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1. 发明授权

EP0670736B1 LABELLED INTERLEUKIN-8 AND MEDICAL USES THEREOF 失效
标题翻译：标记的白细胞介素-8及其医学应用
公开(公告)号：EP0670736B1
公开(公告)日：2001-09-19
申请号：EP93923789.7
申请日：1993-10-04
申请人： MALLINCKRODT MEDICAL, INC. , The Regents of The University of Michigan Technology Management Wolverine Tower Office
发明人： LYLE, Leon, R. , KUNKEL, Steven, L.
IPC分类号： A61K51/08
CPC分类号： A61K51/08 , A61K2123/00
摘要： A method of imaging a target site in an animal's body in which a labelled CXC chemokine is introduced into the animal's body and allowed to accumulate at a target site which includes Interleukin-8 receptor molecules. The accumulated, labelled CXC chemokine is then detected so as to image the target site of the body.

2. 发明公开

EP0948361A4 MAGNETIC RESONANCE BLOOD POOL AGENTS 失效
标题翻译：自旋共振造影剂BLOOD
公开(公告)号：EP0948361A4
公开(公告)日：2001-02-07
申请号：EP97949385
申请日：1997-11-12
申请人： MALLINCKRODT MEDICAL INC
发明人： WOULFE STEVEN R
IPC分类号： A61K49/00 , A61K49/06 , G01N31/00 , G01N33/48
CPC分类号： A61K49/06
摘要： The present invention provides compositions comprising contrast agents capable of binding non-covalently to blood proteins. The compositions of the invention provide increased residence time of contrast agents in the vasculature, thus providing effective blood pool contrast agents. The invention also provides methods for imaging a patient comprising administering a composition of the invention to a patient and obtaining an image.

3. 发明公开

EP0886634A4 PROCESS FOR PRODUCING IOVERSOL 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON IOVERSOL
公开(公告)号：EP0886634A4
公开(公告)日：2000-08-02
申请号：EP97903077
申请日：1997-01-27
申请人： MALLINCKRODT MEDICAL INC
发明人： DUNN THOMAS JEFFREY , WHITE DAVID H , KNELLER MILLS THOMAS , JONES MICHELLE M , DORAN NARCISCO OCAMPO III , BAILEY ALLAN R
IPC分类号： C07C237/46 , C07C233/05 , A61K31/165 , A61K49/00 , C07C231/12 , C07C233/65
CPC分类号： 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-triiodoisopthalamide 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-triiodoisopthalamide; (b) reacting the product of (a) with a base to produce N,N'-bis(2,3-dihydroxypropyl)-5-(2-chloroacetamido)-2,4,6-triiodoisopthalamide; (c) reacting the product of (b) with an alkylating agent capable of producing a hydroxyethylated product in the presence of a base and water to produce N,N'-bis(2,3-dihydroxypropyl)-5-[N-(2-hydroxyethyl) (2-chloroacetamido)]-2,4,6-triiodoisopthalamide; and (d) reacting the product of (c) in water and acetate ions to produce ioversol.
摘要翻译：（a）使5-氨基-N，N'-双（2,3-二羟基丙基）-2,4,6-三碘代异戊酰胺与氯乙酰氯反应生成碘代醇（以OPTIRAY3市售）产生N，N'-双[2,3-二（2-氯乙酰氧基）丙基] -5-（2-氯乙酰氨基）-2,4,6-三碘异烟酰胺; （b）使（a）的产物与碱反应以制备N，N'-双（2,3-二羟丙基）-5-（2-氯乙酰氨基）-2,4,6-三碘异烟酰胺; （c）使（b）的产物与能够在碱和水存在下生成羟乙基化产物的烷基化剂反应，生成N，N'-双（2,3-二羟基丙基）-5- [N-（（2-氯乙酰胺基）] - 2,4,6-三碘异烟酰胺; 和（d）使（c）的产物在水和乙酸根离子中反应以产生碘佛醇。

