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1. 发明公开

EP0637252A1 NHR CONTRAST AGENTS 失效
标题翻译： NHR造影剂
公开(公告)号：EP0637252A1
公开(公告)日：1995-02-08
申请号：EP93911859.0
申请日：1993-04-22
申请人： COCKBAIN, Julian Roderick Michaelson , NYCOMED IMAGING AS
发明人： KLAVENESS, Jo , BERG, Arne
IPC分类号： A61K49
CPC分类号： A61K49/06
摘要： The invention provides parenterally administrable, liver-specific MR imaging contrast media comprising Mn(II) chelates of N,N'-EDTA bisamides.
摘要翻译：本发明提供了包含N，N'-EDTA双酰胺的Mn（II）螯合物的肠胃外可施用的肝特异性MR成像造影剂。

2. 发明公开

EP0511275A1 CHELATING COMPOUNDS 失效
标题翻译：复合。
公开(公告)号：EP0511275A1
公开(公告)日：1992-11-04
申请号：EP91902985.0
申请日：1991-01-18
申请人： COCKBAIN, Julian Roderick Michaelson , NYCOMED AS
发明人： KLAVENESS, Jo , RONGVED, Pal , BERG, Arne
IPC分类号： A61K31 , A61K49 , A61K51 , A61P39 , C07D257 , C07D471 , C07D487 , C07D498
CPC分类号： C07D471/08 , A61K49/06
摘要： L'invention se rapporte à de nouveaux agents de chélation macrocycliques condensés, représentés par la formule [X(CR2R3)n]m où chaque X représente séparément un atome d'oxygène ou de soufre ou un groupe de formule NH, N(CR2R3)pR4, N(CR2R3)pY, ou N(CR2R3)nN((CR2R3)pY)2; chaque Y représente séparément un groupe COZ, SO2Z, POZ2, CON(OH)R2, CH2SR2, CS2R2 ou CSZ; chaque Z représente séparément un groupe OR2 ou NR2R2; n est égal à un nombre entier compris entre 1 et 4; m est égal à un nombre entier compris entre 3 et 8; p est égal à un nombre entier compris entre 1 et 3; chaque R2 représente séparément un atome d'hydrogène ou un groupe alkyle C1-8 éventuellement mono-substitué ou poly-substitué par des groupes hydroxyle ou alkoxy C1-8 et au moins une paire de groupes R2, pour lesquels l'un des éléments de chaque paire provient d'une fraction (CR2R3)n et l'autre d'une fraction (CR2R3)n ou (CR2R3)p, représente, conjointement avec les atomes intervenant, une chaîne fermée fusionnée et saturée à 5-8 éléments, contenant éventuellement un ou plusieurs hétéro-atomes à chaîne fermée choisis parmi l'azote, l'oxygène et le soufre, cette chaîne fusionnée étant éventuellement substituée par un groupe R1; chaque R1 représente séparément un groupe R4 ou un groupe (CR2R3)pY fixé à l'azote; chaque R3 représente séparément un atome d'hydrogène ou un groupe alkyle C1-8 ou alkoxy C1-8, éventuellement mono-substitué ou poly-substitué par des groupes hydroxy ou alkoxy C1-8; et chaque R4 représente séparément un atome d'hydrogène, un atome d'halogène ou un groupe hydroxyle ou un groupe alkyle C1-8 éventuellement mono-hydroxylé ou poly-hydroxylé, alkoxy C1-8, (alkoxy C1-8)- alkyle C1-8 ou poly- (alkoxy C1-8)- alkyle C1-8, un groupe sulfonate ou un groupe (CR2R3)pY; à condition qu'au moins deux groupes Y soient présents. Ces agents de chélation sont utiles dans la préparation d'agents diagnostiques et thérapeutiques, tels que notamment des complexes de chélate utilisables comme agents de contraste dans les techniques de formation d'images

