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1. 发明申请

WO9940947A2 ANGIOGENESIS TARGETING MOLECULES 审中-公开
标题翻译：血管生成指标分子
公开(公告)号：WO9940947A2
公开(公告)日：1999-08-19
申请号：PCT/CA9900101
申请日：1999-02-11
申请人： RESOLUTION PHARM INC , FAUCONNIER THERESA , POLLAK ALFRED , THORNBACK JOHN , ESHIMA DENNIS
发明人： FAUCONNIER THERESA , POLLAK ALFRED , THORNBACK JOHN , ESHIMA DENNIS
IPC分类号： A61K51/08 , A61K51/00
CPC分类号： A61K51/08 , A61K51/088
摘要： The present invention relates to compounds that are effective for targeting sites of angiogenesis for diagnostic and therapeutic purposes. The compounds are of the Formula (I): A-(B)n-C, wherein A is a chelator moiety capable of complexing a radionuclide metal or a moiety capable of binding to a halogen; B is a spacer group; C is an angiogenesis targeting molecule; and n is selected from the integers 0 and 1. The invention also relates to a method of imaging sites of angiogenesis and treating patients through the administration of the compounds of the present invention.
摘要翻译：本发明涉及对于靶向用于诊断和治疗目的的血管生成位点有效的化合物。所述化合物具有式（I）：A-（B）n-C，其中A是能够络合放射性核素金属或能够结合卤素的部分的螯合剂部分; B是间隔基; C是血管生成靶向分子; 并且n选自整数0和1.本发明还涉及通过施用本发明的化合物对血管生成位点进行成像并治疗患者的方法。

2. 发明申请

WO1995017419A1 METAL CHELATORS 审中-公开
标题翻译：金属制造商
公开(公告)号：WO1995017419A1
公开(公告)日：1995-06-29
申请号：PCT/CA1994000718
申请日：1994-12-22
申请人： RESOLUTION PHARMACEUTICALS INC. , POLLAK, Alfred , GOODBODY, Anne
发明人： RESOLUTION PHARMACEUTICALS INC.
IPC分类号： C07K05/097
CPC分类号： C07K5/0821 , A61K51/088
摘要： Radionuclide chelating compounds are provided for coupling to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targeting molecules may be used in diagnosis and therapy.
摘要翻译：提供放射性核素螯合化合物用于与靶分子如蛋白质，肽或抗体偶联。所得标记的靶向分子可用于诊断和治疗。

3. 发明申请

WO1996003427A1 PEPTIDE DERIVED RADIONUCLIDE CHELATORS 审中-公开
标题翻译：肽衍生的放射性核素螯合剂
公开(公告)号：WO1996003427A1
公开(公告)日：1996-02-08
申请号：PCT/CA1995000249
申请日：1995-04-28
申请人： RESOLUTION PHARMACEUTICALS INC. , POLLAK, Alfred , GOODBODY, Anne
发明人： RESOLUTION PHARMACEUTICALS INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/0827 , A61K51/0478 , A61K51/088 , A61K2123/00 , Y02P20/55
摘要： For use in imaging sites of diagnostic interest within the body, the present invention provides radionuclide chelators of formula (I), wherein X is a linear or branched, saturated or unsaturated C1-4alkyl chain that is optionally interrupted by one or two heteroatoms selected from N, O and S; and is optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl, C1-4alkyl, aryl and C(O)Z; Y is H or a substituent defined by X; X and Y may together form a 5- to 8-membered saturated or unsaturated heterocyclic ring optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl, oxo, C1-4alkyl, aryl and C(O)Z; R through R are selected independently from H; carboxyl; C1-4alkyl; C1-4alkyl substituted with a group selected from hydroxyl, amino, sulfhydryl, halogen, carboxyl, C1-4alkoxycarbonyl and aminocarbonyl; an alpha carbon side chain of a D- or L-amino acid other than proline; and C(O)Z; R and R are selected independently from H; carboxyl; amino; C1-4alkyl; C1-4alkyl substituted by hydroxyl, carboxyl or amino; and C(O)Z; R is selected from H and a sulfur protecting group; and Z is selected from hydroxyl, C1-4alkoxy and a targeting molecule.
摘要翻译：本发明提供式（I）的放射性核素螯合剂，其中X是直链或支链的饱和或不饱和C 1-4烷基链，其任选被一个或两个选自以下的杂原子中断： N，O和S; 并且任选被至少一个选自卤素，羟基，氨基，羧基，C 1-4烷基，芳基和C（O）Z的基团取代; Y是H或由X定义的取代基; X和Y可以一起形成任选被至少一个选自卤素，羟基，氨基，羧基，氧代，C 1-4烷基，芳基和C（O）Z中的基团取代的5至8元饱和或不饱和杂环; R 1至R 4独立地选自H; 羧基; C 1-4烷基; 被选自羟基，氨基，巯基，卤素，羧基，C 1-4烷氧基羰基和氨基羰基取代的C 1-4烷基; 除脯氨酸以外的D-或L-氨基酸的α碳侧链; 和C（O）Z; R 5和R 6独立地选自H; 羧基; 氨基; C 1-4烷基; 被羟基，羧基或氨基取代的C 1-4烷基; 和C（O）Z; R 7选自H和硫保护基; Z选自羟基，C 1-4烷氧基和靶向分子。

