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1. 发明申请

US20230133715A1 CONTINUOUS CRYSTALLISATION METHOD 有权
公开(公告)号：US20230133715A1
公开(公告)日：2023-05-04
申请号：US17912646
申请日：2021-03-31
申请人： GE Healthcare AS
发明人： Torfinn Haaland , Arne Askildsen , Heidi Kvande
IPC分类号： C07C231/24 , C07C237/46
摘要： The invention provides a method of purifying 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide, comprising adding a portion of acid to a stream comprising crude 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide in a solvent and continuously crystallising the 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide from the crude 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophathalamide, with removal of at least a fraction of the solvent, wherein the crystallisation is carried out in a continuous reactor, wherein the continuous reactor is a plug flow reactor. At least three further portions of acid are added to the continuous reactor during the crystallisation.

2. 发明申请

US20180169607A1 Process for the Preparation of Intermediates Useful in the Preparation of Non-ionic Contrast Agents 审中-公开
公开(公告)号：US20180169607A1
公开(公告)日：2018-06-21
申请号：US15578952
申请日：2016-06-02
申请人： Hovione Scientia Limited
发明人： William Heggie , John Naber , Patrick R. Bazinet , Filipe Tomas
IPC分类号： B01J19/18 , B01J19/00 , C07C237/46 , C07C231/02 , C07C233/69 , C07C227/04 , C07C227/18 , C07C229/62 , C07C17/12 , C07C22/04
CPC分类号： B01J19/1818 , B01J19/0006 , B01J19/0053 , B01J2219/00033 , B01J2219/0004 , B01J2219/00051 , B01J2219/00162 , B01J2219/00164 , B01J2219/00182 , B01J2219/00186 , C07C17/12 , C07C22/04 , C07C227/04 , C07C227/16 , C07C227/18 , C07C229/62 , C07C231/02 , C07C231/12 , C07C233/69 , C07C237/46 , C07C237/32 , C07C235/16
摘要： The invention relates to a process for the preparation of one or more intermediate chemical compounds useful in the preparation of non-ionic contrast agents wherein the process is carried out continuously using one or more flow procedures.

3. 发明授权

US09730902B2 Polyamine transport inhibitors as novel therapeutics 有权
公开(公告)号：US09730902B2
公开(公告)日：2017-08-15
申请号：US14962195
申请日：2015-12-08
申请人： Otto Phanstiel, IV , Jennifer J. Archer
发明人： Otto Phanstiel, IV , Jennifer J. Archer
IPC分类号： A61K31/135 , A61K31/166 , C07C237/46 , C07D295/13 , A61K31/137 , C07C211/27 , C07C231/02 , C07C233/78 , C07C235/10 , A61K31/192 , A61K31/197 , A61K45/06
CPC分类号： A61K31/166 , A61K31/137 , A61K31/192 , A61K31/197 , A61K45/06 , C07C211/27 , C07C231/02 , C07C233/78 , C07C235/10 , C07C237/46 , C07D295/13
摘要： Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.

4. 发明申请

US20160200670A1 RADIOPAQUE MONOMERS, POLYMERS, MICROSPHERES, AND METHODS RELATED THERETO 审中-公开
标题翻译：放射性单体，聚合物，微球和与之相关的方法
公开(公告)号：US20160200670A1
公开(公告)日：2016-07-14
申请号：US14992580
申请日：2016-01-11
申请人： Biosphere Medical, Inc.
发明人： Philippe Reb
IPC分类号： C07C237/04 , A61K31/785 , A61K49/04 , A61K49/18 , C08F222/38 , C08F220/58 , A61K49/12 , A61K31/704 , C07C237/46
CPC分类号： A61K49/1818 , A61K9/0019 , A61K9/1635 , A61K31/704 , A61K47/02 , A61K49/0438 , A61K49/0442 , A61K49/048 , A61K49/126 , C07C231/08 , C08F220/58 , C08F222/385 , C07C237/52
摘要： Radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of using the radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of manufacturing radiopaque monomers, polymers, and microspheres are disclosed herein.
摘要翻译：本文公开了不透射线单体，聚合物和微球。本文公开了使用不透射线单体，聚合物和微球的方法。本文公开了制造不透射线单体，聚合物和微球的方法。

