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公开(公告)号：US09238615B2
公开(公告)日：2016-01-19
申请号：US13265165
申请日：2010-04-08
申请人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
发明人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
IPC分类号： C07C227/16
CPC分类号： C07C227/16 , C07C229/62
摘要： The present invention relates to a process for the preparation of iodinated anilines; in particular, it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted anilines to the corresponding 3,5-disubstituted-2,4,6-triiodoanilines, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
摘要翻译： 本发明涉及一种制备碘化苯胺的方法; 特别涉及一种方法，其包括将3,5-二取代的2,4,6-三碘苯胺与适当的活化的碘直接碘化为3,5-二取代-2,4,6-三碘苯胺，其是用于合成 x射线造影剂，以及造影剂本身的制备。
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公开(公告)号：US20120041224A1
公开(公告)日：2012-02-16
申请号：US13265165
申请日：2010-04-08
申请人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
发明人： Attilio Citterio , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli , Aurelia Ferrigato , Gabriele Meli , Roberta Fretta , Roberta Mazzon
IPC分类号： C07C231/02 , C07C231/12 , C07C227/16
CPC分类号： C07C227/16 , C07C229/62
摘要： The present invention relates to a process for the preparation of iodinated anilines; in particular, it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted anilines to the corresponding 3,5-disubstituted-2,4,6-triiodoanilines, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
摘要翻译： 本发明涉及一种制备碘化苯胺的方法; 特别涉及一种方法，其包括将3,5-二取代的2,4,6-三碘苯胺与适当的活化的碘直接碘化为3,5-二取代-2,4,6-三碘苯胺，其是用于合成 x射线造影剂，以及造影剂本身的制备。
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公开(公告)号：US08766003B2
公开(公告)日：2014-07-01
申请号：US13702223
申请日：2011-06-09
申请人： Attilio Citterio , Elisa Battistini , Davide Belnome , Federica Buonsanti , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli
发明人： Attilio Citterio , Elisa Battistini , Davide Belnome , Federica Buonsanti , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli
IPC分类号： C07C231/12 , C07C231/14 , C07B39/00
CPC分类号： C07B39/00 , C07C231/10 , C07C231/12 , C07C231/14 , C07C235/48 , C07C237/46
摘要： The present invention relates to a process for the preparation of iodinated phenols; in particular; it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted phenol compounds to the corresponding 3,5-disubstituted-2,4,6-triiodophenols, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
摘要翻译： 本发明涉及一种制备碘化酚的方法; 尤其是; 它涉及一种方法，包括将适当活化的碘直接碘化为3,5-二取代的苯酚化合物与相应的3,5-二取代-2,4,6-三碘苯酚的有用的中间体， 射线造影剂，以及造影剂本身的制备。
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公开(公告)号：US20130072719A1
公开(公告)日：2013-03-21
申请号：US13702223
申请日：2011-06-09
申请人： Attilio Citterio , Elisa Battistini , Davide Belnome , Federica Buonsanti , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli
发明人： Attilio Citterio , Elisa Battistini , Davide Belnome , Federica Buonsanti , Luciano Lattuada , Gabriella Leonardi , Fulvio Uggeri , Evelin Vignale , Massimo Visigalli
IPC分类号： C07B39/00 , C07C231/14 , C07C231/12
CPC分类号： C07B39/00 , C07C231/10 , C07C231/12 , C07C231/14 , C07C235/48 , C07C237/46
摘要： The present invention relates to a process for the preparation of iodinated phenols; in particular; it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted phenol compounds to the corresponding 3,5-disubstituted-2,4,6-triiodophenols, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
摘要翻译： 本发明涉及一种制备碘化酚的方法; 尤其是; 它涉及一种方法，包括将适当活化的碘直接碘化为3,5-二取代的苯酚化合物与相应的3,5-二取代-2,4,6-三碘苯酚的有用的中间体， 射线造影剂，以及造影剂本身的制备。
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5.发明申请Process for the Preparation of Gadobenate Dimeglumine Complex in a Solid Form 审中-公开以固体形式制备钆酸二甲酚复合物的方法公开(公告)号：US20120232151A1
公开(公告)日：2012-09-13
申请号：US13510409
申请日：2010-11-23
申请人： Pier Lucio Anelli , Pierfrancesco Morisini , Silvia Ceragioli , Fulvio Uggeri , Luciano Lattuada , Roberta Fretta , Aurelia Ferrigato
发明人： Pier Lucio Anelli , Pierfrancesco Morisini , Silvia Ceragioli , Fulvio Uggeri , Luciano Lattuada , Roberta Fretta , Aurelia Ferrigato
IPC分类号： C07C227/00 , A61K31/197 , C07C229/36
CPC分类号： A61K49/1887 , A61K9/0019 , B29C67/24 , C07C213/10 , C07C227/38 , C07C227/40 , Y10T428/2982 , C07C229/22
摘要： The present invention discloses a process for the preparation of gadobenate dimeglumine complex in a solid form. In particular, said solid form is conveniently obtained by spray-drying a corresponding liquid suspension at a given temperature and concentration. The present invention is particularly advantageous for the industrial scale as the solid form may be obtained by employing water as a solvent, which is a non-toxic solvent, easy to handle and basically not requiring troublesome health or safety precautions.
