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    Amorphous object of cinnamide compound
    1.
    发明申请
    Amorphous object of cinnamide compound 失效
    肉桂酰胺化合物的无定形物

    公开(公告)号：US20090203916A1

    公开(公告)日：2009-08-13

    申请号：US11663550

    申请日：2005-10-25

    申请人： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    发明人： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    IPC分类号： C07D401/10

    CPC分类号： C07D401/10

    摘要： An amorphous object of (3E)-1-[l(s)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4methyl-1H-imidazol-1-yl)benzylidene]piperidine-2-one, which is represented by the formula (1) and has Aβ-production inhibitory activity. The amorphous object has such satisfactory properties that it has excellent solubility, is stable, does not readily become a crystalline form, and has low hygroscopicity. It is hence suitable for use in pharmaceutical preparations.

    摘要翻译： （3E）-1- [1（S）-1-（4-氟苯基）乙基] -3- [3-甲氧基-4-（4-甲基-1H-咪唑-1-基）亚苄基] （1）表示，具有Abeta生产抑制活性。 无定形物具有这样令人满意的性质，其具有优异的溶解性，稳定性，不容易变成结晶形式，并且具有低吸湿性。 因此适用于药物制剂。

    Amorphous object of cinnamide compound
    2.
    发明授权
    Amorphous object of cinnamide compound 失效
    肉桂酰胺化合物的无定形物

    公开(公告)号：US07923563B2

    公开(公告)日：2011-04-12

    申请号：US11663550

    申请日：2005-10-25

    申请人： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    发明人： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    IPC分类号： C07D401/06

    CPC分类号： C07D401/10

    摘要： An amorphous object of (3E)-1-[l(s)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4methyl-1H-imidazol-1-yl)benzylidene]piperidine-2-one, which is represented by the formula (1) and has Aβ-production inhibitory activity. The amorphous object has such satisfactory properties that it has excellent solubility, is stable, does not readily become a crystalline form, and has low hygroscopicity. It is hence suitable for use in pharmaceutical preparations.

    摘要翻译： （3E）-1- [1（S）-1-（4-氟苯基）乙基] -3- [3-甲氧基-4-（4-甲基-1H-咪唑-1-基）亚苄基] （1）表示并具有生产抑制活性。 无定形物具有这样令人满意的性质，其具有优异的溶解性，稳定性，不容易变成结晶形式，并且具有低吸湿性。 因此适用于药物制剂。

    SALTS OF CYNNAMIDE COMPOUND OR SOLVATES THEREOF
    3.
    发明申请
    SALTS OF CYNNAMIDE COMPOUND OR SOLVATES THEREOF 审中-公开
    氰化合物或其溶剂的盐

    公开(公告)号：US20090048448A1

    公开(公告)日：2009-02-19

    申请号：US12093929

    申请日：2006-11-17

    申请人： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito ,  Taiju Nakamura

    发明人： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito ,  Taiju Nakamura

    IPC分类号： C07D401/10

    CPC分类号： C07D401/10

    摘要： The invention provides crystals of dihydrochloride monohydrate of the compound of the following formula having an Aβ production inhibiting effect which crystals are characterized by exhibiting a diffraction peak at an angle of diffraction (2θ±0.2°) of 10.9° in powder X-ray diffractometry. Further, the invention also provides the compound in the form of various salts, crystal forms and amorphous forms which are suitable for the development of drugs.

    摘要翻译： 本发明提供下式化合物的二盐酸盐一水合物晶体，其具有抑制Aβ生成的作用，其结晶的特征在​​于在粉末X射线衍射中以衍射角（2θ±0.2°）为10.9°的衍射峰。 此外，本发明还提供了适合于开发药物的各种盐，晶型和无定形形式的化合物。

    Crystalline 1H-imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate and its pharmaceutical uses
    7.
    发明授权
    Crystalline 1H-imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate and its pharmaceutical uses 失效
    结晶的1H-咪唑并[4,5-b]吡啶-5-胺，7- [5 - [（环己基甲基氨基） - 甲基] -1H-吲哚-2-基] -2-甲基硫酸盐（1:1） 三水合物及其制药用途