5. 发明授权

US09193659B2 Process for the iodination of aromatic compounds 有权
标题翻译：芳香族化合物碘化方法
公开(公告)号：US09193659B2
公开(公告)日：2015-11-24
申请号：US12918001
申请日：2009-02-16
申请人： Giovanni Battista Giovenzana , Camilla Cavallotti , Luciano Lattuada , Fulvio Uggeri
发明人： Giovanni Battista Giovenzana , Camilla Cavallotti , Luciano Lattuada , Fulvio Uggeri
IPC分类号： C07C221/00 , C07C51/363 , C07B39/00 , C07C37/62 , C07C67/307 , C07C231/12 , C07C237/46 , C25B3/06
CPC分类号： C07C51/363 , C07B39/00 , C07C37/62 , C07C67/307 , C07C231/12 , C07C237/46 , C25B3/06 , C07C65/03 , C07C69/88 , C07C235/48 , C07C39/27
摘要： The present invention relates to a process for the preparation of iodinated phenols, —in particular, it relates to a process including the electrochemical iodination of 3,5-disubstituted phenols of formula (1) to the corresponding 3,5-disubstituted-2, 4,6-triiodophenols of formula (2), which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves. Furthermore, the present invention includes the electrochemical iodination of 3, 5- disubstituted anilines of formula (6) to the corresponding 3,5-disubstituted-2,4,6-triiodoanilins of formula (7).
摘要翻译：本发明涉及一种制备碘化酚的方法，特别涉及一种方法，其包括将式（1）的3,5-二取代的酚电化学碘化为相应的3,5-二取代的-2，式（2）的4,6-三碘苯酚，其是用于合成x射线造影剂的有用的中间体，以及造影剂本身的制备。此外，本发明包括将式（6）的3,5-二取代的苯胺电化学碘化为相应的式（7）的3,5-二取代-2,4,6-三碘苯胺。

6. 发明申请

US20110207963A1 PREPARATION OF IODIXANOL 审中-公开
标题翻译：伊曲康醇的制备
公开(公告)号：US20110207963A1
公开(公告)日：2011-08-25
申请号：US12862023
申请日：2010-08-24
申请人： OLE MAGNE HOMESTAD
发明人： OLE MAGNE HOMESTAD
IPC分类号： C07C237/46
CPC分类号： C07C231/08 , C07C237/46
摘要： A process for the preparation of iodixanol by dimerisation of 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”) in which, after the dimerisation step, unreacted Compound A is precipitated from the reaction mixture and recovered for re-use. The process substantially increases the net yield of iodixanol and simplifies its purification.
摘要翻译：通过5-乙酰氨基-N，N'-双（2,3-二羟基丙基）-2,4,6-三碘 - 间苯二甲酰胺（“化合物A”）的二聚制备碘克沙醇的方法，其中二聚步骤，未反应的化合物A从反应混合物中沉淀并回收再利用。该方法大大提高了碘克沙醇的净产率，并简化了其纯化。