摘要翻译： 本发明公开了一种以固体形式制备钆酸二甲酚络合物的方法。 特别地，所述固体形式通过在给定温度和浓度下喷雾干燥相应的液体悬浮液而方便地得到。 本发明对于工业规模是特别有利的，因为固体形式可以通过使用水作为溶剂，其是无毒溶剂，易于处理并且基本上不需要麻烦的健康或安全预防措施来获得。
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6.发明授权Use of bile acid conjugates, derivatives thereof with metal complexes as blood pool agents for nuclear magnetic resonance diagnostics 有权使用胆汁酸共轭物，其衍生物与金属络合物作为核磁共振诊断的血液池剂公开(公告)号：US06461588B1
公开(公告)日：2002-10-08
申请号：US09318618
申请日：1999-05-26
申请人： Pier Lucio Anelli , Marino Brocchetta , Christoph De Haen , Ornella Gazzotti , Luciano Lattuada , Giovanna Lux , Giuseppe Manfredi , Pierfrancesco Morosini , Daniela Palano , Michele Serleti , Fulvio Uggeri , Massimo Visigalli
发明人： Pier Lucio Anelli , Marino Brocchetta , Christoph De Haen , Ornella Gazzotti , Luciano Lattuada , Giovanna Lux , Giuseppe Manfredi , Pierfrancesco Morosini , Daniela Palano , Michele Serleti , Fulvio Uggeri , Massimo Visigalli
IPC分类号： A61B5055
CPC分类号： A61K49/10 , A61K49/085 , Y10S977/928 , Y10S977/929 , Y10S977/93
摘要： Blood pool imaging contrast agents containing paramagnetic bi- and tri-valent metal ion chelates of bile acid conjugates with molecules having chelating activity are used in magnetic resonance imaging of the vascular system and particularly the coronaries.
摘要翻译： 血液成像造影剂含有胆酸偶联物与具有螯合活性的分子的顺磁性二价和三价金属离子螯合物用于血管系统特别是冠状动脉的磁共振成像。
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公开(公告)号：US09694090B2
公开(公告)日：2017-07-04
申请号：US13639682
申请日：2011-04-08
申请人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
发明人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
摘要： The present invention generally relates to a process for the preparation of aqueous solutions of hyperpolarized molecules ready for use in in-vivo MR diagnostic imaging, the use thereof as MRI contrast agent in investigation methods for producing diagnostic MR images of a human or non-human animal body organ, region or tissue.
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公开(公告)号：US20130096420A1
公开(公告)日：2013-04-18
申请号：US13639682
申请日：2011-04-08
申请人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
发明人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
摘要： The present invention generally relates to a process for the preparation of aqueous solutions of hyperpolarized molecules ready for use in in-vivo MR diagnostic imaging, the use thereof as MRI contrast agent in investigation methods for producing diagnostic MR images of a human or non-human animal body organ, region or tissue.
