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    BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS
    2.
    发明申请
    BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS 有权
    双氟烷基-1,4-苯并嗪酮化合物

    公开(公告)号：US20140100365A1

    公开(公告)日：2014-04-10

    申请号：US14100896

    申请日：2013-12-09

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： Ashvinikumar V. Gavai ,  Claude A. Quesnelle ,  Soong-Hoon Kim ,  Francis Y. Lee

    IPC: C07D243/24

    CPC classification number: C07D243/24 ,  A61K31/138 ,  A61K31/337 ,  A61K31/5513 ,  A61K31/555 ,  A61K31/573 ,  A61K45/06 ,  A61K2300/00

    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. 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）的化合物或其前药; 其中：R1是-CH2CF3或-CH2CH2CF3; R2是-CH2CF3，-CH2CH2CF3或-CH2CH2CH2CF3; R3是H或-CH3; 每个R a独立地为F，Cl，-CN，-OCH 3和/或-NHCH 2 CH 2 OCH 3; 并且z为零，1或2.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。

    Combination therapy for the treatment of proliferative diseases
    5.
    发明授权
    Combination therapy for the treatment of proliferative diseases 有权
    用于治疗增殖性疾病的联合疗法

    公开(公告)号：US09492469B2

    公开(公告)日：2016-11-15

    申请号：US14782235

    申请日：2014-04-04

    Applicant: Bristol-Myers Squibb Company

    Inventor： Francis Y. Lee

    IPC: A01N43/04 ,  A61K31/70 ,  A61K31/7068 ,  A61K31/5513 ,  A61K31/7064 ,  A61K31/706

    CPC classification number: A61K31/7068 ,  A61K31/5513 ,  A61K31/706 ,  A61K31/7064 ,  A61K2300/00

    Abstract: A method of treating a proliferative disease, such as cancer, is disclosed. The method comprises administering to a mammal in need thereof synergistically therapeutically effective amounts of: (i) (2R,3S)—N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-di-hydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide; (ii) 2-deoxy-2,2-difluorocytidine monohydrochloride (beta-isomer); and (iii) optionally, one or more additional anticancer agents.

    Abstract translation: 公开了治疗增殖性疾病如癌症的方法。 该方法包括向有需要的哺乳动物施用协同治疗有效量的：（i）（2R，3S）-N - （（3S）-1-甲基-2-氧代-5-苯基-2,3-二 - 氢-3H-1,4-苯并二氮杂-3-基）-2,3-双（3,3,3-三氟丙基）琥珀酰胺; （ii）2-脱氧-2,2-二氟胞苷一盐酸盐（β-异构体）; 和（iii）任选的一种或多种另外的抗癌剂。

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