3. 发明公开

EP0453507A1 CHELATING AGENT DERIVATIVES 失效
标题翻译：螯合剂的衍生物。
公开(公告)号：EP0453507A1
公开(公告)日：1991-10-30
申请号：EP90902777.0
申请日：1990-01-15
申请人： COCKBAIN, Julian Roderick Michaelson , NYCOMED AS
发明人： ALM N, Torsten , BERG, Arne , KLAVENESS, Jo , RONGVED, P l
IPC分类号： C07D295 , A61K31 , A61K51 , A61P39 , C07C259 , C07C309 , C07D211 , C07F9 , C09K3
CPC分类号： C07C309/14 , C07C259/06 , C07F9/3808
摘要： Sont décrits des agents chélateurs particulièrement utiles pour al préparation d'agents diagnostiques et thérapeutiques destinés à l'imagerie par résonance magnétique, la scintigraphie, l'imagerie ultrasonore, la radiothérapie et la détoxication des métaux lourds, lesdits agents étant des composés de formule (I): X-CHR1-NZ-(CHR1)nA-(CHR1)m-NZ-CHR1-X (dans laquelle chacun des groupes Z est un groupe -CHR1X ou bien les groupes Z ensemble sont un groupe -(CHR1)q-A'-(CHR1)r-, où A' est un atome d'oxygène ou de soufre ou un groupe NY; m, n, q et r valent chacun 2, 3 ou 4, de préférence 2; et les groupes A, X, Y et R1 ont la notation ci-définie.

4. 发明公开

EP0755385A1 CHELANT COMPOUNDS 失效
标题翻译：螯合物
公开(公告)号：EP0755385A1
公开(公告)日：1997-01-29
申请号：EP95915244.0
申请日：1995-04-12
申请人： NYCOMED IMAGING AS
发明人： VARADARAJAN, John , WATSON, Alan, David , BERG, Arne
IPC分类号： A61K31 , A61K49 , C07C217 , C07C237 , C07C323 , C07D255 , C07D257 , C07D259 , C07D273 , C07F5
CPC分类号： A61K49/06 , C07C237/08 , C07D255/02 , C07D257/02 , C07D259/00 , C07D273/00
摘要： The invention provides amphiphilic compounds of the formula (I) Ch-(-L-Ar-(-AH)n)m (where Ch is a hydrophilic chelant moiety or a salt or a chelate thereof); each L is an optionally oxo substituted C2-25-alkylene linker wherein at least one CH2 moiety is replaced by a group X1 (e.g. L may include a chain sequence, an X1(CH2CH2X1)u (where u is a positive integer) such as X1CH2CH2X1, CH2X1CH2CH2X1CH2CH2X1, CH2X1CH2CH2X1CH2CH2X1CH2CH2X1, etc.), and wherein L is optionally interrupted by a metabolizable group M but with the provisos that the terminus of L adjacent Ch is CH¿2? and that the terminus of L adjacent Ar is X?1¿ or a CH¿2? group adjacent or separated by one CH2 from a group X?1¿ (thus, for example the L-Ar linkage may be L?1-X1-Ar, L1-CH¿2-Ar, L1-X1CH2-Ar or L1-X1CH2CH2-Ar, where L1 is the residue of L; each Ar is an aryl ring optionally substituted by or having fused thereto a further aryl ring; each AH is a protic acid group, preferably an oxyacid, e.g. a carbon, sulphur or phosphorus oxyacid or a salt thereof; each X1 is O, S, NR?1 or PR1¿, preferably no more than 3 X1 groups being present in L; each R1 is hydrogen, alkyl or aryl; and m and n are positive integers, m being for example 1 to 4, especially 1 or 2 and n being for example 1, 2 or 3) which are especially suited for use in diagnostic imaging of the hepatobiliary system.

