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1. 发明申请

US20140171647A1 CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF 审中-公开
标题翻译： LAQUINIMOD SODIUM的晶体及其制造方法
公开(公告)号：US20140171647A1
公开(公告)日：2014-06-19
申请号：US14185470
申请日：2014-02-20
申请人： Anton Frenkel , Eduard Gurevich , Avital Laxer
发明人： Anton Frenkel , Eduard Gurevich , Avital Laxer
IPC分类号： C07D215/56
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/54
摘要： Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
摘要翻译：公开了一种在形成盐形成步骤之后除去杂质的拉喹莫德钠的制备方法，从而得到更高纯度的晶体以及具有改善的结晶特性的晶体。

2. 发明授权

US08647646B2 Crystals of laquinimod sodium, and process for the manufacture thereof 有权
标题翻译：拉喹莫德钠晶体及其制造方法
公开(公告)号：US08647646B2
公开(公告)日：2014-02-11
申请号：US13011233
申请日：2011-01-21
申请人： Anton Frenkel , Eduard Gurevich , Avital Laxer
发明人： Anton Frenkel , Eduard Gurevich , Avital Laxer
IPC分类号： C07D215/00 , A01N43/42 , A61K31/47
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/54
摘要： Disclosed is a process for the preparation of laguinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
摘要翻译：本发明公开了一种在盐形成步骤之后除去杂质的拉可霉素钠的制备方法，从而得到更高纯度的晶体以及具有改善的结晶特性的晶体。

3. 发明申请

US20070088050A1 Crystals of laquinimod sodium, and process for the manufacture thereof 有权
标题翻译：拉喹莫德钠晶体及其制造方法
公开(公告)号：US20070088050A1
公开(公告)日：2007-04-19
申请号：US11583282
申请日：2006-10-18
申请人： Anton Frenkel , Eduard Gurevich , Avital Laxer
发明人： Anton Frenkel , Eduard Gurevich , Avital Laxer
IPC分类号： A61K31/4704
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/54
摘要： Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
摘要翻译：公开了一种在形成盐形成步骤之后除去杂质的拉喹莫德钠的制备方法，从而得到更高纯度的晶体以及具有改善的结晶特性的晶体。

4. 发明授权

US08673322B2 Crystals of laquinimod sodium, and process for the manufacture thereof 有权
标题翻译：拉喹莫德钠晶体及其制造方法
公开(公告)号：US08673322B2
公开(公告)日：2014-03-18
申请号：US13011187
申请日：2011-01-21
申请人： Anton Frenkel , Eduard Gurevich , Avital Laxer
发明人： Anton Frenkel , Eduard Gurevich , Avital Laxer
IPC分类号： C07D215/00 , A01N43/42 , A61K31/47
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/54
摘要： Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
摘要翻译：公开了一种制备拉喹莫德钠的方法，该方法在盐形成步骤之后除去杂质，从而产生更高纯度的晶体以及具有改善的结晶特性的晶体。

5. 发明申请

US20110118308A1 CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF 有权
标题翻译： LAQUINIMOD SODIUM的晶体及其制造方法
公开(公告)号：US20110118308A1
公开(公告)日：2011-05-19
申请号：US13011187
申请日：2011-01-21
申请人： Anton Frenkel , Eduard Gurevich , Avital Laxer
发明人： Anton Frenkel , Eduard Gurevich , Avital Laxer
IPC分类号： A61K31/47 , C07D215/58 , A61P37/02
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/54
摘要： Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
摘要翻译：公开了一种在形成盐形成步骤之后除去杂质的拉喹莫德钠的制备方法，从而得到更高纯度的晶体以及具有改善的结晶特性的晶体。

6. 发明申请

US20110112141A1 CRYSTALS OF LAQUINIMOD SODIUM, AND PROCESS FOR THE MANUFACTURE THEREOF 有权
标题翻译： LAQUINIMOD SODIUM的晶体及其制造方法
公开(公告)号：US20110112141A1
公开(公告)日：2011-05-12
申请号：US13011233
申请日：2011-01-21
申请人： Anton Frenkel , Eduard Gurevich , Avital Laxer
发明人： Anton Frenkel , Eduard Gurevich , Avital Laxer
IPC分类号： A61K31/47 , C07D215/58 , A61P37/02
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/54
摘要： Disclosed is a process for the preparation of laguinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
摘要翻译：本发明公开了一种在盐形成步骤之后除去杂质的拉可霉素钠的制备方法，从而得到更高纯度的晶体以及具有改善的结晶特性的晶体。