4. 发明申请

WO1995022996A3 PEPTIDE-CHELATOR CONJUGATES 审中-公开
公开(公告)号：WO1995022996A3
公开(公告)日：1995-08-31
申请号：PCT/CA1995000106
申请日：1995-02-24
申请人： RESOLUTION PHARMACEUTICALS INC. , GOODBODY, Anne , POLLAK, Alfred
发明人： RESOLUTION PHARMACEUTICALS INC.
IPC分类号： A61K51/08

5. 发明申请

WO9522996A2 PEPTIDE-CHELATOR CONJUGATES 审中-公开
标题翻译：肽组合物
公开(公告)号：WO9522996A2
公开(公告)日：1995-08-31
申请号：PCT/CA9500106
申请日：1995-02-24
申请人： RESOLUTION PHARM INC , GOODBODY ANNE , POLLAK ALFRED
发明人： GOODBODY ANNE , POLLAK ALFRED
IPC分类号： A61K51/00 , A61K51/08 , C07K7/02 , C07K7/06
CPC分类号： A61K51/088 , A61K2123/00
摘要： Peptide-chelator conjugates are provided that when labelled with a traceable metal are useful for diagnostic imaging of sites of inflammation. The peptide component is an antagonist of the naturally occurring tetrapeptide tuftsin while the chelator component serves as a labelling site for metals, in particular radionuclide metals such as technetium-99m.
摘要翻译：提供了肽 - 螯合剂缀合物，当用可追踪的金属标记时可用于炎症部位的诊断成像。肽组分是天然存在的四肽簇绒的拮抗剂，而螯合剂组分用作金属的标记位点，特别是诸如锝-99m的放射性核素金属。

6. 发明申请

WO1995013832A1 IMMOBILIZED LABELLING METHOD 审中-公开
标题翻译：固定标签方法
公开(公告)号：WO1995013832A1
公开(公告)日：1995-05-26
申请号：PCT/CA1994000637
申请日：1994-11-16
申请人： RESOLUTION PHARMACEUTICALS INC. , POLLAK, Alfred , DUNN-DUFAULT, Robert
发明人： RESOLUTION PHARMACEUTICALS INC.
IPC分类号： A61K47/48
CPC分类号： A61K51/08 , A61K51/088 , A61K2121/00 , A61K2123/00
摘要： Described is a process for labelling ligands with metals comprising the steps of covalently coupling the ligand to a solid support via a metal-cleavable linker; introducing a complex-forming metal to the support; and collecting the metal-ligand complex released from the support. The metal catalyzes cleavage of the ligand from the support upon complex formation resulting in a solution substantially free of unlabelled ligand.
摘要翻译：描述了用金属标记配体的方法，包括通过金属可切割连接体将配体共价偶联到固体支持物的步骤; 将复合物形成金属引入载体; 并收集从载体释放的金属 - 配体络合物。在络合物形成时，金属催化配体从载体上的裂解，得到基本上不含未标记的配体的溶液。

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