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    Crystalline forms of [1S-(1alpha, 3alpha, 4beta)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one
    1.
    发明申请
    Crystalline forms of [1S-(1alpha, 3alpha, 4beta)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one 审中-公开
    [1S-（1α，3α，4β）] - 2-氨基-1,9-二氢-9- [4-羟基-3-（羟甲基）-2-亚甲基环戊基] -6H-嘌呤-6-酮的结晶形式

    公开(公告)号：US20070060599A1

    公开(公告)日：2007-03-15

    申请号：US11222597

    申请日：2005-09-09

    申请人： John DiMarco ,  Jack Gougoutas

    发明人： John DiMarco ,  Jack Gougoutas

    IPC分类号： A61K31/522 ,  C07D473/04

    CPC分类号： C07D473/18

    摘要： The present invention relates to crystalline forms containing [1S-(1α,3α,4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one represented by formula I; processes for the production thereof; pharmaceutical compositions thereof; methods for preparing the pharmaceutical composition; and the use of these crystalline forms in the treatment of hepatitis B viral infections.

    摘要翻译： 本发明涉及含有[1S-（1α，3α，4beta）] - 2-氨基-1,9-二氢-9- [4-羟基-3-（羟甲基）-2-亚甲基环戊基] 由式I表示的嘌呤-6-酮; 生产过程; 其药物组合物; 制备药物组合物的方法; 以及这些结晶形式在治疗乙型肝炎病毒感染中的应用。

    Process for preparing atazanavir bisulfate and novel forms
    4.
    发明申请
    Process for preparing atazanavir bisulfate and novel forms 有权
    制备阿扎那韦硫酸氢盐和新型形式的方法

    公开(公告)号：US20050256202A1

    公开(公告)日：2005-11-17

    申请号：US11119558

    申请日：2005-05-02

    申请人： Soojin Kim ,  Bruce Lotz ,  Mary Malley ,  Jack Gougoutas ,  Martha Davidovich ,  Sushil Srivastava

    发明人： Soojin Kim ,  Bruce Lotz ,  Mary Malley ,  Jack Gougoutas ,  Martha Davidovich ,  Sushil Srivastava

    IPC分类号： A61K31/16 ,  C07C231/02 ,  C07C243/26 ,  C07D213/42

    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。

    Pyridyl-substituted spiro-hydantoin crystalline forms and process
    5.
    发明申请
    Pyridyl-substituted spiro-hydantoin crystalline forms and process 审中-公开
    吡啶基取代的螺 - 乙内酰脲结晶形式及方法

    公开(公告)号：US20060142319A1

    公开(公告)日：2006-06-29

    申请号：US11301433

    申请日：2005-12-13

    申请人： Bang-Chi Chen ,  Albert Delmonte ,  T.G. Dhar ,  Michael Galella ,  Margaret Gleeson ,  Jack Gougoutas ,  Douglas McLeod ,  Huiping Zhang

    发明人： Bang-Chi Chen ,  Albert Delmonte ,  T.G. Dhar ,  Michael Galella ,  Margaret Gleeson ,  Jack Gougoutas ,  Douglas McLeod ,  Huiping Zhang

    IPC分类号： A61K31/4747 ,  C07D487/10

    CPC分类号： C07D487/10

    摘要： The invention provides crystalline forms of 6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl]nicotinic acid, its pharmaceutically acceptable salts, or solvates, thereof Further, a process is provided for preparing substituted spiro-hydantoin compounds of the formula I wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A1, A2, G, and Q are linkers; and R2, R4a, R4c, and R16 are defined in the specification. The process includes the reaction of N-substituted glycine compound and methylene precursor compound with an alkene compound. The substituted spiro-hydantoin compounds of formulae I and II are useful in the treatment of immune and/or inflammatory diseases.

    摘要翻译： 本发明提供6 - [（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]非7-基]烟酸，其药学上可接受的盐或溶剂化物。此外，提供了制备式I的取代的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b， SUB>; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 1，A 2，G和Q是连接体; 和R 2，R 4a，R 4c和R 16在本说明书中定义。 该方法包括N-取代的甘氨酸化合物和亚甲基前体化合物与烯烃化合物的反应。 式I和II的取代的螺 - 乙内酰脲化合物可用于治疗免疫和/或炎性疾病。

    Crystalline forms and process for preparing spiro-hydantoin compounds
    9.
    发明申请
    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：US20060074099A1

    公开(公告)日：2006-04-06

    申请号：US11238427

    申请日：2005-09-29

    申请人： Albert DelMonte ,  T. Dhar ,  Yu Fan ,  Jack Gougoutas ,  Mary Malley ,  Douglas McLeod ,  Robert Waltermire ,  Chenkou Wei

    发明人： Albert DelMonte ,  T. Dhar ,  Yu Fan ,  Jack Gougoutas ,  Mary Malley ,  Douglas McLeod ,  Robert Waltermire ,  Chenkou Wei

    IPC分类号： A61K31/4747 ,  A61K31/4188 ,  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。

    Synthetic process, and crystalline forms of a pyrrolotriazine compound
    10.
    发明申请
    Synthetic process, and crystalline forms of a pyrrolotriazine compound 审中-公开
    合成方法和吡咯并三嗪化合物的结晶形式

    公开(公告)号：US20060014741A1

    公开(公告)日：2006-01-19

    申请号：US11149525

    申请日：2005-06-10

    申请人： John DiMarco ,  Jack Gougoutas ,  Bharat Patel

    发明人： John DiMarco ,  Jack Gougoutas ,  Bharat Patel

    IPC分类号： A61K31/5377 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention provides a process for preparing pyrrolotriazine compounds of formula (I) or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the pyrrolotriazine compound [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2, 1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester and pharmaceutical compositions comprising at least one crystalline form, as well of methods of using the crystalline forms in the treatment of a proliferative disease, and methods for obtaining such crystalline forms. The compounds of formula (I), including [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester, are useful for inhibiting tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

    摘要翻译： 本发明提供了制备式（I）的吡咯并三嗪化合物或其药学上可接受的盐的方法。 还提供了吡咯并三嗪化合物[4 - [[1-（3-氟苯基）甲基] -1H-吲唑-5-基氨基] -5-甲基 - 吡咯并[2,1-f] [1,2， 4]三嗪-6-基] - 氨基甲酸，（3S）-3-吗啉基甲酯和包含至少一种结晶形式的药物组合物，以及使用结晶形式治疗增殖性疾病的方法，以及用于 获得这样的结晶形式。 式（I）化合物包括[4 - [[1-（3-氟苯基）甲基] -1H-吲唑-5-基氨基] -5-甲基 - 吡咯并[2,1-f] 4]三嗪-6-基] - 氨基甲酸，（3S）-3-吗啉基甲基酯可用于抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其可用作抗增殖剂，用于治疗 癌症等疾病。