摘要翻译： 本发明一般涉及准备用于体内MR诊断成像的超极化分子的水溶液的制备方法，其用于生成人或非人的诊断性MR图像的调查方法中的MRI造影剂 动物体器官，区域或组织。
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9.发明授权Contrast agents endowed with high relaxivity for use in magnetic resonance imaging (MRI) which contain a chelating moiety with polyhydroxylated substituents 有权对比剂具有高的放松性，用于磁共振成像（MRI），其含有具有多羟基化取代基的螯合部分公开(公告)号：US07988950B2
公开(公告)日：2011-08-02
申请号：US11630605
申请日：2005-06-28
申请人： Silvio Aime , Matteo Galli , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri , Kondareddiar Ramalingam
发明人： Silvio Aime , Matteo Galli , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri , Kondareddiar Ramalingam
CPC分类号： C07H15/26 , A61K49/085 , A61K49/124 , C07C237/08 , C07D243/08 , C07D243/10 , C07F9/3808 , C07F9/4006 , C07F9/5728 , C07H17/02
摘要： The present invention relates to a novel class of paramagnetic ion-based contrast i agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic i profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity. Formula (I): A(LR)v wherein: A is a linear or cyclic chelating backbone moiety; R is, independently, H or a C2-C70aminopolyol moiety comprising a ‘straight or branched alkyl chain substituted by from 2 to 30 hydroxyl groups, the said chain being optionally interrupted by one or more groups selected from -0-, —NH—, —N NCO—; and optionally substituted by one or more C4-C10 cyclic units; L is, independently, a direct bond or “a divalent straight or branched linker moiety between A and R, at most comprising 20 carbon atoms; V is a positive integer from 1 to 7; with the proviso that at least one of the R groups is other than H; or a physiologically acceptable salt of such ligand.
摘要翻译： 本发明涉及一类新颖的式（I）的顺磁离子型对比剂，其中螯合骨架部分通过存在一个或多个多羟基化链而被高度官能化，其显示类似于 常用的T1一般血管外药物（NSA），但其进一步特征在于较高的松弛度。 式（I）：A（LR）v其中：A是直链或环状螯合骨架部分; R独立地是H或包含被2至30个羟基取代的“直链或支链烷基链”的C2-C70氨基多酚部分，所述链任选地被一个或多个选自-O-，-NH-， -N'， - CO - ， - CONH - ， - NHCO-，-CON'或> NCO-; 并任选地被一个或多个C 4 -C 10环单元取代; L独立地是直接键或“A和R之间的二价直链或支链连接体部分，最多包含20个碳原子; V是1到7的正整数; 条件是至少一个R基团不是H; 或这种配体的生理上可接受的盐。
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10.发明授权Paramagnetic metal icon chelates and use thereof as contrast agents in magnetic resonance imaging 失效顺磁性金属图标螯合物及其在磁共振成像中作为造影剂的用途
公开(公告)号：US5649537A
公开(公告)日：1997-07-22
申请号：US443342
申请日：1995-05-17
申请人： Pier Lucio Anelli , Christoph De Haen , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri
发明人： Pier Lucio Anelli , Christoph De Haen , Luciano Lattuada , Pierfrancesco Morosini , Fulvio Uggeri
CPC分类号： A61K49/10 , A61K49/085 , A61K51/0493 , A61K51/0497 , A61K2123/00
摘要： Novel paramagnetic metal ion chelates and their use as contrast agents in the diagnostic technique known as "magnetic resonance imaging" (M.R.I.) of the gastrointestinal tract and particularly of the liver, are described. The novel compounds result from the conjugation of a bile acid with a chelating agent and are capable of chelating the ions of bivalent and trivalent metals. The compounds have formula A-L-B in which A is the residue of a bile acid and derivatives of a bile acid, B is the residue of a chelating agent of a bivalent or trivalent metal ion having an atomic number of 20 to 31, 39, 42, 43, 44, 49, 57 to 83, L is a ligand between A and B.
摘要翻译： 描述了新型顺磁性金属离子螯合物及其在称为“磁共振成像”（M.R.I.）的胃肠道特别是肝脏的诊断技术中作为造影剂的用途。 新型化合物由胆汁酸与螯合剂结合而产生，并能螯合二价和三价金属的离子。 所述化合物具有式ALB，其中A是胆汁酸的残基和胆汁酸的衍生物，B是二价或三价金属离子的螯合剂的残基，其原子序数为20至31,39,42， 43，44，49，57至83，L是A和B之间的配体。
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