4. 发明公开

EP0828978A4 AGRESSIVE CONVECTIVE DRYING IN A NUTSCHE TYPE FILTER/DRYER 失效
标题翻译：侵略性对流的吸入过滤器/干燥器
公开(公告)号：EP0828978A4
公开(公告)日：2000-06-28
申请号：EP96920190
申请日：1996-05-14
申请人： MALLINCKRODT MEDICAL INC
发明人： HALEEN LEN W
IPC分类号： B01D29/075 , F26B5/04 , F26B11/14 , F26B21/00 , F26B21/14 , F26B11/00
CPC分类号： F26B11/14 , F26B5/04 , F26B21/14

5. 发明公开

EP0828979A4 AGGRESSIVE CONVECTIVE DRYING IN A CONICAL SCREW TYPE MIXER/DRYER 失效
标题翻译： AGGRESSIVE对流在锥形混合器/干燥器中的SCREW原理AFTER
公开(公告)号：EP0828979A4
公开(公告)日：2000-06-14
申请号：EP96923192
申请日：1996-05-14
申请人： MALLINCKRODT MEDICAL INC
发明人： HALEEN LEN W
IPC分类号： F26B11/14 , F26B3/092 , F26B5/04 , F26B11/12 , F26B21/00 , F26B11/00
CPC分类号： F26B11/12 , F26B3/092 , F26B5/04
摘要： The present invention relates to improved drying techniques which increase the capacity and efficiency of agitated pan type dryers. In particular, the present invention relates to a conical screw type mixer/dryer apparatus (210) and method for aggressive convective drying of hard to dry chemical compounds, such as pharmaceuticals. The aggressive drying is brought about by creating turbulence (280) within the drying vessel (210) during the drying cycle. Significant reductions in drying cycle times have been achieved.

6. 发明公开

EP0776334A4 STABLE ANALOGS OF BIOACTIVE PEPTIDES CONTAINING DISULFIDE LINKAGES 失效
标题翻译： STABILE ANALOGE BIOAKTIVER PEPTIDE WELCHE DISULFIDBINDUNGEN BEINHALTEN
公开(公告)号：EP0776334A4
公开(公告)日：2000-05-03
申请号：EP95926734
申请日：1995-07-18
申请人： MALLINCKRODT MEDICAL INC
发明人： SRINIVASAN ANANTHACHARI , LYLE LEON R , RAJAGOPALAN RAGHAVAN
IPC分类号： A61K38/00 , A61K45/00 , A61K51/00 , C07K1/00 , C07K7/06 , C07K7/16 , C07K14/52 , C07K14/655 , C07K14/70 , C09K3/00
CPC分类号： C07K14/655 , C07K1/006 , C07K7/16 , C07K14/52 , C07K14/6555 , C07K14/70 , Y10S930/28
摘要： Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c) thioketal expansion, or (d) alkylation expansion. In sulfide contraction the disulfide bond (-S-S-) is replaced with a monosulfide bond (-S-) in which a bifunctional effector molecule, such as a ligand or chemotoxic agent, is bound to the new peptide linkage. In isosteric substitution, one sulfur atom is replaced with a carbon atom and at least one of the carbon atoms at the modified side is a bifuctional effector molecule. In thioketal expansion, an alkylidene unit (-CR1R2-) is inserted between the two sulfur atoms. In alkylation expansion, an alkyl moiety of from C2 to C3, is inserted between the two sulfur atoms.
摘要翻译：公开了含有二硫键的环肽的稳定类似物。二硫键通过四种方法之一进行修饰：（a）硫化物收缩，（b）等排取代，（c）硫代缩酮扩展或（d）烷基化扩展。在硫化物收缩中，二硫键（-S-S-）用单硫键（-S-）代替，其中双功能效应子分子如配体或化学毒性剂与新的肽键结合。在等排取代中，一个硫原子被碳原子取代，并且在修饰位点处的至少一个碳原子是双功能效应子分子。在缩酮缩醛中，在两个硫原子之间插入亚烷基单元（-CR1R2-）。在烷基化膨胀中，C2至C3的烷基部分插入在两个硫原子之间。