7. 发明授权

US07884208B2 Crystals of laquinimod sodium, and process for the manufacture thereof 有权
标题翻译：拉喹莫德钠晶体及其制造方法
公开(公告)号：US07884208B2
公开(公告)日：2011-02-08
申请号：US11583282
申请日：2006-10-18
申请人： Anton Frenkel , Eduard Gurevich , Avital Laxer
发明人： Anton Frenkel , Eduard Gurevich , Avital Laxer
IPC分类号： A01N43/42 , A61K35/00
CPC分类号： C07D215/56 , A61K31/4704 , C07D215/54
摘要： Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
摘要翻译：公开了一种在形成盐形成步骤之后除去杂质的拉喹莫德钠的制备方法，从而得到更高纯度的晶体以及具有改善的结晶特性的晶体。

8. 发明授权

US08975279B2 Amine salts of laquinimod 有权
标题翻译：拉喹莫德的胺盐
公开(公告)号：US08975279B2
公开(公告)日：2015-03-10
申请号：US14068599
申请日：2013-10-31
申请人： Anton Frenkel , Avital Laxer , Judith Aronheim
发明人： Anton Frenkel , Avital Laxer , Judith Aronheim
IPC分类号： C12Q1/68 , C07D215/56 , C07C215/08 , C07C215/10 , C07C229/26
CPC分类号： C07D215/56 , C07C215/08 , C07C215/10 , C07C215/40 , C07C229/26
摘要： The subject invention provides a Laquinimod amine salt, which is laquinimod meglumine, laquinimod choline hydroxide, laquinimod L-lysine or laquinimod monoethanolamine.
摘要翻译：本发明提供了拉喹莫德胺盐，其为拉喹莫德葡甲胺，拉喹莫德胆碱氢氧化物，拉喹莫德L-赖氨酸或拉喹莫德单乙醇胺。

9. 发明授权

US09233927B2 Crystals of laquinimod sodium and improved process for the manufacture thereof 有权
标题翻译：拉喹莫德钠晶体及其制备方法
公开(公告)号：US09233927B2
公开(公告)日：2016-01-12
申请号：US14214191
申请日：2014-03-14
申请人： Anton Frenkel , Avital Laxer
发明人： Anton Frenkel , Avital Laxer
IPC分类号： C07D215/56
CPC分类号： C07D215/56 , A61K31/47 , C07B2200/13 , G01N30/06 , G01N33/15
摘要： The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroqunoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; or f) an amount of methyl 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate (MCQME) in the mixture is no more than 0.12% relative to the amount of laquinimod sodium as measured by HPLC.
摘要翻译：本发明提供结晶laquinimod钠颗粒的混合物，其中（i）拉喹莫德钠颗粒的总体积的90％或更多具有40微米或更小的尺寸或（ii）总量的50％或更多拉喹莫德钠颗粒的体积量具有15微米或更小的尺寸，并且其中：a）混合物的堆积密度为0.2g / mL至0.4g / mL; b）混合物的密度为0.40g / mL至0.7g / mL; c）混合物中重金属的量相对于拉喹莫德钠的重量计不超过0.002％重金属; d）混合物中5-氯-4-羟基-1-甲基-2-氧代-1,2-二氢喹啉（MCQ）的量相对于通过HPLC测定的拉喹莫德钠的量不超过0.15％; e）混合物中5-氯-4-羟基-1-甲基-2-氧代-1,2-二氢喹啉-3-羧酸（MCQCA）的量相对于拉喹莫德钠的量不超过0.15％通过HPLC测量; 或f）混合物中5-氯-4-羟基-1-甲基-2-氧代-1,2-二氢喹啉-3-羧酸甲酯（MCQME）的量相对于拉喹莫德的量不超过0.12％通过HPLC测量的钠。

10. 发明申请

US20140128430A1 AMINE SALTS OF LAQUINIMOD 有权
标题翻译： LAQUINIMOD的胺盐
公开(公告)号：US20140128430A1
公开(公告)日：2014-05-08
申请号：US14068599
申请日：2013-10-31
申请人： Anton Frenkel , Avital Laxer , Judith Aronheim
发明人： Anton Frenkel , Avital Laxer , Judith Aronheim
IPC分类号： C07D215/56 , C07C229/26 , C07C215/08 , C07C215/10
CPC分类号： C07D215/56 , C07C215/08 , C07C215/10 , C07C215/40 , C07C229/26
摘要： The subject invention provides a Laquinimod amine salt, which is laquinimod meglumine, laquinimod choline hydroxide, laquinimod L-lysine or laquinimod monoethanolamine.
摘要翻译：本发明提供了拉喹莫德胺盐，其为拉喹莫德葡甲胺，拉喹莫德胆碱氢氧化物，拉喹莫德L-赖氨酸或拉喹莫德单乙醇胺。

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