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    TRIAZOLOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF
    2.
    发明申请
    TRIAZOLOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开

    公开(公告)号：US20190337946A1

    公开(公告)日：2019-11-07

    申请号：US16515253

    申请日：2019-07-18

    Applicant: Genentech, Inc.

    Inventor： Simon Charles Goodacre ,  Nicholas Charles Ray ,  Mark Edward Zak ,  Yun-Xing Cheng ,  Wei Li

    IPC: C07D471/04 ,  C07D471/10

    Abstract: Triazolopyridine compounds that are inhibitors of JAK kinase, such as JAK1, compositions containing these compounds and methods for treating diseases mediated by a JAK kinase. In particular, provided are compounds of formula (I), stereoisomers, tautomers, solvates, prodrugs or pharmaceutically acceptable salts thereof, where R1a, R1b, R1c, R2, R3, R4 and R5 are defined herein, pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, for example, for treating a disease or condition mediated by a JAK kinase in a patient.

    TRIAZOLOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF
    7.
    发明申请
    TRIAZOLOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开

    公开(公告)号：US20180327402A1

    公开(公告)日：2018-11-15

    申请号：US15975462

    申请日：2018-05-09

    Applicant: Genentech, Inc.

    Inventor： Simon Charles Goodacre ,  Nicholas Charles Ray ,  Mark Edward Zak ,  Yun-Xing Cheng ,  Wei Li

    IPC: C07D471/04 ,  C07D471/10

    CPC classification number: C07D471/04 ,  C07D471/10

    Abstract: Provided are triazolopyridine compounds that are inhibitors of JAK kinase, such as JAK1, compositions containing these compounds and methods for treating diseases mediated by a JAK kinase. In particular, provided are compounds of formula (I), stereoisomers, tautomers, solvates, prodrugs or pharmaceutically acceptable salts thereof, where R1a, R1b, R1c, R2, R3, R4 and R5 are defined herein, pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, for example, for treating a disease or condition mediated by a JAK kinase in a patient.

    DIAZACARBAZOLES AND METHODS OF USE
    9.
    发明申请
    DIAZACARBAZOLES AND METHODS OF USE 审中-公开
    DIAZACARBAZOLES和使用方法

    公开(公告)号：US20150368244A1

    公开(公告)日：2015-12-24

    申请号：US14137972

    申请日：2013-12-20

    Applicant: Genentech, Inc.

    Inventor： Hazel Joan Dyke ,  Emanuela Gancia ,  Lewis J. Gazzard ,  Simon Charles Goodacre ,  Joseph P. Lyssikatos ,  Calum MacLeod ,  Karen Williams ,  Huifen Chen

    IPC: C07D471/14 ,  A61K31/496 ,  A61K45/06 ,  A61K31/519

    CPC classification number: C07D471/14 ,  A61K31/496 ,  A61K31/519 ,  A61K45/06

    Abstract: The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

    Abstract translation: 本发明涉及有用的式（I），（Ia），（Ib），（Ic），（Id），（Ie），（If），（Ig）和（Ih）的1,5-二氮杂咔唑化合物 作为激酶抑制剂，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。 本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或 治疗哺乳动物细胞或相关病理状况。

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