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    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
    5.
    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 审中-公开
    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]三氮杂- 碳酰胺和生产的新型稳定形式

    公开(公告)号：US20120108594A1

    公开(公告)日：2012-05-03

    申请号：US13293204

    申请日：2011-11-10

    申请人： Soojin Kim ,  Mary F. Malley ,  Zhongping Shi

    发明人： Soojin Kim ,  Mary F. Malley ,  Zhongping Shi

    IPC分类号： A61K31/53 ,  A61P29/00 ,  A61P11/06 ,  A61P11/00 ,  A61P19/02 ,  A61P1/00 ,  A61P19/10 ,  A61P17/06 ,  A61P37/06 ,  A61P9/10 ,  C07D487/04 ,  A61P3/10

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。

    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
    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 审中-公开
    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]三氮杂- 碳酰胺和生产的新型稳定形式

    公开(公告)号：US20090312331A1

    公开(公告)日：2009-12-17

    申请号：US12478210

    申请日：2009-06-04

    申请人： Soojin Kim ,  Mary F. Malley ,  Zhongping Shi

    发明人： Soojin Kim ,  Mary F. Malley ,  Zhongping Shi

    IPC分类号： A61K31/53 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。

    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
    8.
    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 审中-公开
    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

    公开(公告)号：US20060235020A1

    公开(公告)日：2006-10-19

    申请号：US11398102

    申请日：2006-04-04

    申请人： Soojin Kim ,  Mary Malley ,  Zhongping Shi

    发明人： Soojin Kim ,  Mary Malley ,  Zhongping Shi

    IPC分类号： C07D253/08 ,  A61K31/53

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。