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    TRICYCLIC HETEROCYCLE COMPOUNDS
    13.
    发明申请
    TRICYCLIC HETEROCYCLE COMPOUNDS 有权
    三聚异构体化合物

    公开(公告)号：US20150246930A1

    公开(公告)日：2015-09-03

    申请号：US14429923

    申请日：2013-09-20

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： Weifang Shan ,  Ashvinikumar V. Gavai ,  James Aaron Balog

    IPC: C07D498/04 ,  A61K45/06 ,  C07D487/04 ,  A61K31/553 ,  A61K31/5513

    CPC classification number: C07D498/04 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/555 ,  A61K31/573 ,  A61K45/06 ,  C07D487/04 ,  C07D487/06 ,  C07D498/06 ,  A61K2300/00

    Abstract: Disclosed are compounds of Formula (I), wherein: X is O or —NR3; R1 is —CH2CH2CH3, —CH2CF3, —CH2CH2CF3, —CH2CF2CH3, —CH2CH2CH2CF3, —CH2CH2CF2CH3, —CH2CH(CH3)CF3, —CH2CH2CH2F, or CH2(cyclopropyl); R2 is —CH2CH2CH3, —CH2CF3, —CH2CH2CF3, —CH2CF2CH3, —CH2CH2CH2CF3, —CH2CH2CH2F, —CH2CH(CH3)CF3, CH2CH2CF2CH3, —CH2(cyclopropyl), —CH(CH3)(cyclopropyl), phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, pyridinyl, formula (i), formula (ii), formula (iii), formula (iv) or formula (v); Ring A is phenyl or pyridinyl; and R3, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

    Abstract translation: 公开了式（I）的化合物，其中：X是O或-NR 3; R1是-CH2CH2CH3，-CH2CF3，-CH2CH2CF3，-CH2CF2CH3，-CH2CH2CH2CF3，-CH2CH2CF2CH3，-CH2CH（CH3）CF3，-CH2CH2CH2F或CH2（环丙基）; R2是-CH2CH2CH3，-CH2CF3，-CH2CH2CF3，-CH2CF2CH3，-CH2CH2CH2CF3，-CH2CH2CH2F，-CH2CH（CH3）CF3，CH2CH2CF2CH3，-CH2（环丙基），-CH（CH3）（环丙基），苯基，氟苯基，氯苯基， 三氟苯基，甲基异恶唑基，吡啶基，式（ⅰ），式（ⅱ），式（ⅲ），式（ⅳ）或式（Ⅴ）; 环A是苯基或吡啶基; 并且R 3，R a，R b，R c，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。

    Tricyclic heterocycle compounds
    18.
    发明授权
    Tricyclic heterocycle compounds 有权
    三环杂环化合物

    公开(公告)号：US09249157B2

    公开(公告)日：2016-02-02

    申请号：US14429923

    申请日：2013-09-20

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： Weifang Shan ,  Ashvinikumar V. Gavai ,  James Aaron Balog

    IPC: C07D487/04 ,  C07D498/04 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/555 ,  A61K31/573 ,  A61K31/5513 ,  A61K31/553 ,  A61K45/06

    CPC classification number: C07D498/04 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/555 ,  A61K31/573 ,  A61K45/06 ,  C07D487/04 ,  C07D487/06 ,  C07D498/06 ,  A61K2300/00

    Abstract: Disclosed are compounds of Formula (I), wherein: X is O or —NR3; R1 is —CH2CH2CH3, —CH2CF3, —CH2CH2CF3, —CH2CF2CH3, —CH2CH2CH2CF3, —CH2CH2CF2CH3, —CH2CH(CH3)CF3, —CH2CH2CH2F, or CH2(cyclopropyl); R2 is —CH2CH2CH3, —CH2CF3, —CH2CH2CF3, —CH2CF2CH3, —CH2CH2CH2CF3, —CH2CH2CH2F, —CH2CH(CH3)CF3, CH2CH2CF2CH3, —CH2(cyclopropyl), —CH(CH3)(cyclopropyl), phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, pyridinyl, formula (i), formula (ii), formula (iii), formula (iv) or formula (v); Ring A is phenyl or pyridinyl; and R3, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

    Abstract translation: 公开了式（I）的化合物，其中：X是O或-NR 3; R1是-CH2CH2CH3，-CH2CF3，-CH2CH2CF3，-CH2CF2CH3，-CH2CH2CH2CF3，-CH2CH2CF2CH3，-CH2CH（CH3）CF3，-CH2CH2CH2F或CH2（环丙基）; （CH 2）2，CH 2 CH 2 CH 3，-CH 2（环丙基） 三氟苯基，甲基异恶唑基，吡啶基，式（ⅰ），式（ⅱ），式（ⅲ），式（ⅳ）或式（Ⅴ）; 环A是苯基或吡啶基; 并且R 3，R a，R b，R c，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。

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