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    Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
    34.
    发明授权
    Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors 失效
    制备可用作蛋白激酶抑制剂的嘧啶衍生物的方法

    公开(公告)号：US08637666B2

    公开(公告)日：2014-01-28

    申请号：US13424736

    申请日：2012-03-20

    Applicant: Jean-Damien Charrier ,  Steven Durrant ,  David Kay

    Inventor： Jean-Damien Charrier ,  Steven Durrant ,  David Kay

    IPC: C07D487/12

    CPC classification number: C07D487/14

    Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclization conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).

    Abstract translation: 制备由结构式（I）表示的化合物或其药学上可接受的盐的方法，其中结构式（I）的变量如说明书和权利要求书中所述，包括以下步骤：a）使代表的化合物 通过结构式A：在合适的还原环化条件下，形成由结构式B表示的化合物：其中R10是LG1或-X1R1，-LG1是合适的离去基团; 和b）任选地，当结构式（B）的R 10是LG 1时，还包括用-X1R1替代结构式（B）的-LG1以形成由结构式（I）表示的化合物的步骤。

    Caspase inhibitor prodrugs
    39.
    发明授权
    Caspase inhibitor prodrugs 失效
    胱天蛋白酶抑制剂前药

    公开(公告)号：US08168798B2

    公开(公告)日：2012-05-01

    申请号：US12971649

    申请日：2010-12-17

    Applicant: Steven Durrant ,  Jean-Damien Charrier ,  John Studley

    Inventor： Steven Durrant ,  Jean-Damien Charrier ,  John Studley

    IPC: C07D498/14

    CPC classification number: C07D498/04

    Abstract: This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors.This invention also relates to the processes for preparing these prodrugs of caspase inhibitors.This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.

    Abstract translation: 本发明涉及包含呋喃并[3,2-d]恶唑啉-5-酮部分的胱天蛋白酶抑制剂的前体药物，其在特定条件下可转化为生物活性化合物，特别是胱天蛋白酶抑制剂。 本发明还涉及制备这些半胱天冬酶抑制剂前药的方法。 本发明还涉及包含所述前药的药物组合物及其用于治疗与炎性或退行性疾病相关的疾病的用途。

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