组成和分类肿瘤诊断和治疗
公开(公告)号：EP1846015A4
公开(公告)日：2009-08-12
申请号：EP06733745
申请日：2006-01-19
申请人： ZUCKERMAN MATHEW MARK
发明人： ZUCKERMAN MATHEW MARK
IPC分类号： A61K38/00 , A01N37/18 , C07K5/00
CPC分类号： G01N33/57488 , A61K51/0476 , C07K14/475 , C07K14/52 , C07K14/71 , C07K14/715 , G01N2333/475 , G01N2333/485 , G01N2500/00

3. 发明授权

EP1474396B1 N-SUBSTITUTED3-HYDROXY-4-PYRIDINONES AND PHARMACEUTICALS CONTAINING THEREOF 有权
标题翻译： N-取代的3-羟基-4-吡啶酮和含有PHARMACEUTICALS
公开(公告)号：EP1474396B1
公开(公告)日：2007-09-19
申请号：EP03737635.7
申请日：2003-02-05
申请人： Bristol-Myers Squibb Company
发明人： LIU, Shuang
IPC分类号： C07D213/89 , A61K31/4412 , A61K51/04 , A61P31/12
CPC分类号： C07D213/89 , A61K51/0476 , C07B2200/05 , C07D401/12 , C07D409/12
摘要： N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.

4. 发明授权

EP1283729B1 TC AND RE CARBONYL COMPLEXES PREPARED FROM PERTECHNETATES AND PERRHENATES 有权
标题翻译： TC和RE羰基配合物从PERTECHNETATES和PERRHENATES制备
公开(公告)号：EP1283729B1
公开(公告)日：2006-08-30
申请号：EP01944139.3
申请日：2001-05-08
申请人： MALLINCKRODT INC.
发明人： PIPES, David, W. , DYSZLEWSKI, Mary, E. , WEBB, Elizabeth, G.
IPC分类号： A61K51/04 , C07F13/00
CPC分类号： A61K51/0476 , A61K49/101 , A61K51/0474 , C07F13/005 , Y10S530/811
摘要： The invention relates to novel aminocarboxylate ligands that are suitable for complexing with a radionuclide, and are useful as therapeutic agents and as imaging agents for diagnostic purposes. In accordance with the present invention, a method of preparing a compound of formula fac-[M(CO)3(OH2)3]+ (I) wherein M is Mn, ?99mTc, 186Re or 188¿Re, involves reacting a metal in permetallate form with carbon monoxide and stannous ion. The compound of formula (I) can be reacted with a ligand L¿x?, to form a compound of the formula fac-[M(CO)3Lx]?n¿ (II) wherein M is as defined above, L¿x? is a monodentate or multidentate ligand or a mixture of these ligands, and n is a charge of the ligand Lx increased with one + charge. The invention also is directed to novel compounds, and kits for carrying out the disclosed methods.
摘要翻译：本发明涉及适用于与放射性核素络合的新型氨基羧酸盐配体，并且可用作诊断目的的治疗剂和成像剂。根据本发明，制备其中M为Mn，≥99mTc，186Re或188Re的式fac- [M（CO）3（OH 2）3] +（I）的化合物的方法包括使金属与一氧化碳和亚锡离子形成过金属化物形式。式（I）化合物可以与配体L 1 x反应形成式fac- [M（CO）3 L x] n（II）的化合物，其中M如上所定义，L x ？是单齿或多齿配体或这些配体的混合物，并且n是用一个+电荷增加的配体Lx的电荷。本发明还涉及用于实施所公开的方法的新化合物和试剂盒。

5. 发明授权

EP1192166B1 GROUP(VII) TRANSITION-METAL COMPLEXES WITH MULTIDENTATE AMINOPOLYCARBOXYLATE LIGANDS AND A KIT FOR PRODUCING THEM 有权
标题翻译：与多齿氨基多羧酸盐LIGAND VII侧组过渡金属络合物和用于生产KIT
公开(公告)号：EP1192166B1
公开(公告)日：2004-09-29
申请号：EP00952136.0
申请日：2000-06-28
申请人： MALLINCKRODT INC.
发明人： DYSZLEWSKI, Mary, M. , ALBERTO, Roger , BUGAJ, Joseph, E.
IPC分类号： C07F13/00 , A61K51/04
CPC分类号： A61K51/0476 , A61K51/0478 , C07F13/005

