ANTON FRENKEL,AVITAL LAXER,VLADIMIR IOFFE,KARL JANSSON,ULF TOMAS ERIC - FRISTEDT
申请号：
ARP140101184
公开号：
AR095562A1
申请日:
2014.03.17
申请国别(地区):
AR
年份:
2015
代理人:
摘要：
It provides a mixture of particles of laquinimod Sodium Crystalline(i) where 90% or more of the total volume of sodium laquinimod particles have a size of 40 mm or less, or (ii) 50% or more of the total volume of the particles of LAquinimod Sodium have a size of 15 mm or less and where: (a) the mixture has an apparent density of 0.2 g / ml of 0.4 g / ml； (b) the mixture is Compacted density of 0.4 g / ml to 0.7 g / ml； (c) a quantity of heavy metal in the mixture is not more than 0,002% of heavy metal with relation to the weight of laquinimod sodium； (d) an amount of 5 - Chloro - 4 - hydroxy - 3 - methyl - 2 - oxo - 1.2 - dihidroquinolina (MCQ) in the mixture is not more than 0,15% relative to the amount of sodium laquinimod agree with the Measurement through HPLC and acid)； an amount of 5 - Chloro - 4 - hydroxy - 3 - methyl - 2 - oxo - 12 - 3 - dihidroquinolin acid (mcqca) in the mixture is not more than 0,15% relative to the amount of sodium laquinimod agree with the Measurement through HPLC； or (f) a quantity of methyl Chloro - 5 - 4 - hydroxy - 3 - methyl - 2 - oxo - 1Dihidroquinolin - 2 - 3 - carboxylate (mcqme) in the mixture is of no more than 0.12% compared to the amount of sodium laquinimod agree with the Measurement through HPLC.It also provides a Pharmaceutical composition comprising an amount of at least one laquinimod between acid and 2 - Chloro - 5 - (3 - (Ethyl (phenyl) amino) - 2 - hydroxy - 3 - methyl - N - oxopropanamido benzoic (BH) - 3 - hlaq)5 - Chloro - 4 - hydroxy - 3 - metilquinolin - 2 (1H) - One (MCQ) acid, chloro - 5 - 4 - hydroxy - 3 - methyl - 2 - oxo - 1.2 - dihidroquinolin acid (mcqca) - 3, 5 - chloro methyl - 4 - hydroxy - 3 - methyl - 2 - oxo - 1Dihidroquinolin - 2 - 3 - carboxylate (mcqme), N - etilanilina (NEA), and Ethyl Chloro - 5 - 4 - hydroxy - 3 - methyl - 2 - oxo - 1.2 - dihidroquinolin - 3 - carboxylate (mcqee).Processes for preparing BH - 3 - hlaq, McQ, mcqca, mcqme, mcqee and compounds prepared by such processes. A pro