5. 发明授权

EP0752889B1 LIPOSOMES CONTAINING A X-RAY- OR ULTRASOUND CONTRAST AGENT 失效
标题翻译：脂质体含有X射线和超声造影剂
公开(公告)号：EP0752889B1
公开(公告)日：2002-06-26
申请号：EP95913223.4
申请日：1995-03-27
申请人： Nycomed Imaging AS , DAIICHI PHARMACEUTICAL CO., LTD.
发明人： KLAVENESS, Jo , BERG, Arne , JACOBSEN, Trond Vegard , RONGVED, Pal , EGE, Thorfinn , KIKUCHI, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , YACHI, Kiyoto, Daiichi Pharmaceutical Co., Ltd.
IPC分类号： A61K49/00 , A61K49/04
CPC分类号： A61K49/227 , A61K49/0466 , A61K49/1812
摘要： The invention provides a diagnostic composition for administration to human or animal subjects the composition containing multilamellar liposomes, optionally together with unilamellar liposomes, the liposomes containing at least one imaging agent and being suspended in an aqueous medium containing said imaging agent, wherein the liposomes comprise a neutral phospholipid and a charged phospholipid, the average particle diameter of the liposomes is 50-3000 nm and the concentration of imaging agent in any aqueous phase filling the interior of the liposomes is substantially the same as that in the aqueous medium in which the liposomes are suspended. The contrast agents concerned are typically X-ray, MRI or ultrasound contrast agents.

6. 发明公开

EP0782564A1 IODINATED X-RAY CONTRAST MEDIA 失效
标题翻译：碘化X射线造影剂
公开(公告)号：EP0782564A1
公开(公告)日：1997-07-09
申请号：EP95932109.0
申请日：1995-09-22
申请人： NYCOMED IMAGING AS
发明人： ALMEN, Torsten , ANDERSSON, Sven , WISTRAND, Lars-Göran , GOLMAN, Klaes , ANTONSEN, Oyvind , FOSSHEIM, Rune , WIGGEN, Unni, Nordby , WIKSTRÖM, Häkan, Medicinal Chemistry unit , KLINGSTEDT, Tomas , LEUNBACH, Ib , BERG, Arne , DUGSTAD, Harald
IPC分类号： A61K49 , C07C33 , C07C43 , C07C49 , C07C69 , C07C233 , C07C235 , C07C237 , C07C275 , C07C307 , C07C311 , C07C317
CPC分类号： C07C33/46 , A61K49/0433 , C07C33/483 , C07C235/16 , C07C237/46
摘要： The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula (I), wherein n is 0 or 1, and where n is 1 each C6R5 moiety may be the same or different; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M1, two or three non-adjacent R groups in each C6R5 moiety being iodine and at least one, and preferably two or three, R groups in each C6R5 moiety being M or M1 moieties; X denotes a bond or a group providing a 1 to 7 atom chain linking two C6R5 moieties or, where n is 0, X denotes a group R; each M independently is a non-ionic hydrophilic moiety; and each M1 independently represents a C1-4alkyl group substituted by at least one hydroxyl group and optionally linked to the phenyl ring via a carbonyl, sulphone or sulphoxide group, at least one R group being an M1 moiety; with the proviso that where n is zero either at least one M1 group other than a hydroxymethyl or 1,2-dihydroxyethyl group is present or then if one hydroxymethyl or 1,2-dihydroxyethyl M1 group is present at least one nitrogen-attached or hydroxylated-C3-4 alkyl moiety-containing M group is also present and isomers thereof.

7. 发明授权

EP0593624B1 IMPROVEMENTS IN OR RELATING TO CONTRAST AGENTS 失效
标题翻译：改进造影剂
公开(公告)号：EP0593624B1
公开(公告)日：1997-04-23
申请号：EP92915200.7
申请日：1992-07-03
申请人： NYCOMED IMAGING AS
发明人： BERG, Arne , KLAVENESS, Jo , STRANDE, Per , STUBBERUD, Lars
IPC分类号： A61K49/00 , A61K49/04
CPC分类号： A61K49/226 , A61K49/223
摘要： Ultrasound contrast agents comprising a microbubble-generating suspension of a microparticulate X-ray contrast agent in a liquid carrier medium.

