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    METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS
    3.
    发明申请
    METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS 审中-公开

    公开(公告)号：US20190300561A1

    公开(公告)日：2019-10-03

    申请号：US16356198

    申请日：2019-03-18

    Applicant: Epizyme, Inc.

    Inventor： Edward J. OLHAVA

    IPC: C07H19/16 ,  C07D235/12 ,  A61K31/4184 ,  A61K31/7076

    Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT 1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

    METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS
    6.
    发明公开
    METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS 审中-公开

    公开(公告)号：US20230287033A1

    公开(公告)日：2023-09-14

    申请号：US18081347

    申请日：2022-12-14

    Applicant: Epizyme, Inc.

    Inventor： Edward J. OLHAVA

    IPC: C07H19/16 ,  A61K31/7076 ,  A61K31/4184 ,  C07D235/12

    CPC classification number: C07H19/16 ,  A61K31/7076 ,  A61K31/4184 ,  C07D235/12 ,  C07H19/06

    Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

    METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS
    9.
    发明申请
    METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS 有权

    公开(公告)号：US20210230210A1

    公开(公告)日：2021-07-29

    申请号：US17025508

    申请日：2020-09-18

    Applicant: Epizyme, Inc.

    Inventor： Edward J. OLHAVA

    IPC: C07H19/16 ,  A61K31/7076 ,  A61K31/4184 ,  C07D235/12

    Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

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