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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。

    PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS
    8.
    发明申请
    PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS 有权
    制备ATAZANAVIR BISULFATE和新型的方法

    公开(公告)号：US20110124689A1

    公开(公告)日：2011-05-26

    申请号：US12900588

    申请日：2010-10-08

    申请人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

    发明人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

    IPC分类号： A61K31/4418 ,  C07D213/42 ,  A61P31/12

    CPC分类号： C07D213/42

    摘要： A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate.A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

    摘要翻译： 提供了一种制备HIV蛋白酶抑制剂阿扎那韦硫酸氢盐的方法，其中阿扎那韦游离碱的溶液与浓硫酸反应的量与小于约15重量％的游离碱反应，阿扎那韦的A型晶体种子 将硫酸氢盐加入到反应混合物中，并且以硫酸氢盐形式的结晶，按照立方式以增加的速率以多个阶段多次加入另外的浓硫酸，以实现阿扎那韦硫酸氢盐的形式A晶体的形成。 还提供了制备作为图案C材料的阿扎那韦硫酸氢盐的方法。 还提供了一种新型形式的阿扎那韦硫酸氢盐，其为E3型，其是来自乙醇的硫酸氢盐的高度结晶的三乙醇盐溶剂合物。

    PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS
    10.
    发明申请
    PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS 有权
    制备ATAZANAVIR BISULFATE和新型的方法

    公开(公告)号：US20090203630A1

    公开(公告)日：2009-08-13

    申请号：US12360468

    申请日：2009-01-27

    申请人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

    发明人： Soojin Kim ,  Bruce T. Lotz ,  Mary F. Malley ,  Jack Z. Gougoutas ,  Martha Davidovich ,  Sushil K. Srivastava

    IPC分类号： A61K38/05 ,  C07C243/18 ,  A61P31/12

    CPC分类号： C07D213/42

    摘要： A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate.A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

    摘要翻译： 提供了一种制备HIV蛋白酶抑制剂阿扎那韦硫酸氢盐的方法，其中阿扎那韦游离碱的溶液与浓硫酸反应的量与小于约15重量％的游离碱反应，阿扎那韦的A型晶体种子 将硫酸氢盐加入到反应混合物中，并且以硫酸氢盐形式的结晶，按照立方式以增加的速率以多个阶段多次加入另外的浓硫酸，以实现阿扎那韦硫酸氢盐的形式A晶体的形成。 还提供了制备作为图案C材料的阿扎那韦硫酸氢盐的方法。 还提供了一种新型形式的阿扎那韦硫酸氢盐，其为E3型，其是来自乙醇的硫酸氢盐的高度结晶的三乙醇盐溶剂合物。