7. 发明申请

US20100233097A1 CONTRAST AGENTS 失效
标题翻译：对比剂
公开(公告)号：US20100233097A1
公开(公告)日：2010-09-16
申请号：US12739989
申请日：2008-11-06
申请人： Veronique Morrison-Iverson , Duncan George Wynn
发明人： Veronique Morrison-Iverson , Duncan George Wynn
IPC分类号： A61K49/04 , C07C237/46 , A61P43/00
CPC分类号： C07C237/46 , A61K49/0433
摘要： Compounds of formula (I) RA—CO—N(R2)—(CR12)n—N(R5)—RB and salts or optical active isomers thereof, wherein each R1 independently are the same or different and denotes a hydrogen atom, a hydroxyl group, a C1 to C4 straight of branched alkyl group or a C1 to C4 straight of branched oxyalkyl group; R2 denotes a hydrogen atom or a C1 to C4 straight of branched alkyl group; R5 independently are the same or different and denotes a acyl moiety; RA and RB independently are the same or different and denote a triiodinated phenyl group, preferably a 2,4,6-triiodinated phenyl group further substituted by two groups R3 in the 3 and 5 positions wherein each R3 are the same or different and denote a hydrogen atom or a non-ionic hydrophilic moiety, provided that at least one R3 group in the compound of formula (I) is a hydrophilic moiety; and n denotes a positive integer of 1 to 6. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.
摘要翻译：式（I）化合物RA-CO-N（R2） - （CR12）n-N（R5）-RB及其盐或光学活性异构体，其中每个R 1各自独立地相同或不同，表示氢原子，羟基，支链烷基的C1〜C4直链或支链烷氧基的C1〜C4直链; R2表示氢原子或支链烷基的C1〜C4直链; R5独立地相同或不同，表示酰基部分; RA和RB独立地相同或不同，表示三碘代苯基，优选2,4,6-三碘代苯基，其进一步被3和5位的R3基团取代，其中每个R 3相同或不同，表示氢原子或非离子亲水部分，条件是式（I）化合物中的至少一个R 3基团是亲水部分; 并且n表示1至6的正整数。本发明还涉及这种诊断组合物作为造影剂在诊断成像中，特别是在X射线成像中的用途，以及含有这些化合物的造影剂。

8. 发明申请

US20090253935A1 PREPARATION OF IODIXANOL 有权
标题翻译：伊曲康醇的制备
公开(公告)号：US20090253935A1
公开(公告)日：2009-10-08
申请号：US11573283
申请日：2005-08-08
申请人： Jan Cervenka , Khalid Hussain
发明人： Jan Cervenka , Khalid Hussain
IPC分类号： C07C237/46
CPC分类号： C07C231/24 , C07C237/46
摘要： A process for the manufacture of iodixanol by performing a purification process of the crude product in a solvent comprising 1-methoxy-2-propanol. The crude product may be obtained in aqueous solution from dimerisation of 5-acetamido-N,N′-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”).
摘要翻译：通过在包含1-甲氧基-2-丙醇的溶剂中进行粗产物的纯化方法制备碘克沙醇的方法。粗产物可以从5-乙酰氨基-N，N'-双（2,3-二羟丙基）-2,4,6-三碘 - 间苯二酰胺（“化合物A”）的二聚的水溶液中获得。

9. 发明授权

US6137006A Preparation of tri-iodo benzene compounds 有权
标题翻译：三碘苯化合物的制备
公开(公告)号：US6137006A
公开(公告)日：2000-10-24
申请号：US436654
申请日：1999-11-09
申请人： William Thieking , Einar Odd Ingvoldstad , Trygve Gulbrandsen
发明人： William Thieking , Einar Odd Ingvoldstad , Trygve Gulbrandsen
IPC分类号： C07C22/00 , C07C231/12 , C07C233/00 , C07C237/46
CPC分类号： C07C231/12
摘要： The invention provides a process by which ultra low salt content triiodinated aromatic compounds may be isolated from a highly acidic hot triiodination raction medium in a straightforward fashion. The process involves increasing the pH to above 5 with sodium hydroxide, addition of sodium bisulphite and/or sodium dithionite, addition of seed crystals, cooling slowly, and washing the collected precipitate with water.
摘要翻译：本发明提供了一种可以以直接的方式从高酸性热三碘化靛化反应介质中分离出超低盐含量的三碘化芳族化合物的方法。该方法包括用氢氧化钠将pH调节至5以上，加入亚硫酸氢钠和/或连二亚硫酸钠，加入晶种，缓慢冷却，并用水洗涤收集的沉淀物。