    公开(公告)号：US07655800B2

    公开(公告)日：2010-02-02

    申请号：US11344534

    申请日：2006-02-01

    申请人： Charles E. Chase ,  Ikuo Kushida

    发明人： Charles E. Chase ,  Ikuo Kushida

    IPC分类号： C07D471/04 ,  A61K31/437

    CPC分类号： C07D471/04

    摘要： The invention relates to crystalline 1H-Imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate, E6070, its method of preparation, and its therapeutic uses. Pharmaceutical compositions containing crystalline E6070 and a pharmaceutically acceptable carrier represent one embodiment of the invention. The invention also relates to methods for treating an inflammatory disorder, an autoimmune disorder, or a proliferative disorder comprising the step of administering to a patient in need thereof a therapeutically effective amount of crystalline E6070.

    摘要翻译： 本发明涉及结晶1H-咪唑并[4,5-b]吡啶-5-胺，7- [5 - [（环己基甲基氨基）甲基] -1H-吲哚-2-基] -2-甲基硫酸盐（1 ：1），三水合物，E6070，其制备方法及其治疗用途。 含有结晶E6070和药学上可接受的载体的药物组合物代表本发明的一个实施方案。 本发明还涉及用于治疗炎症性疾病，自身免疫性疾病或增殖性疾病的方法，包括向有需要的患者施用治疗有效量的结晶E6070的步骤。

    CRYSTALLINE CINNAMIDE COMPOUNDS OR SALTS THEREOF
    8.
    发明申请
    CRYSTALLINE CINNAMIDE COMPOUNDS OR SALTS THEREOF 审中-公开
    晶体结构化合物或其盐

    公开(公告)号：US20100317860A1

    公开(公告)日：2010-12-16

    申请号：US12864794

    申请日：2009-01-26

    申请人： Ikuo Kushida ,  Nobuaki Sato ,  Yoshiaki Sato

    发明人： Ikuo Kushida ,  Nobuaki Sato ,  Yoshiaki Sato

    IPC分类号： C07F9/6506

    CPC分类号： C07F9/65583 ,  C07C57/145 ,  C07C57/15

    摘要： Disclosed are crystals of the compound represented by Formula (1), which has A□-production-reducing effects and is a prodrug of compounds effective in treating neural degenerative diseases of which A□ is the cause, for example, diseases such as Alzheimer's disease, Down syndrome, etc., and salts thereof or crystals of salts thereof. These are particularly useful as stock for pharmaceutical products.

    摘要翻译： 公开了由式（1）表示的化合物的晶体，其具有Aβ产生减少作用，并且是有效治疗其中A□的神经变性疾病的化合物的前药，例如阿尔茨海默氏病 ，唐氏综合征等，及其盐或其盐的晶体。 这些作为药品的库存特别有用。

    Salt of tetrahydrotriazolopyridine derivative and crystal thereof
    9.
    发明授权
    Salt of tetrahydrotriazolopyridine derivative and crystal thereof 有权
    四氢三唑并吡啶衍生物的盐及其结晶

    公开(公告)号：US08703954B2

    公开(公告)日：2014-04-22

    申请号：US13143130

    申请日：2010-02-24

    申请人： Takuma Minamisono ,  Noritaka Kitazawa ,  Ikuo Kushida

    发明人： Takuma Minamisono ,  Noritaka Kitazawa ,  Ikuo Kushida

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention provides a crystal of a 1.5 D-tartrate of a compound represented by the formula (1) having an A production inhibitory effect, characterized in that the crystal has a diffraction peak at a diffraction angle (20.2) of 23.2 in powder X-ray diffractometry; a crystal of a disulfate of the compound of the formula (1), characterized in that the crystal has a diffraction peak at a diffraction angle (20.2) of 17.1 in powder X-ray diffractometry; various other salts of the compound of the formula (1); crystal polymorphs of these salts; and the like, which are expected to be used as drug substances.

    摘要翻译： 本发明提供具有A生成抑制作用的式（1）表示的化合物的1.5酒石酸盐的晶体，其特征在于，所述晶体在粉末X中的衍射角（20.2）为23.2°的衍射峰 射线衍射; 式（1）化合物的二硫酸盐的结晶，其特征在于，在粉末X射线衍射中，晶体具有衍射角（20.2）为17.1°的衍射峰; 式（1）化合物的各种其它盐; 这些盐的晶体多晶型物; 等等，其预期用作药物物质。