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    Fused ring compounds and use thereof
    222.
    发明授权
    Fused ring compounds and use thereof 失效
    稠环化合物及其用途

    公开(公告)号：US08673942B2

    公开(公告)日：2014-03-18

    申请号：US12936785

    申请日：2009-04-09

    Applicant: Tsuneo Yasuma ,  Nobuyuki Takakura

    Inventor： Tsuneo Yasuma ,  Nobuyuki Takakura

    IPC: A61K31/4436 ,  C07D417/14

    CPC classification number: C07D417/04 ,  C07D417/14

    Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.

    Abstract translation: 本发明的目的在于提供一种用作预防或治疗糖尿病，肥胖症等药物的药剂的葡糖激酶活化剂。 本发明提供含有式（I）表示的化合物的葡糖激酶活化剂：其中每个符号在说明书中定义，或其盐或其前药。

    PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES
    224.
    发明申请
    PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES 审中-公开
    生产光学活性胺衍生物的方法

    公开(公告)号：US20140066499A1

    公开(公告)日：2014-03-06

    申请号：US14079607

    申请日：2013-11-13

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Shinichi Urayama ,  Eigo Mutou ,  Atsushi Inagaki ,  Takashi Okada ,  Shigeharu Sugisaki

    IPC: C07D307/77

    CPC classification number: C07D307/77 ,  A61K31/343 ,  C07D307/80 ,  C07D307/81

    Abstract: An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture.

    Abstract translation: 一种以高产率生产高纯度光学活性胺衍生物同时抑制副产物形成的工业方法，其包括使（E）-2-（1,6,7,8-四氢-2H-茚并[5 ，4-b]呋喃-8-亚基）乙胺进行不对称还原，在40〜100℃的反应温度和3〜9的pH下催化还原得到的（S）-2-（ 1,6,7,8-四氢-2H-茚并[5,4-b]呋喃-8-基）乙胺进行丙酰化，然后使反应混合物结晶。

    ORGAN-SPECIFIC GENE, METHOD FOR IDENTIFYING THE SAME AND USE THEREOF
    226.
    发明申请
    ORGAN-SPECIFIC GENE, METHOD FOR IDENTIFYING THE SAME AND USE THEREOF 审中-公开
    有机基因，鉴别及其用途的方法

    公开(公告)号：US20140046047A1

    公开(公告)日：2014-02-13

    申请号：US13951897

    申请日：2013-07-26

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： Saku MIYAMOTO ,  Kenji TAKAMI ,  Akira HORINOUCHI

    IPC: C12Q1/68

    CPC classification number: C12Q1/6876 ,  C12Q1/6881 ,  C12Q2600/158 ,  G16B25/00

    Abstract: The present invention provides a method of extracting an organ- or tissue-specific highly expressed gene, including: (1) a step for measuring expression level of a specified gene group for each organ or tissue in 2 or more individuals, (2) a step for acquiring (a) a minimum value of expression levels in a particular organ or tissue in all individuals, and (b) a maximum value of expression levels in other organs and tissues in all individuals, for each gene, and (3) a step for extracting the gene as a gene highly expressed specifically in the particular organ or tissue if the above-described (a)/(b) ratio is larger than 1. By the present invention, truly organ- or tissue-specific genes are extracted.

    Abstract translation: 本发明提供一种提取器官或组织特异性高表达基因的方法，包括：（1）测定2个以上个体中各器官或组织的特定基因组的表达水平的步骤，（2） 获得（a）所有个体的特定器官或组织中表达水平的最小值的步骤，和（b）每个基因的所有个体的其他器官和组织中的表达水平的最大值，和（3）a 如果上述（a）/（b）比大于1，则将该基因提取为特异性高度表达于特定器官或组织的基因的步骤。通过本发明，提取真正的器官或组织特异性基因 。

    PYRROLE COMPOUNDS
    227.
    发明申请
    PYRROLE COMPOUNDS 审中-公开
    吡咯化合物

    公开(公告)号：US20140031393A1

    公开(公告)日：2014-01-30

    申请号：US14043018

    申请日：2013-10-01

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

    IPC: A61K31/444

    CPC classification number: A61K31/444 ,  C07D401/14

    Abstract: The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.

    Abstract translation: 本发明涉及由下式表示的化合物：其中A是具有至少一个取代基的吡啶基，其中R 1，R 2和R 3各自为氢原子，卤素原子，任选被卤素取代的C 1-6烷基或 任选被卤素取代的C 1-6烷氧基，R 4和R 6各自为氢原子，卤素原子或任选被卤素取代的C 1-6烷基，R 5为氢原子，卤素原子，C 1-6烷基 任选被卤素取代或被卤素任意取代的C 1-6烷氧基，R 7是氢原子或任选被卤素或其盐取代的C 1-6烷基，或含有它们的药物组合物。

    POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS
    228.
    发明申请
    POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS 有权
    POLY（ADP-RIBOSE）聚合酶（PARP）抑制剂

    公开(公告)号：US20140024654A1

    公开(公告)日：2014-01-23

    申请号：US14030771

    申请日：2013-09-18

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Jason W. Brown ,  Anthony R. Gangloff ,  Andre K. Kiryanov

    IPC: C07D471/14

    CPC classification number: C07D471/14

    Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.

    Abstract translation: 提供下式的化合物用于PARP：其中变量如本文所定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物的方法。

    LAMINATED TABLET AND MANUFACTURING METHOD THEREFOR
    229.
    发明申请
    LAMINATED TABLET AND MANUFACTURING METHOD THEREFOR 有权
    层压板及其制造方法

    公开(公告)号：US20140023708A1

    公开(公告)日：2014-01-23

    申请号：US14002451

    申请日：2012-03-02

    Applicant: Kazuki Harada ,  Hikaru Fukuyama ,  Masahiko Koike

    Inventor： Kazuki Harada ,  Hikaru Fukuyama ,  Masahiko Koike

    IPC: A61K9/20

    CPC classification number: A61K9/2095 ,  A61K9/2072 ,  A61K9/2086 ,  A61K9/209 ,  A61K45/06

    Abstract: According to the present invention, a multilayer tablet showing suppressed layer separation and a production method thereof are provided. A concave portion having a depth of not less than 0.1 mm Ka is formed on at least one surface Sa of the both front and back surfaces (Sa, Sb) of a multilayer tablet. Particularly, a multilayer structure obtained by, in tableting, forming a convex portion for forming the concave portion on at least the upper punch, and preliminarily compressing all layers in the multilayer tablet with the upper punch to form a concave portion having the same shape with a depth of not less than 0.1 mm on the upper surface of all layers, wherein the powder materials of the next layer are protruding into the concave portion, is a preferable embodiment.

    Abstract translation: 根据本发明，提供了显示抑制层分离的多层片剂及其制备方法。 在多层片剂的前表面（Sa，Sb）的至少一个表面Sa上形成具有不小于0.1mm的深度的凹部的凹部。 特别是，通过在至少在上冲头上形成用于形成凹部的凸部的压片成型，并用上冲头预先压缩多层片剂中的所有层而形成具有相同形状的凹部而获得的多层结构， 在所有层的上表面上的深度不小于0.1mm，其中下一层的粉末材料突出到凹部中，是优选的实施方案。

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