8. 发明公开

EP0752889A1 LIPOSOMES 失效
标题翻译：脂质体
公开(公告)号：EP0752889A1
公开(公告)日：1997-01-15
申请号：EP95913223.0
申请日：1995-03-27
申请人： NYCOMED IMAGING AS , DAIICHI PHARMACEUTICAL CO., LTD.
发明人： KLAVENESS, Jo , BERG, Arne , JACOBSEN, Trond Vegard , RONGVED, Pal , EGE, Thorfinn , KIKUCHI, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , YACHI, Kiyoto, Daiichi Pharmaceutical Co., Ltd.
IPC分类号： A61K49 , A61K51
CPC分类号： A61K49/227 , A61K49/0466 , A61K49/1812
摘要： The invention provides a diagnostic composition for administration to human or animal subjects the composition containing multilamellar liposomes, optionally together with unilamellar liposomes, the liposomes containing at least one imaging agent and being suspended in an aqueous medium containing said imaging agent, wherein the liposomes comprise a neutral phospholipid and a charged phospholipid, the average particle diameter of the liposomes is 50-3000 nm and the concentration of imaging agent in any aqueous phase filling the interior of the liposomes is substantially the same as that in the aqueous medium in which the liposomes are suspended. The contrast agents concerned are typically X-ray, MRI or ultrasound contrast agents.
摘要翻译：本发明提供了用于给人或动物对象施用含有多层脂质体的组合物的组合物，所述组合物任选地与单层脂质体一起，所述脂质体含有至少一种显像剂并悬浮于含有所述显像剂的含水介质中，其中所述脂质体包含中性磷脂和带电荷的磷脂，脂质体的平均粒径为50-3000nm，并且填充脂质体内部的任何水相中显像剂的浓度基本上与脂质体在其中的含水介质中的浓度相同暂停。有关的造影剂通常是X射线，MRI或超声造影剂。

9. 发明授权

EP0689461B1 IMPROVEMENTS IN OR RELATING TO CONTRAST AGENTS 失效
标题翻译：改进和有关造影剂
公开(公告)号：EP0689461B1
公开(公告)日：2000-07-05
申请号：EP94909226.6
申请日：1994-03-16
申请人： NYCOMED IMAGING AS
发明人： BERG, Arne , DUGSTAD, Harald , FOSS, Per, Antonius , KLAVENESS, Jo , OSTENSEN, Jonny , RONGVED, Pal , STRANDE, Per
IPC分类号： A61K49/00
CPC分类号： A61K49/226 , A61K49/223

10. 发明公开

EP0776219A2 COMPOSITIONS 失效
标题翻译：成分
公开(公告)号：EP0776219A2
公开(公告)日：1997-06-04
申请号：EP95929155.0
申请日：1995-08-18
申请人： NYCOMED IMAGING AS , COCKBAIN, Julian
发明人： GOLMAN, Klaes , PETTERSSON, Göran , BERG, Arne , KLAVENESS, Jo , RONGVED, PAl , LEANDER, Peter , LEUNBACH, Ib , GUNTHER, Wolfgang
IPC分类号： A61K49
摘要： There is provided a contrast medium composition comprising a physiologically tolerable manganese compound, an uptake promoter and a physiologically tolerable carrier or excipient, having a manganese concentration of at least 0.3mM or being in a dosage unit form containing at least 300 νmol manganese, wherein the uptake promoter comprises a physiologically tolerable reducing compound containing an α-hydroxy ketone group, a physiologically tolerable acid containing α- and/or β-hydroxy or amino groups, or a salt thereof, and/or vitamin D. Such compositions are particularly suitable for imaging of the liver.

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