Condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same
    2.
    发明授权
    Condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same 有权
    缩合吡啶或稠合嘧啶衍生物,以及包含其的药剂

    公开(公告)号:US08765771B2

    公开(公告)日:2014-07-01

    申请号:US13806940

    申请日:2011-06-24

    IPC分类号: A61K31/519 C07D491/00

    摘要: The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic β cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, andthe compound represented by the following formula (1): wherein one of A and B represents a nitrogen atom and the other represents a nitrogen atom or CR10, X represents an oxygen atom, a sulfur atom or —(CH2)n-N(R12)—, Y represents an oxygen atom, a sulfur atom or —N(R13)—, and R1 to R9 each represent a hydrogen atom or another substituent, or a salt thereof, or a solvate of the compound or the salt.

    摘要翻译: 本发明涉及提供一种具有促进胰腺胰岛素分泌活性的新型化合物, 细胞,因此可用作由高血糖引起的疾病如糖尿病的预防和/或治疗剂,以及由下式(1)表示的化合物:其中A和B之一表示氮原子,另一个表示 氮原子或CR 10,X表示氧原子,硫原子或 - (CH 2)n N(R 12) - ,Y表示氧原子,硫原子或-N(R 13) - ,R 1〜 原子或其它取代基,或其盐,或化合物或其盐的溶剂化物。

    External liquid preparation containing indomethacin
    3.
    发明授权
    External liquid preparation containing indomethacin 失效
    含吲哚美辛的外用液体制剂

    公开(公告)号:US08673960B2

    公开(公告)日:2014-03-18

    申请号:US12067722

    申请日:2006-10-16

    IPC分类号: A61K31/405

    摘要: The present invention provides an indomethacin-containing external liquid preparation which provides good feeling of use, which exhibits high percutaneous absorption of indomethacin, and which, particularly in a low-temperature environment, does not cause precipitation of crystals with time.The present invention is drawn to an external liquid preparation containing indomethacin, a lower alcohol, water, a sulfite, and polyethylene glycol having an average molecular weight of 3,000 to 15,000.

    摘要翻译: 本发明提供了含有吲哚美辛的外用液体制剂,其具有良好的使用感,其表现出高消耗吲哚美辛的经皮吸收,特别是在低温环境下,不会随时间引起晶体沉淀。 本发明涉及含有平均分子量为3,000〜15,000的吲哚美辛,低级醇,水,亚硫酸盐和聚乙二醇的外用液体制剂。

    AGENT FOR INHIBITING EXPRESSION OF LIPID METABOLISM RELATED MRNA

    公开(公告)号:US20130225618A1

    公开(公告)日:2013-08-29

    申请号:US13824782

    申请日:2011-10-03

    IPC分类号: A61K31/505

    CPC分类号: A61K31/505 C07D239/47

    摘要: The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solvate of any of them as an active ingredient: wherein the symbols are the same as those given in the description.

    Iontophoresis preparation for treating breast cancer and/or mastitis
    5.
    发明授权
    Iontophoresis preparation for treating breast cancer and/or mastitis 失效
    用于治疗乳腺癌和/或乳腺炎的离子电渗疗法

    公开(公告)号:US08442629B2

    公开(公告)日:2013-05-14

    申请号:US12988047

    申请日:2009-04-17

    IPC分类号: A61N1/30 A61K33/00

    摘要: Provided is to enhance the therapeutic effect of an iontophoretic preparation for treatment of breast cancer or mastitis.An iontophoretic preparation for treatment of breast cancer and/or mastitis containing, as an active ingredient, a nonsteroidal anti-inflammatory analgesic agent and/or an anticancer agent, wherein an electrolyte is topically administered through the nipple part into the mammary gland; subsequently, a donor is applied to the nipple part; and the active ingredient is topically administered through the nipple part into the mammary gland by application of current.

    摘要翻译: 提供用于治疗乳腺癌或乳腺炎的离子电渗疗法的治疗效果。 一种用于治疗乳腺癌和/或乳腺炎的离子电渗疗法制剂,其包含作为活性成分的非甾体抗炎止痛剂和/或抗癌剂,其中电解质通过乳头部分局部施用到乳腺中; 随后,将供体施加到乳头部分; 并且活性成分通过施加电流通过乳头部分局部施用到乳腺中。

    Iontophoretic preparation for treatment of breast cancer and/or mastitis
    6.
    发明授权
    Iontophoretic preparation for treatment of breast cancer and/or mastitis 失效
    用于治疗乳腺癌和/或乳腺炎的离子电渗疗法

    公开(公告)号:US08362027B2

    公开(公告)日:2013-01-29

    申请号:US13204803

    申请日:2011-08-08

    摘要: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.

    摘要翻译: 本发明提供通过局部施用非甾体抗炎止痛剂和/或抗癌剂并使其有效地进入乳腺来治疗乳腺癌和/或乳腺炎的方法。 本发明提供了一种用于治疗乳腺癌和/或乳腺炎的离子电渗疗法,其包含非甾体抗炎止痛剂和/或抗癌剂作为活性成分,并且具有施用于乳头部分的供体,用于局部施用 通过施加电位从乳头部分到乳腺的活性成分。

    Process for production of 4-fluoroisoquinoline-5-sulfonyl halide or salt thereof
    8.
    发明授权
    Process for production of 4-fluoroisoquinoline-5-sulfonyl halide or salt thereof 有权
    4-氟异喹啉-5-磺酰卤或其盐的制备方法

    公开(公告)号:US07872136B2

    公开(公告)日:2011-01-18

    申请号:US11816377

    申请日:2006-02-23

    IPC分类号: C07D217/22

    CPC分类号: C07D217/22

    摘要: To provide an effective and simple process for producing 4-fluoroisoquinoline-5-sulfonylhalide or a salt thereof, and a simple method for separating for purification of the product from a by-produced position isomer thereof. The process for producing 4-fluoroisoquinoline-5-sulfonyl halide or a salt thereof, characterized in that the process includes reacting 4-fluoroisoquinoline or a salt thereof with sulfuric anhydride in the presence or absence of sulfuric acid, to thereby form 4-fluoroisoquinoline-5-sulfonic acid or a salt thereof, and, subsequently, reacting the formed sulfonic acid compound with a halogenating reagent.

    摘要翻译: 提供生产4-氟异喹啉-5-磺酰卤或其盐的有效和简单的方法,以及用于从副产物位置异构体纯化产物的简单方法。 制备4-氟异喹啉-5-磺酰卤或其盐的方法,其特征在于该方法包括在硫酸存在或不存在下使4-氟异喹啉或其盐与硫酸酐反应,由此形成4-氟异喹啉 - 然后使所形成的磺酸化合物与卤化试剂反应。

    Process for production of optically active PPAR-activating compound and intermediate of the same
    10.
    发明授权
    Process for production of optically active PPAR-activating compound and intermediate of the same 有权
    光学活性PPAR活化化合物及其中间体的制备方法

    公开(公告)号:US07790903B2

    公开(公告)日:2010-09-07

    申请号:US11816472

    申请日:2006-02-23

    IPC分类号: C07D263/58

    CPC分类号: C07D263/58

    摘要: A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided.A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.

    摘要翻译: 提供了以高产率和高光学收率获得化合物(1)及其中间体的方法。 一种制备化合物(4)的方法,该方法包括在碱的存在下使化合物(2)与化合物(3)反应; 和化合物(1)的制造方法,其特征在于,在碱的存在下使化合物(2)与化合物(3)反应,得到化合物(4),然后使化合物(4)脱酯化。 其中R表示碳原子数1〜6的烷基或碳原子数7〜8的芳烷基。