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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

    Applicant: Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    Inventor： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    IPC: C07D401/10

    CPC classification number: C07D401/10

    Abstract: 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.

    Abstract translation: （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。

    Salt of tetrahydrotriazolopyridine derivative and crystal thereof
    3.
    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

    Applicant: Takuma Minamisono ,  Noritaka Kitazawa ,  Ikuo Kushida

    Inventor： Takuma Minamisono ,  Noritaka Kitazawa ,  Ikuo Kushida

    IPC: C07D471/04

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    SALT OF TETRAHYDROTRIAZOLOPYRIDINE DERIVATIVE AND CRYSTAL THEREOF
    6.
    发明申请
    SALT OF TETRAHYDROTRIAZOLOPYRIDINE DERIVATIVE AND CRYSTAL THEREOF 有权
    四氢呋喃并吡啶衍生物及其结晶的盐

    公开(公告)号：US20110275822A1

    公开(公告)日：2011-11-10

    申请号：US13143130

    申请日：2010-02-24

    Applicant: Takuma Minamisono ,  Noritaka Kitazawa ,  Ikuo Kushida

    Inventor： Takuma Minamisono ,  Noritaka Kitazawa ,  Ikuo Kushida

    IPC: C07D471/04

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 本发明提供具有A生成抑制效果的式（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。

    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.
    发明申请
    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：US20060194833A1

    公开(公告)日：2006-08-31

    申请号：US11344534

    申请日：2006-02-01

    Applicant: Charles Chase ,  Ikuo Kushida

    Inventor： Charles Chase ,  Ikuo Kushida

    IPC: C07D471/02 ,  A61K31/4745

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    Amorphous object of cinnamide compound
    9.
    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

    Applicant: Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    Inventor： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito

    IPC: C07D401/06

    CPC classification number: C07D401/10

    Abstract: 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.

    Abstract translation: （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。

    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
    10.
    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

    Applicant: Charles E. Chase ,  Ikuo Kushida

    Inventor： Charles E. Chase ,  Ikuo Kushida

    IPC: C07D471/04 ,  A61K31/437

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

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