7. 发明授权

EP0584256B1 COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR DETECTING AND LOCALIZING TISSUES HAVING NEUROKININE 1 RECEPTORS 失效
标题翻译：化合物和药物组合检测及组织与神经激肽-1受体ISOLATION
公开(公告)号：EP0584256B1
公开(公告)日：1999-11-10
申请号：EP92912903.9
申请日：1992-04-22
申请人： MALLINCKRODT MEDICAL, INC.
发明人： VISSER, Theofilus, J. Octrooibureau Zoan B.V. , LAMBERTS, Steven, W., J. Octrooibureau Zoan B.V. , KRENNING, Eric, P. Octrooibureau Zoan B.V. , BAKKER, Willem, H. Octrooibureau Zoan B.V. , VAN HAGEN, Petrus, M. Octrooibureau Zoan B.V.
IPC分类号： C07K7/08 , A61K51/00 , G01N33/68
CPC分类号： C07K7/22 , A61K38/00 , A61K51/08 , A61K51/088 , A61K2123/00

8. 发明公开

EP0910416A2 RADIOPHARMACEUTICAL COMPOSITIONS CAPABLE OF LOCALIZING AT SITES OF THROMBUS 失效
标题翻译： RADIO注明化合物血栓IMAGING
公开(公告)号：EP0910416A2
公开(公告)日：1999-04-28
申请号：EP97931012.0
申请日：1997-06-05
申请人： G.D. SEARLE & CO. , MALLINCKRODT MEDICAL, INC.
发明人： FEIGEN, Larry, P. , FLYNN, Daniel, Lee , NEEDLEMAN, Philip , SRINIVASAN, Ananthachari , ZABLOCKI, Jeffery, Alan , SCHMIDT, Michelle A.
IPC分类号： A61K38 , A61K51 , C07K5
CPC分类号： C07K5/06113 , A61K51/088 , A61K2121/00 , A61K2123/00
摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.

9. 发明公开

EP0850072A4 A METHOD FOR PREPARING RADIOLABELED PEPTIDES 失效
标题翻译：用于生产放射性标记肽
公开(公告)号：EP0850072A4
公开(公告)日：1999-01-20
申请号：EP96919257
申请日：1996-06-07
申请人： MALLINCKRODT MEDICAL INC
发明人： SRINIVASAN ANANTHACHARI
IPC分类号： A61K51/08 , C07C227/18 , C07C229/16 , C07C229/24 , A61K51/00 , A61M36/14
CPC分类号： A61K51/088 , A61K51/083 , C07C227/18 , Y02P20/55 , C07C229/16 , C07C229/24
摘要： A method for radiolabelling peptides using polyaminocarboxylate ligands having suitable protecting groups such that they can be added to peptides by standard solid phase or solution phase peptide synthetic chemistry and can be deprotected using standard cleavage/deprotection reagents and produce the peptide/chelate conjugate as a high purity monoaddition product is provided. The cleaved and deprotected ligand-peptide molecules can then be labeled with lanthanide or actinide radionuclides. The protected polyaminocarboxylate ligands form mono-anhydrides or mono-active esters under solid phase or solution phase conditions and permit only the desired monoaddition chelate-peptide conjugate to be formed.

10. 发明公开

EP0888129A1 MAGNETIC RESONANCE BLOOD POOL AGENTS BOUND TO HUMAN SERUM ALBUMIN 失效
标题翻译：磁共振血池药剂结合人血清白蛋白
公开(公告)号：EP0888129A1
公开(公告)日：1999-01-07
申请号：EP97906624.0
申请日：1997-02-18
申请人： MALLINCKRODT MEDICAL, INC.
发明人： COOPER, Stephen R. , MOORE, Dennis A. , HYNES, Michael R. , WALLACE, Rebecca Abernathy
IPC分类号： A61K49 , G01N33
CPC分类号： A61K49/122 , A61K49/085 , A61K49/143 , G01N33/68
摘要： The present invention provides compositions comprising a contrast agent capable of reversibly binding to thiol groups of blood-borne proteins. The compositions of the invention provide increased residence time of the contrast agent in the vasculature, thus providing effective blood pool contrast agents. The invention also provides methods for imaging a patient comprising administering a composition of the invention and obtaining an image.
摘要翻译：本发明提供了包含能够可逆结合血媒蛋白质的巯基的造影剂的组合物。本发明的组合物提供造影剂在脉管系统中的增加的停留时间，从而提供有效的血液池造影剂。本发明还提供了对患者进行成像的方法，其包括施用本发明的组合物并获得图像。

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