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1. 发明申请

WO1993015770A1 RADIOLABELLED PEPTIDE COMPOUNDS 审中-公开
标题翻译：放射性肽化合物
公开(公告)号：WO1993015770A1
公开(公告)日：1993-08-19
申请号：PCT/US1993000939
申请日：1993-02-04
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , LYLE, Leon , RAJAGOPALAN, Raghavan , DEUTSCH, Karen , DUNN, Thomas, Jeffrey , SRINIVASAN, Ananthachari , VANDERHEYDEN, J., L.
IPC分类号： A61K49/02
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/083 , A61K51/088 , A61K2121/00 , A61K2123/00 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555
摘要： The present invention relates to novel ligands and labelling techniques. The present invention further relates to a diagnostic composition suitable for administration to a warm-blooded animal comprising somatostatin or hirudin or a molecule capable of interacting with the somatostatin receptor or with the hirudin receptor labeled with a radionuclide by means of a chelate ligand capable of administration to an animal to produce reliable visual imaging of tumors or therapeutic effects on tumors and blood clots.
摘要翻译：本发明涉及新的配体和标记技术。本发明还涉及一种适于给予温血动物的诊断组合物，其包含生长抑素或水蛭素或能够与生长抑素受体相互作用的分子，或与通过能够施用的螯合配体的放射性核素标记的水蛭素受体给动物产生肿瘤的可靠视觉成像或对肿瘤和血块的治疗作用。

2. 发明申请

WO1996040286A1 PROCESS FOR PRODUCING IOVERSOL 审中-公开
标题翻译：生产IOVERSOL的方法
公开(公告)号：WO1996040286A1
公开(公告)日：1996-12-19
申请号：PCT/US1996010097
申请日：1996-06-06
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , DUNN, Thomas, Jeffrey , WHITE, David, H. , KNELLER, Mills, Thomas , JONES, Michelle, M. , DORAN, Narciso, Ocampo, III
IPC分类号： A61K49/00
CPC分类号： C07C231/12 , C07C237/46
摘要： The present invention discloses a new process for producing ioversol (marketed as OPTIRAY3) comprising: (a) reacting 5-amino-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide with chloroacetyl chloride in a polar aprotic solvent, or combinations thereof, to produce N,N'-bis[2,3-di(2-chloroacetoxy)propyl]-5-(2-chloroacetamido)-2,4,6-triiodoisophthalamide; (b) reacting the product of (a) with sodium hydroxide to produce N,N'-bis(2,3-dihydroxypropyl)-5-(2-chloroacetamido)-2,4,6-triiodoisophthalamide; (c) reacting the product of (b) in water and sodium acetate to produce N,N'-bis(2,3-dihydroxypropyl)-5-glycolamido-2,4,6-triiodoisophthalamide; and (d) reacting the product of (c) with an alkylating agent capable of producing hydroxylhylated product in the presence of a base and water to produce ioversol.
摘要翻译：本发明公开了一种新的制备碘奥昔芬（市售为OPTIRAY3）的方法，包括：（a）使5-氨基-N，N'-双（2,3-二羟丙基）-2,4,6-三碘间苯二酰胺与氯乙酰氯反应极性非质子溶剂或其组合，以产生N，N'-双[2,3-二（2-氯乙酰氧基）丙基] -5-（2-氯乙酰胺基）-2,4,6-三碘间苯二酰胺; （b）使（a）的产物与氢氧化钠反应以产生N，N'-双（2,3-二羟丙基）-5-（2-氯乙酰胺基）-2,4,6-三碘间苯二酰胺; （c）使（b）的产物在水和乙酸钠中反应，得到N，N'-双（2,3-二羟丙基）-5-乙醇酰氨基-2,4,6-三碘间苯二酰胺; 和（d）使（c）的产物与能够在碱和水的存在下产生羟基化产物的烷基化剂反应以制备碘奥昔莫。

3. 发明申请

WO1993010887A1 PURIFICATION OF CRUDE IOVERSOL USING REVERSE OSMOSIS 审中-公开
标题翻译：使用反向OSMOSIS对原发性肝硬化的清除
公开(公告)号：WO1993010887A1
公开(公告)日：1993-06-10
申请号：PCT/US1992006401
申请日：1992-07-31
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , BOSWORTH, Mark, E. , DUNN, Thomas, Jeffrey , HALL, Warren, Earl , JOHNSON, Richard, Gardner , KNELLER, Mills, Thomas , LIN, Youlin , WALLACE, Rebecca, Abernathy , WHITE, David, Hill , WONG, David, M.
IPC分类号： B01D61/00
CPC分类号： B01D61/025 , A61K49/0433 , C07C231/24 , C07C237/46
摘要： A process of using reverse osmosis membrane as an alternative or substitute method for the purification of a crude diagnostic agent. Crude ioversol can be purified by drawing ioversol in a process tank (12), and pumping it into a housing cartridge (16) containing a reverse osmosis membrane (18), which allows the passage of aqueous solution of low molecular weight impurities, and retain larger molecular weight molecules of ioversol which are returned to the process tank (12).

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