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    STABLE PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION
    1.
    发明申请
    STABLE PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION 有权

    公开(公告)号：US20230129146A1

    公开(公告)日：2023-04-27

    申请号：US18085842

    申请日：2022-12-21

    申请人： ASTELLAS PHARMA INC.

    发明人： Masakazu MIYAZAKI ,  Ryohei ISHIBA ,  Yuki TAKAISHI ,  Fumiaki UEJO

    IPC分类号： A61K31/497 ,  A61K47/26 ,  A61K47/10 ,  A61K9/20

    摘要： Provided is a stable pharmaceutical composition for oral administration comprising 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide (hereinafter referred to as compound A) or a pharmaceutically acceptable salt thereof, wherein the generation of related substances during storage is inhibited. In the stable pharmaceutical composition for oral administration, the proportion of crystals of compound A or a pharmaceutically acceptable salt thereof is 60% or more with respect to the total amount of compound A or a pharmaceutically acceptable salt thereof.

    Granular Pharmaceutical Composition
    2.
    发明申请
    Granular Pharmaceutical Composition 有权

    公开(公告)号：US20230113303A1

    公开(公告)日：2023-04-13

    申请号：US18063216

    申请日：2022-12-08

    申请人： Astellas Pharma, Inc.

    发明人： Mare Nishiura ,  Kenichi Ashihara ,  Kanehira Imai ,  Atsushi Muro ,  Tsukasa Nishikawahara

    IPC分类号： A61K38/10 ,  A61K9/16 ,  A61K9/20 ,  A61K9/50 ,  A61K38/12

    摘要： The present invention relates to a granular pharmaceutical composition obtained by coating a nucleus with: (1) a layer containing a material having a damp-proofing function, and (2) a drug layer containing linaclotide, a pharmaceutically acceptable salt, or a hydrate thereof, and (3) a layer containing a material having a damp-proofing function. Also, the present invention relates to a method for manufacturing the granular pharmaceutical composition obtained by coating the nucleus with (1) the layer containing the material having a damp-proofing function, (2) the drug layer containing the linaclotide, the pharmaceutically acceptable salt, or the hydrate thereof, and (3) the layer containing the material having a damp-proofing function.

    FATTY ACID DERIVATIVE LABELED WITH POSITRON-EMITTING RADIONUCLIDE
    3.
    发明申请
    FATTY ACID DERIVATIVE LABELED WITH POSITRON-EMITTING RADIONUCLIDE 有权

    公开(公告)号：US20230065079A1

    公开(公告)日：2023-03-02

    申请号：US17793091

    申请日：2021-01-15

    申请人： ASTELLAS PHARMA INC.

    发明人： Yoshihiro Murakami ,  Hiroshi Fushiki ,  Koichi Yonezawa

    IPC分类号： A61K51/04 ,  C07C319/20 ,  C07C323/52 ,  C07C323/53 ,  C07C323/54 ,  G01T1/161

    摘要： [Problem] To provide a labeled fatty acid derivative for diagnostic imaging that enables the quantification of myocardial fatty acid metabolic activity. [Solution] The inventors, engaging in diligent research into methods that enable the quantification of fatty acid metabolic activity, discovered that a labeled fatty acid derivative represented by formula (1), in which [18F] has been substituted at a specific position of a long-chain carboxylic acid compound containing a sulfur atom, or a salt thereof, has good accumulation in the myocardium, and enables imaging of fatty acid metabolic activity via positron emission tomography (PET). Therefore, the labeled fatty acid derivative according to the present invention can be used as a radiotracer for swift and noninvasive quantification of myocardial fatty acid metabolic activity, diagnostic imaging of heart diseases such as ischemic heart disease, diagnostic imaging of the therapeutic effects yielded by a heart disease therapeutic agent, and so forth.

    CRYSTAL OF INDOCYANINE COMPOUND
    4.
    发明申请
    CRYSTAL OF INDOCYANINE COMPOUND 有权

    公开(公告)号：US20230020197A1

    公开(公告)日：2023-01-19

    申请号：US17780138

    申请日：2020-11-25

    申请人： ASTELLAS PHARMA INC.

    发明人： Hiroyuki Yamashita ,  Kouji Yamazaki

    IPC分类号： C09B23/01 ,  C09B67/48

    摘要： The present invention is a crystal of 3-(3-{[3-(cyclomaltoheptaos-21-O-yl)propyl]amino}-3-oxopropyl)-2-{(1E)-2-[(3E)-3-{(2E)-2-[3-(3-{[3-(cyclomaltoheptaos-21-O-yl)propyl]amino}-3-oxopropyl)-1,1-dimethyl-1,3-dihydro-2H-benzo[e]indo1-2-ylidene]ethylidene}-2-methoxycyclohex-1-en-1-yl]ethen-1-yl}-1,1-dimethyl-1H-benzo [e]indol-3-ium chloride.

    METHOD FOR PRODUCING NANOPARTICLE HAVING METAL PARTICLE WHICH CONTAINS IRON OXIDE TO WHICH ONE OR MORE HYDROPHILIC LIGANDS ARE COORDINATION BONDED
    9.
    发明申请
    METHOD FOR PRODUCING NANOPARTICLE HAVING METAL PARTICLE WHICH CONTAINS IRON OXIDE TO WHICH ONE OR MORE HYDROPHILIC LIGANDS ARE COORDINATION BONDED 有权

    公开(公告)号：US20220089455A1

    公开(公告)日：2022-03-24

    申请号：US17418704

    申请日：2019-12-27

    申请人： ASTELLAS PHARMA INC.

    发明人： Takashi KIKUCHI ,  Tsuyoshi MIZUTANI ,  Hiroki TOYA ,  Akio KURODA ,  Yota GOTO ,  Shun HIRASAWA ,  Toshiyuki SUGIMORI

    IPC分类号： C01G49/06 ,  A61K49/18 ,  C01G49/08

    摘要： [Problem]
    A novel method for producing a nanoparticle having a metal particle which contains iron oxide to which one or more hydrophilic ligands are coordination bonded is provided, where the nanoparticle is useful as a contrast agent for magnetic resonance imaging.
    [Means for Solution]
    As the novel method for producing a nanoparticle having a metal particle which contains iron oxide to which one or more hydrophilic ligands are coordination bonded, by performing ligand exchange to a hydrophilic ligand from an iron oxide nanoparticle having a surface to which a hydrophobic ligand is coordination bonded in one step using a phase transfer catalyst, it is possible to expect shortening of production processes and reduction of hydrophilic ligands used.
    Furthermore, by producing an iron oxide nanoparticle having a surface to which a hydrophobic ligand is coordination bonded using a dropwise addition method, it is possible to avoid a rapid temperature rise and a reaction at a high temperature of 200° C. or higher, which is more advantageous for industrial production.