10. 发明授权

US5965772A Process for the preparation of 5-(acetyl(2,3-dihydroxypropyl)amino-N,N-bis(2,3-dihydroxypropyl)-2,4,6-t riiodo 失效
标题翻译：制备5-（乙酰基（2,3-二羟基丙基）氨基-N，N-双（2,3-二羟基丙基）-2,4,6-三碘代
公开(公告)号：US5965772A
公开(公告)日：1999-10-12
申请号：US84922
申请日：1998-05-28
申请人： Nicola Desantis
发明人： Nicola Desantis
IPC分类号： C07C233/00 , C07C229/62 , C07C231/02 , C07C231/08 , C07C233/33 , C07C237/46 , C07C237/52 , C07C233/05
CPC分类号： C07C227/18 , C07C231/02 , C07C231/08 , C07C237/52
摘要： A process for the preparation of 5-[acetyl(2,3-dihydroxypropyl)amino]-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide of formula (I), starting from 5-amino-1,3-benzenedicarboxylic acid of formula (II), comprising the following steps:step a) is the reaction in heterogeneous phase between 5-amino-2,4,6-triiodo-1,3-benzenedicarboxylic acid and thionyl chloride in a solvent selected from the group consisting of: straight or branched (C.sub.7 -C.sub.16) hydrocarbons, (C.sub.7 -C.sub.8) aromatic hydrocarbons, 1,1,1-trichloroethane, n-butyl acetate, diglyme (diethylene glycol dimethyl ether), in the presence of catalytic amounts of a tertiary amine, to give compound (III);step b) is the acetylation reaction of compound (III) with glacial acetic acid both as the solvent and the reagent and thionyl chloride;step c) is the formation of compound (V) by reaction of the compound (IV) with 1-amino-2,3-propanediol, by reaction of compound (IV) in a dipolar aprotic solvent, selected from the group of dimethylformamide (DMF), dimethylacetamide (DMA), dimethylsulfoxide (DMSO) or N-methyl-pyrrolidinone;step d) is the alkylation of the compound (V) in aqueous solution at basic pH, by addition of a sodium hydroxide-calcium hydroxide mixture, with 3-chloro-1,2-propanediol or epichlorohydrin, at a temperature of 40-90.degree. C.
摘要翻译：制备式（5）的5- [乙酰基（2,3-二羟丙基）氨基] -N，N'-双（2,3-二羟基丙基）-2,4,6-三碘-1,3-苯二甲酰胺的方法， I），由式（II）的5-氨基-1,3-苯二甲酸开始，包括以下步骤：步骤a）是非均相中5-氨基-2,4,6-三碘-1 （C7-C16）烃，（C7-C8）芳香族烃，1,1,1-三氯乙烷，乙酸正丁酯，二甘醇二甲醚（二乙烯基醚）的溶剂中选择3-苯二甲酸和亚硫酰氯，二乙二醇二甲醚），在催化量的叔胺的存在下，得到化合物（III）; 步骤b）是化合物（III）与冰乙酸作为溶剂和试剂和亚硫酰氯的乙酰化反应; 步骤c）是通过化合物（IV）与1-氨基-2,3-丙二醇的反应，通过化合物（IV）在偶极非质子溶剂中的反应，形成化合物（V），所述偶极非质子溶剂选自二甲基甲酰胺 DMF），二甲基乙酰胺（DMA），二甲基亚砜（DMSO）或N-甲基 - 吡咯烷酮; 步骤d）是在碱性pH下，通过在40-90℃的温度下加入氢氧化钠 - 氢氧化钙混合物与3-氯-1,2-丙二醇或表氯醇，将化合物（Ⅴ）在水溶液中烷基化 DEG C.

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