N-ETHYL-4-HYDROXYL-1-METHYL-5-(METHYL(2,3,4,5,6-PENTAHYDROXYHEXYL)AMINO)-2-OXO-N-PHENYL-1,2-DIHYDROQUINOLINE-3-CARBOXAMIDE
    2.
    发明申请
    N-ETHYL-4-HYDROXYL-1-METHYL-5-(METHYL(2,3,4,5,6-PENTAHYDROXYHEXYL)AMINO)-2-OXO-N-PHENYL-1,2-DIHYDROQUINOLINE-3-CARBOXAMIDE 有权
    N-乙基-4-羟基-1-甲基-5-(甲基(2,3,4,5,6-二羟甲基)氨基)-2-氧代-N-苯基-1,2-二氢喹啉-3-羧酰胺

    公开(公告)号:US20130345256A1

    公开(公告)日:2013-12-26

    申请号:US13888709

    申请日:2013-05-07

    IPC分类号: C07D215/56 A61K31/4704

    摘要: The subject invention provides pharmaceutical compositions containing laquinimod or a pharmaceutically acceptable salt thereof, an isolated compound of N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide or a salt thereof, compositions containing N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide and methods of preparing the same.

    摘要翻译: 本发明提供含有拉喹莫德或其药学上可接受的盐,N-乙基-4-羟基-1-甲基-5-(甲基(2,3,4,5,6-五羟基己基)氨基)的分离化合物的药物组合物, -2-氧代-N-苯基-1,2-二氢喹啉-3-甲酰胺或其盐包含N-乙基-4-羟基-1-甲基-5-(甲基(2,3,4,5, 6-五羟基己基)氨基)-2-氧代-N-苯基-1,2-二氢喹啉-3-甲酰胺及其制备方法。

    CRYSTALS OF LAQUINIMOD SODIUM AND IMPROVED PROCESS FOR THE MANUFACTURE THEREOF
    8.
    发明申请
    CRYSTALS OF LAQUINIMOD SODIUM AND IMPROVED PROCESS FOR THE MANUFACTURE THEREOF 有权
    LAQUINIMOD SODIUM水晶及其制造方法改进

    公开(公告)号:US20140271878A1

    公开(公告)日:2014-09-18

    申请号:US14214191

    申请日:2014-03-14

    IPC分类号: C07D215/56

    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。