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

    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。

    SALT OF TETRAHYDROTRIAZOLOPYRIDINE DERIVATIVE AND CRYSTAL THEREOF
    4.
    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

    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 CINNAMIDE COMPOUNDS OR SALTS THEREOF
    5.
    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

    IPC分类号: C07F9/6506

    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。

    Amorphous object of cinnamide compound
    6.
    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

    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
    7.
    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

    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
    8.
    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

    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
    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

    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。