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    • 7. 发明申请
    • Process for preparing salts of 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide and novel stable forms produced therein
    • 制备4 - [[5 - [(环丙基氨基)羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三嗪-6- 甲酰胺和其中产生的新颖的稳定形式
    • US20060235020A1
    • 2006-10-19
    • US11398102
    • 2006-04-04
    • Soojin KimMary MalleyZhongping Shi
    • Soojin KimMary MalleyZhongping Shi
    • C07D253/08A61K31/53
    • C07D487/04
    • Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well. Novel Form N-1 crystals of the Form N-1 and Form N-4 crystals of the hydrochloride salt and Form N-1 crystals of the methanesulfonic acid salt of the above free base, pharmaceutical compositions containing such novel forms and a method of treating p38 kinase associated conditions, including rheumatoid arthritis are also provided.
    • 提供了选择性和一致地选择性制备新的稳定结晶盐形式的方法,即制备甲磺酸盐的N-1型,和p38激酶抑制剂4的盐酸盐的N-1和N-4型 - [[5 - [(环丙基氨基)羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三嗪-6-甲酰胺。 该方法优选使用包含甲酸/丙酮和甲酸/甲基乙基酮的溶剂体系,其产生具有合适流动性和所需粒径的晶体,并且也可以使用溶剂如N,N-二甲基甲酰胺和N,N-二甲基乙酰胺。 上述游离碱的甲磺酸盐的盐酸盐形式的N-1型和N-4型结晶的新型N-1晶体和形式N-1晶体,含有这种新形式的药物组合物和治疗方法 还提供p38激酶相关病症,包括类风湿性关节炎。