6. 发明公开

EP1283729A2 TC AND RE CARBONYL COMPLEXES FOR PERTECHNETATE AND PERRHENATE 有权
标题翻译： TC和RE碳酰胺复合物用于PERTECHNETATE和PERRHENATE
公开(公告)号：EP1283729A2
公开(公告)日：2003-02-19
申请号：EP01944139.3
申请日：2001-05-08
申请人： MALLINCKRODT INC.
发明人： PIPES, David, W. , DYSZLEWSKI, Mary, E. , WEBB, Elizabeth, G.
IPC分类号： A61K51/04 , C07F13/00
CPC分类号： A61K51/0476 , A61K49/101 , A61K51/0474 , C07F13/005 , Y10S530/811
摘要： The invention relates to novel aminocarboxylate ligands that are suitable for complexing with a radionuclide, and are useful as therapeutic agents and as imaging agents for diagnostic purposes. In accordance with the present invention, a method of preparing a compound of formula fac-[M(CO)3(OH2)3]+ (I) wherein M is Mn, ?99mTc, 186Re or 188¿Re, involves reacting a metal in permetallate form with carbon monoxide and stannous ion. The compound of formula (I) can be reacted with a ligand L¿x?, to form a compound of the formula fac-[M(CO)3Lx]?n¿ (II) wherein M is as defined above, L¿x? is a monodentate or multidentate ligand or a mixture of these ligands, and n is a charge of the ligand Lx increased with one + charge. The invention also is directed to novel compounds, and kits for carrying out the disclosed methods.
摘要翻译：本发明涉及适用于与放射性核素络合的新型氨基羧酸盐配体，并且可用作诊断目的的治疗剂和成像剂。根据本发明，制备其中M为Mn，≥99mTc，186Re或188Re的式fac- [M（CO）3（OH 2）3] +（I）的化合物的方法包括使金属与一氧化碳和亚锡离子形成过金属化物形式。式（I）化合物可以与配体L 1 x反应形成式fac- [M（CO）3 L x] n（II）的化合物，其中M如上所定义，L x ？是单齿或多齿配体或这些配体的混合物，并且n是用一个+电荷增加的配体Lx的电荷。本发明还涉及用于实施所公开的方法的新化合物和试剂盒。

7. 发明授权

EP1019095B1 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：EP1019095B1
公开(公告)日：2002-01-16
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

8. 发明公开

EP0949265A1 RADIOACTIVE TRANSITION METAL NITRIDE HETERO-COMPLEX 失效
标题翻译： NITRID-HETEROKOMPLEXE VON RADIOAKTIVENÜBERGANGSMETALLEN
公开(公告)号：EP0949265A1
公开(公告)日：1999-10-13
申请号：EP97947953.2
申请日：1997-12-16
申请人： Nihon Medi-Physics Co., Ltd.
发明人： DUATTI, Adriano , BOLZATI, Cristina , UCCELLI, Licia , REFOSCO, Fiorenzo , TISATO, Francesco
IPC分类号： C07F9/50 , C07F9/70 , C07F9/72 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0476 , A61K51/0478 , C07F9/5004
摘要： The present invention provides a single radioactive transition metal nitride heterocomplex which permits labeling of a physiologically active substance such as a peptide, hormone or the like without impairing the activity of the substance. The radioactive transition metal nitride heterocomplex of the present invention is represented by the following formula (I):

(M≡N)XY (I)

wherein a radioactive transition metal M is radioactive technetium or radioactive rhenium, N is a nitrogen atom, X is a diphosphine compound or a diarsine compound, and Y is a bindentate ligand having a combination of electron-donating atoms.
摘要翻译：本发明提供了一种单一的放射性过渡金属氮化物异复合体，它允许生物活性物质例如肽，激素等标记，而不损害物质的活性。本发明的放射性过渡金属氮化物异质复合体由下式（I）表示：（M标识N）XY，其中放射性过渡金属M为放射性锝或放射性铼，N为氮原子，X为二膦化合物或赤霞珠化合物，Y是具有给电子原子的组合的结合配体。

