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    Method for producing heterocyclic compound
    131.
    发明授权
    Method for producing heterocyclic compound 有权

    公开(公告)号：US10710989B2

    公开(公告)日：2020-07-14

    申请号：US16488770

    申请日：2018-02-27

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： Makoto Kanematsu ,  Kazuhisa Ishimoto ,  Tomoaki Katou

    IPC: C07D405/14 ,  C07D231/12 ,  C07D405/10

    Abstract: The present invention provides a method of producing a heterocyclic compound useful as an agent for the prophylaxis and/or treatment of Alzheimer's disease and the like. The present invention relates to a method of producing 1,5-anhydro-2,4-dideoxy-2-(4-fluoro-5-methyl-1-oxo-6-(4-(1H-pyrazol-1-yl)benzyl)-1,3-dihydro-2H-isoindol-2-yl)-L-threo-pentitol or a salt thereof, which comprises reacting 4-fluoro-3-hydroxy-5-methyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2-benzofuran-1(3H)-one or a salt thereof, 3-fluoro-2-formyl-4-methyl-5-[4-(1H-pyrazol-1-yl)benzyl]benzoic acid or a salt thereof, or a mixture thereof, with 2-amino-1,5-anhydro-2,4-dideoxy-L-threo-pentitol.

    Microneedle patch
    132.
    发明授权
    Microneedle patch 审中-公开

    公开(公告)号：US10668260B2

    公开(公告)日：2020-06-02

    申请号：US14774385

    申请日：2014-03-11

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： Yoshihiro Omachi ,  Yasuhiro Hiraishi ,  Masami Kusaka ,  Shigehiro Asano ,  Masao Nagao

    IPC: A61M37/00 ,  A61K9/00 ,  A61K9/70 ,  B29C45/00 ,  B29C45/16 ,  B29K101/12 ,  B29L9/00 ,  B29L31/00

    Abstract: The present invention provides a microneedle patch which can solve the problem that microneedle production is difficult and requires high accuracy, the problem that time and mental burdens on a health professional and a patient are large, and the problem caused by compounding a plurality of drugs. The microneedle patch comprises a large number of drug-carrying microprojections 4 erected on one support sheet, each microprojection 4 having a drug layer 5 soluble in vivo at its top part and having an intermediate layer 6 under the drug layer 5, the intermediate layer 6 containing a polymeric substance for adhesion of the drug layer 5 to the support sheet, the drug layer 5 at the top part of the microprojection 4 containing a single drug, the microprojections 4 holding difference types of drugs being arranged together on the support sheet 2.

    Method for producing sulfonyl chloride compound
    139.
    发明授权
    Method for producing sulfonyl chloride compound 有权

    公开(公告)号：US10370357B2

    公开(公告)日：2019-08-06

    申请号：US15899055

    申请日：2018-02-19

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： Keisuke Majima

    IPC: C07D401/12 ,  C07D213/71 ,  A61K9/28 ,  A61K9/20

    Abstract: An object of the present invention is to provide a production method of an intermediate used in the production method of a sulfonylpyrrole compound useful as a pharmaceutical product. The present invention relates to a method of producing sulfonylpyrrole compound (VI) by reacting a pyridine-3-sulfonic acid compound with phosphorus pentachloride in a solvent of chlorobenzene or trifluoromethylbenzene to give a pyridine-3-sulfonyl chloride compound, reacting the compound without isolation with compound (III) to give compound (IV), and subjecting the compound (IV) to a reductive amination reaction. wherein R2 is a hydrocarbon group etc. and R3 and R4 are each a hydrogen atom etc., wherein R2 is an optionally substituted pyridin-3-yl group, and the other symbols are as defined above, wherein R5 is an alkyl group and the other symbols are as defined above.

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