Process for Preparing Crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic Acid and Use for Production of Primovist®
    1.
    发明申请
    Process for Preparing Crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic Acid and Use for Production of Primovist® 审中-公开
    制备结晶3,6,9-三氮杂-3,6,9-三(羧甲基)-4-(4-乙氧基苄基)十一烷二酸的方法和用于生产Primovist®

    公开(公告)号:US20130158241A1

    公开(公告)日:2013-06-20

    申请号:US13703579

    申请日:2011-06-06

    IPC分类号: C07C227/18 C07C229/26

    摘要: The invention relates to a method for producing crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I by saponifying 3,6,9-triaza-3,6,9-tris(tert-butoxycarbonylmethyl)-4-(4-ethoxybenzyl)-undecanedioic acid di-tert-butyl ester of the formula II in an aqueous alkali metal hydroxide solution and using 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I for producing the gadolinium complex of 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid [(Gd-EOB-DTPA)=Primovist®].

    摘要翻译: 本发明涉及通过皂化3,6,9-三氮杂的方法制备式I的结晶3,6,9-三氮杂-3,6,9-三(羧甲基)-4-(4-乙氧基苄基)十一烷二酸 -3,6,9-三(叔丁氧基羰基甲基)-4-(4-乙氧基苄基) - 十二烷二酸二叔丁酯在碱金属氢氧化物水溶液中,并使用3,6,9-三氮杂 具有式I的-3,6,9-三(羧甲基)-4-(4-乙氧基苄基)十一烷二酸,用于制备3,6,9-三氮杂-3,6,9-三(羧甲基) - 4-(4-乙氧基苄基)十一烷二酸[(Gd-EOB-DTPA)= Primovist]。

    PROCESS FOR THE PREPARATION OF CALCOBUTROL
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF CALCOBUTROL 有权
    制备加工液的方法

    公开(公告)号:US20120309962A1

    公开(公告)日:2012-12-06

    申请号:US13508198

    申请日:2010-11-02

    IPC分类号: C07D257/02

    CPC分类号: C07D257/02

    摘要: The invention concerns a process for the preparation of the calcium complex of 0-(2,3-Dihydroxy-1-(hydroxymethyl)propyl)-1,4,7,10-tetraazacyclodecane-4,7-triacetic acid, also known as Calcobutrol, starting from the pure gadolinium complex (Gadobutrol). The invention furthermore concerns Calcobutrol with a hitherto unknown level of purity.

    摘要翻译: 本发明涉及制备O-(2,3-二羟基-1-(羟甲基)丙基)-1,4,7,10-四氮杂环癸烷-4,7-三乙酸的钙络合物的方法,也称为 Calcobutrol,从纯钆复合物(Gadobutrol)开始。 本发明还涉及迄今为止未知的纯度水平的卡布斯丁(Calcobutrol)。

    Preparation of high-purity gadobutrol

    公开(公告)号:US10072027B2

    公开(公告)日:2018-09-11

    申请号:US14112994

    申请日:2012-04-17

    IPC分类号: C07F5/00 A61K49/10 C07D257/02

    摘要: What is described is a process for producing high-purity gadobutrol in a purity (according to HPLC) of more than 99.7 or 99.8 or 99.9% and the use for preparing a pharmaceutical formulation for parenteral administration. The process is carried out using specifically controlled crystallization conditions. The more recent developments in the field of the gadolinium-containing MR contrast agents (EP 0448191 B1, CA Patent 1341176, EP 0643705 B1, EP 0986548 B1, EP 0596586 B1) include the MRT contrast agent gadobutrol (Gadovist® 1.0) which has been approved for a relatively long time in Europe and more recently also in the USA under the name Gadavist®.

    Process for the preparation of calcobutrol
    4.
    发明授权
    Process for the preparation of calcobutrol 有权
    制备钙调蛋白的方法

    公开(公告)号:US09447053B2

    公开(公告)日:2016-09-20

    申请号:US13508198

    申请日:2010-11-02

    IPC分类号: C07D257/02

    CPC分类号: C07D257/02

    摘要: A process for the preparation of the calcium complex of 10-(2, 3-Dihydroxy-1-(hydroxymethyl)propyl)-1,4,7,10-tetraazacyclodecane-4,7-triacetic acid, also known as Calcobutrol, starting from the pure gadolinium complex (Gadobutrol) is disclosed. Also disclosed is Calcobutrol with a hitherto unknown level of purity.

    摘要翻译: 一种制备10-(2,3-二羟基-1-(羟甲基)丙基)-1,4,7,10-四氮杂环癸烷-4,7-三乙酸的钙络合物的方法,也被称为卡布斯丁(Calcobutrol),起始 来自纯钆络合物(Gadobutrol)。 还公开了具有迄今未知的纯度水平的Calcobutrol。

    PREPARATION OF HIGH-PURITY GADOBUTROL
    5.
    发明申请
    PREPARATION OF HIGH-PURITY GADOBUTROL 审中-公开
    高纯GADOBUTROL的制备

    公开(公告)号:US20140107325A1

    公开(公告)日:2014-04-17

    申请号:US14112994

    申请日:2012-04-17

    IPC分类号: C07F5/00

    摘要: What is described is a process for producing high-purity gadobutrol in a purity (according to HPLC) of more than 99.7 or 99.8 or 99.9% and the use for preparing a pharmaceutical formulation for parenteral administration. The process is carried out using specifically controlled crystallization conditions. The more recent developments in the field of the gadolinium-containing MR contrast agents (EP 0448191 B1, CA Patent 1341176, EP 0643705 B1, EP 0986548 B1, EP 0596586 B1) include the MRT contrast agent gadobutrol (Gadovist® 1.0) which has been approved for a relatively long time in Europe and more recently also in the USA under the name Gadavist®.

    摘要翻译: 所描述的是用于制备纯度(根据HPLC)高于99.7或99.8或99.9%的高纯度钆布醇的方法以及用于制备胃肠外给药的药物制剂的用途。 该方法使用特定控制的结晶条件进行。 含钆MR造影剂(EP 0448191B1,CA专利1341176,EP 0643705B1,EP0986548B1,EP0596586B1)领域中最近的发展包括已经被使用的MRT造影剂钆布醇(Gadovist?1.0) 批准在欧洲相对较长的时间,最近也在美国以Gadavist®名义批准。