9. 发明公开

EP0537242A1 PROCEDE DE PREPARATION DE COMPLEXES NITRURO DE METAUX DE TRANSITION 失效
标题翻译：制备过渡金属硝基配合物的方法
公开(公告)号：EP0537242A1
公开(公告)日：1993-04-21
申请号：EP91912410.0
申请日：1991-07-03
申请人： CIS BIO INTERNATIONAL
发明人： PASQUALINI, Roberto , COMAZZI, Véronique , BELLANDE, Emmanuel
IPC分类号： A61K51 , C01B21 , C01G47 , C01G99 , C07B59 , C07F9 , C07F11 , C07F13 , C07F15
CPC分类号： C07F13/005 , A61K51/0476 , A61K51/12 , A61K2123/00 , C07B59/004
摘要： L'invention concerne un procédé de préparation de complexes nitruro de métaux de transition utilisables comme produits radiopharmaceutiques ou pour la synthèse de nouveaux produits pharmaceutiques. Ce procédé consiste à faire réagir un composé oxygéné d'un métal de transition tel que 99mTc, 186Re ou 188Re, avec un premier ligand azoté tel que l'azoture de sodium ou un composé azoté comme le S-méthyl, N-méthyl dithiocarbazate, et un agent réducteur constitué soit par de l'étain (II) soit par un dithionite. Le produit ainsi obtenu peut être utilisé pour la préparation de produits radiopharmaceutiques par réaction avec un deuxième ligand tel que le dithiocarbamate de sodium.
摘要翻译：本发明涉及制备用作放射性药物或用于合成新药物产品的过渡金属氮化物配合物的方法。这个过程包括过渡金属如99m Tc和186Re或188铼的含氧化合物如叠氮化钠或氮化合物如S - 甲基，N-甲基dithiocarbazate反应，与第一氮配体，和由锡（II）或连二亚硫酸盐组成的还原剂。由此获得的产物可用于通过与第二配体如二硫代氨基甲酸钠反应制备放射性药物。

10. 发明授权

EP0403524B1 PREPARATION DE COMPLEXES NITRURO UTILISABLES COMME PRODUITS RADIOPHARMACEUTIQUES 失效
标题翻译：可用作无线电制药产品的硝基化合物的制备
公开(公告)号：EP0403524B1
公开(公告)日：1993-02-10
申请号：EP89903166.0
申请日：1989-03-08
申请人： CIS BIO INTERNATIONAL
发明人： PASQUALINI, Roberto , MAGON, Luciano , BARDY, André , DUATTI, Adriano , MARCHI, Andrea
IPC分类号： C07F13/00 , C07B59/00 , A61K43/00 , A61K49/00
CPC分类号： G01N33/6887 , A61K51/0476 , A61K51/10 , A61K51/1093 , A61K2121/00 , A61K2123/00 , C07F5/003 , C07F13/005 , G01N33/574 , G01N33/57423 , G01N33/60
摘要： Preparation of 99m technetium or 186 rhenium or 188 rhenium compounds usable as radiopharmaceutical products. To obtain said preparation an oxygenated compound of 99mTc, 186Re or 188Re, for example an ammonium or alcaline metal pertechnetate or perrhenate, is made to react with a first ligand chosen from the group of aliphatic and aromatic phosphines and polyphosphines, either substituted or not, and a second nitrogen-containing ligand composed of an ammonium or metal nitride pharmaceutically acceptable or a nitrogen-containing compound comprising a unit (alpha) such as hydrazine, a derivative of hydrazine, dithiocarbazic acid and the derivatives of dithiocarbazic acid. The product obtained can be used as such as a radiopharmaceutical product or be used as an intermediary for preparing other radiopharmaceutical products by exchange reaction with a third ligand, a monoclonal antibody or an antibody fragment.

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