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    CRYSTALLINE FORMS AND PROCESS FOR PREPARING SPIRO-HYDANTOIN COMPOUNDS
    6.
    发明申请
    CRYSTALLINE FORMS AND PROCESS FOR PREPARING SPIRO-HYDANTOIN COMPOUNDS 审中-公开
    晶体形式和制备SPIRO-HYDANTOIN化合物的方法

    公开(公告)号：US20080269499A1

    公开(公告)日：2008-10-30

    申请号：US12130915

    申请日：2008-05-30

    申请人： Albert J. DelMonte ,  T.G. Murali Dhar ,  Yu Fan ,  Jack Z. Gougoutas ,  Mary F. Malley ,  Douglas D. McLeod ,  Robert E. Waltermire ,  Chenkou Wei

    发明人： Albert J. DelMonte ,  T.G. Murali Dhar ,  Yu Fan ,  Jack Z. Gougoutas ,  Mary F. Malley ,  Douglas D. McLeod ,  Robert E. Waltermire ,  Chenkou Wei

    IPC分类号： C07D487/10

    CPC分类号： C07D487/10

    摘要： A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.

    摘要翻译： 提供了制备式II的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 2是连接体，G'是连接体; Q是一个连接符; 和R 2，R 4a，R 4c和R h H在本说明书中定义。 该方法任选地包括中间体的对映异构体分离，以允许制备式II的螺 - 乙内酰脲化合物的对映异构体。 取代的螺 - 乙内酰脲化合物可以由式II的螺 - 乙内酰脲化合物制备。 式II的螺 - 乙内酰脲化合物和取代的螺 - 乙内酰脲化合物可用于治疗免疫或炎性疾病。 此外，提供的是本发明方法制备的产物和取代的螺 - 乙内酰脲化合物的5 - [（5S，9R）-9-（4-氰基苯基）-3-（3， 5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[4.4]壬-7-基甲基] - 噻吩-3-甲酸，包括其溶剂合物及其盐，以及 使用它。 提供某些中间体的结晶形式。

    Crystalline forms and process for preparing spiro-hydantoin compounds
    7.
    发明授权
    Crystalline forms and process for preparing spiro-hydantoin compounds 有权
    结晶形式和制备螺 - 乙内酰脲化合物的方法

    公开(公告)号：US07381737B2

    公开(公告)日：2008-06-03

    申请号：US11238427

    申请日：2005-09-29

    申请人： Albert J. DelMonte ,  T. G. Murali Dhar ,  Yu Fan ,  Jack Z. Gougoutas ,  Mary F. Malley ,  Douglas D. McLeod ,  Robert E. Waltermire ,  Chenkou Wei

    发明人： Albert J. DelMonte ,  T. G. Murali Dhar ,  Yu Fan ,  Jack Z. Gougoutas ,  Mary F. Malley ,  Douglas D. McLeod ,  Robert E. Waltermire ,  Chenkou Wei

    IPC分类号： A61K31/4188 ,  C07D235/00

    CPC分类号： C07D487/10

    摘要： A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.

    摘要翻译： 提供了制备式II的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 2是连接体，G'是连接体; Q是一个连接符; 和R 2，R 4a，R 4c和R h H在本说明书中定义。 该方法任选地包括中间体的对映异构体分离，以允许制备式II的螺 - 乙内酰脲化合物的对映异构体。 取代的螺 - 乙内酰脲化合物可以由式II的螺 - 乙内酰脲化合物制备。 式II的螺 - 乙内酰脲化合物和取代的螺 - 乙内酰脲化合物可用于治疗免疫或炎性疾病。 此外，提供的是本发明方法制备的产物和取代的螺 - 乙内酰脲化合物的5 - [（5S，9R）-9-（4-氰基苯基）-3-（3， 5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[4.4]壬-7-基甲基] - 噻吩-3-甲酸，包括其溶剂合物及其盐，以及 使用它。 提供某些中间体的结晶形式。

    CRYSTALLINE FORMS OF (S)-1-(4-(5-CYCLOPROPYL-1H-PYRAZOL-3-YLAMINO)PYRROLO[1,2-f][1,2,4]TRIAZIN-2-YL)-N-(6-FLUOROPYRIDIN-3-YL)-2-METHYLPYRROLIDINE-2-CARBOXAMIDE
    10.
    发明申请
    CRYSTALLINE FORMS OF (S)-1-(4-(5-CYCLOPROPYL-1H-PYRAZOL-3-YLAMINO)PYRROLO[1,2-f][1,2,4]TRIAZIN-2-YL)-N-(6-FLUOROPYRIDIN-3-YL)-2-METHYLPYRROLIDINE-2-CARBOXAMIDE 失效
    （S）-1-（4-（5-环丙基）-1H-吡唑-3-基]氨基]吡咯并[1,2-f] [1,2,4]三嗪-2-基）-N-（ 6-氟吡啶-3-基）-2-甲基吡咯烷-2-羧酸酰胺

    公开(公告)号：US20120302571A1

    公开(公告)日：2012-11-29

    申请号：US13576973

    申请日：2011-02-03

    申请人： Roxana Schlam ,  Alicia Tee Fuay Ng ,  Chenkou Wei

    发明人： Roxana Schlam ,  Alicia Tee Fuay Ng ,  Chenkou Wei

    IPC分类号： C07D487/04 ,  A61P35/00 ,  A61K31/53

    CPC分类号： C07D487/04

    摘要： Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.

    摘要翻译： （S）-1-（4-（5-环丙基-1H-吡唑-3-基氨基）吡咯并[1,2-f] [1,2,4]三嗪-2-基）-N-（ 6-氟吡啶-3-基）-2-甲基吡咯烷-2-甲酰胺。 还提供了包含一种或多种结晶形式的（3R，4R）-4-氨基-1 - [[4 - [（3-甲氧基苯基）氨基]吡咯并[2,1-f] [1,2， 4]三嗪-5-基]甲基]哌啶-3-醇，以及使用一种或多种结晶形式的（3R，4R）-4-氨基-1 - [[4 - [（3-甲氧基苯基） ）氨基]吡咯并[2,1-f] [1,2,4]三嗪-5-基]甲基]哌啶-3-醇用于治疗癌症和其它增殖性疾病。