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    Production and purification methods for efinaconazole
    1.
    发明授权
    Production and purification methods for efinaconazole 有权

    公开(公告)号：US10829475B2

    公开(公告)日：2020-11-10

    申请号：US16795275

    申请日：2020-02-19

    申请人： KAKEN PHARMACEUTICAL CO., LTD.

    发明人： Masahito Watanabe ,  Takeshi Kanayama

    IPC分类号： C07D401/06 ,  C07D487/10 ,  C07D401/14 ,  A61P31/10 ,  A61K31/4439

    摘要： The present invention provides efinaconazole producing and purifying methods adapted to industrial scale that provide high-purity efinaconazole in high yield by simple operations using specific impurities as indices. The efinaconazole producing method comprises:step A of forming a toluene solution comprising compound (II), compound (III), an inorganic base, and toluene in a volume (L) which is 2 to 5 times the mass (kg) of compound (II);step B of subjecting the toluene solution to reaction under heating;step C of washing the reaction mixture from step B to obtain a toluene solution of crude efinaconazole in which the residual amount of 4-MP is not more than 5 wt % of efinaconazole.

    NOVEL EP4 AGONIST
    4.
    发明申请
    NOVEL EP4 AGONIST 有权

    公开(公告)号：US20150018401A1

    公开(公告)日：2015-01-15

    申请号：US14498429

    申请日：2014-09-26

    申请人： Asahi Glass Company, Limited ,  Kaken Pharmaceutical Co., Ltd.

    发明人： Takahiko MURATA ,  Masahiro AMAKAWA ,  Shin TERADAIRA ,  Yasushi MATSUMURA ,  Katsuhiko KONISHI

    IPC分类号： C07D405/06

    CPC分类号： C07D405/06 ,  A61K31/41

    摘要： Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1-4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.

    摘要翻译： 本发明提供由式（1）表示的化合物：其中，R 1和R 2各自独立地为氢原子或碳数为1-3的直链烷基，R 3为氢原子，具有碳数的烷基 1-4，烷氧基烷基，芳基，卤原子或卤代烷基，或其药学上可接受的盐，其与已知的PGI 2类似物不同，具有选择性EP4激动剂作用，和含有该化合物的药物，其中 可用于预防和/或治疗免疫疾病，消化道疾病，心血管疾病，心脏病，呼吸系统疾病，神经系统疾病，眼科疾病，肾病，肝病，骨病，皮肤疾病等。

    AIRLESS CONTAINER
    6.
    发明申请
    AIRLESS CONTAINER 有权

    公开(公告)号：US20210291211A1

    公开(公告)日：2021-09-23

    申请号：US17264764

    申请日：2018-09-03

    申请人： KAKEN PHARMACEUTICAL CO., LTD. ,  KITANO CO., LTD.

    发明人： Katsunori SHIMAKURA ,  Masayoshi TAKAOKA ,  Tatsuro NAGAO

    IPC分类号： B05B11/00

    摘要： An airless container includes a cylindrical container body storing a contained material, which is a fluid, in an airtight state, and a pump attached to an upper edge portion of the container body and configured to externally discharge the contained material. The airless container further includes a bottom lid that closes a lower opening portion of a container bottom portion of the container body, and a piston in the container body between the pump and the bottom lid, which is slidable in the container body in an airtight state. The piston includes a flexible piece that is deformable in a portion that comes into contact with the bottom lid. The flexible piece is deformable against the sliding of the piston toward the bottom lid.

    PRODUCTION AND PURIFICATION METHODS FOR EFINACONAZOLE
    7.
    发明申请
    PRODUCTION AND PURIFICATION METHODS FOR EFINACONAZOLE 审中-公开

    公开(公告)号：US20190292166A1

    公开(公告)日：2019-09-26

    申请号：US16438011

    申请日：2019-06-11

    申请人： KAKEN PHARMACEUTICAL CO., LTD.

    发明人： Masahito WATANABE ,  Takeshi KANAYAMA

    IPC分类号： C07D401/06

    摘要： The present invention provides efinaconazole producing and purifying methods adapted to industrial scale that provide high-purity efinaconazole in high yield by simple operations using specific impurities as indices. The efinaconazole producing method comprises: step A of forming a toluene solution comprising compound (II), compound (III), an inorganic base, and toluene in a volume (L) which is 2 to 5 times the mass (kg) of compound (II); step B of subjecting the toluene solution to reaction under heating; step C of washing the reaction mixture from step B to obtain a toluene solution of crude efinaconazole in which the residual amount of 4-MP is not more than 5 wt % of efinaconazole.