公开(公告)号：EP2196222B1

公开(公告)日：2014-04-23

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

公开(公告)号：EP2708547B1

公开(公告)日：2018-06-20

申请号：EP13185433.3

申请日：2009-03-10

申请人： Universität Zürich

发明人： Alberto, Roger ,  Braband, Henrik

IPC分类号： C07F13/00 ,  A61K51/00

CPC分类号： A61K51/0482 ,  C07F13/005

摘要： A complex having the formula: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ [L 3 MO 3 ] n wherein L 3 represents a tridentate ligand, M represents a metal selected from Tc and Re, and n is a charge from -2 to +1, provided that L 3 is not di-1H-pyrazol-1-ylacetate, bis(3,5-dimethyl-1H-pyrazol-1-yl)acetate, 1,1,1-methanetriyltris(1H-pyrazole), 1,1,1-methanetriyltris(3,5-dimethyl-1H-pyrazole), 1,4,7-triazacyclononane, 1,4,7-trimethyltriazacyclononane, 1,4,7-trithiacyclononane, hydrotris(1-pyrazolyl)borate or [(· 5 -C 5 H 5 )Co{P(OR) 2 (=O)} 3 ] - , where R is methyl or ethyl; or a complex having the formula: [L 3 MO 3 ] n wherein L 3 represents a tridentate ligand bearing one or more functional groups suitable for facilitating the attachment of a targeting moiety, or bearing one or more linker groups capable of bearing such a functional groups, M represents a metal selected from Tc and Re, and n is a charge from -2 to +1, provide that, when L 3 bears one or more linker groups, none of which bears a functional group suitable for the attachment of a targeting moiety, at least one of the linker groups contains at least three carbon atoms, pharmaceutical compositions thereof, and dialato derivatives of [L 3 MO 3 ] n and methods for their synthesis.

公开(公告)号：EP2708547A1

公开(公告)日：2014-03-19

申请号：EP13185433.3

申请日：2009-03-10

申请人： Universität Zürich

发明人： Alberto, Roger ,  Braband, Henrik

IPC分类号： C07F13/00 ,  A61K51/00

CPC分类号： A61K51/0482 ,  C07F13/005

摘要： A complex having the formula:

         [L 3 MO 3 ] n

wherein L 3 represents a tridentate ligand, M represents a metal selected from Tc and Re, and n is a charge from -2 to +1, provided that L 3 is not di-1H-pyrazol-1-ylacetate, bis(3,5-dimethyl-1H-pyrazol-1-yl)acetate, 1,1,1-methanetriyltris(1H-pyrazole), 1,1,1-methanetriyltris(3,5-dimethyl-1H-pyrazole), 1,4,7-triazacyclononane, 1,4,7-trimethyltriazacyclononane, 1,4,7-trithiacyclononane, hydrotris(1-pyrazolyl)borate or [(η 5 -C 5 H 5 )Co{P(OR) 2 (=O)} 3 ] - , where R is methyl or ethyl;
or a complex having the formula:
[L 3 MO 3 ] n
wherein L 3 represents a tridentate ligand bearing one or more functional groups suitable for facilitating the attachment of a targeting moiety, or bearing one or more linker groups capable of bearing such a functional groups, M represents a metal selected from Tc and Re, and n is a charge from -2 to +1, provide that, when L 3 bears one or more linker groups, none of which bears a functional group suitable for the attachment of a targeting moiety, at least one of the linker groups contains at least three carbon atoms,
pharmaceutical compositions thereof, and dialato derivatives of [L 3 MO 3 ] n and methods for their synthesis.

摘要翻译： 具有以下公式的复合物：ƒ€ƒ€ƒ€ƒ€ƒ€ƒ[L 3 MO 3] n其中L 3表示三齿配体，M表示选自Tc和Re的金属，n为 如果L 3不是二-1H-吡唑-1-基乙酸酯，乙酸双（3,5-二甲基-1H-吡唑-1-基）酯，1,1,1-甲基三乙基三 （1H-吡唑），1,1,1-甲基三基三（3,5-二甲基-1H-吡唑），1,4,7-三氮杂环壬烷，1,4,7-三甲基三氮杂环壬烷，1,4,7-三硫代环壬烷，氢化三 （1-吡唑基）硼酸盐或[（5 -C 5 H 5）Co {P（OR）2（= O）} 3] - ，其中R是甲基或乙基; 或具有下式的复合物[L 3 MO 3] n其中L 3表示具有一个或多个适于促进靶向部分连接的官能团的三齿配体，或带有一个或多个能够承载这种功能的连接基团 基团，M表示选自Tc和Re的金属，n是-2至+1的电荷，条件是当L 3具有一个或多个连接基团时，其中没有一个具有适于连接一个或多个连接基团的官能团 靶向部分，至少一个连接基团含有至少三个碳原子，其药物组合物和[L 3 MO 3] n的拨号衍生物及其合成方法。

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。