A PROCESS FOR THE PREPARATION OF PALBOCICLIB
    2.
    发明公开
    A PROCESS FOR THE PREPARATION OF PALBOCICLIB 审中-公开
    一种制备PALBOCICLIB的方法

    公开(公告)号:EP3174878A1

    公开(公告)日:2017-06-07

    申请号:EP15826397.0

    申请日:2015-07-21

    IPC分类号: C07D471/04

    摘要: The present invention relates to a process for the preparation of palbociclib utilizing a silyl-protected crotonic acid derivative to produce a silyl-protected 2-chloro-4-(cyclopentylamino)-5-(1-methyl-2-carboxy-ethen-1-yl)pyrmidine followed by intramolecular cyclization of the pyrmidine intermediate to produce 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one which is then converted to palbociclib.

    摘要翻译: 本发明涉及一种利用甲硅烷基保护的巴豆酸衍生物制备palbociclib以制备甲硅烷基保护的5-(1-甲基-3-羧基 - 丙-1-烯-1-基)-2-氯 - 哌嗪,然后将化合物哌嗪中间体分子内环化生成2-氯-8-环戊基-5-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮,然后将其转化为palbociclib。

    CRYSTALLINE FORM OF BARICITINIB
    3.
    发明公开
    CRYSTALLINE FORM OF BARICITINIB 审中-公开
    结晶形式的巴西亭

    公开(公告)号:EP3136857A1

    公开(公告)日:2017-03-08

    申请号:EP15785897.8

    申请日:2015-04-29

    IPC分类号: A01N43/42

    CPC分类号: C07D487/04 C07B2200/13

    摘要: The present invention provides a crystalline form of baricitinib characterized by an XRPD pattern substantially as depicted in FIG. 1, a process for its preparation, a pharmaceutical composition comprising it, and its use for the treatment of JAK-associated diseases.

    摘要翻译: 本发明提供了一种结晶形式的巴里替尼,其制备方法,包含其的药物组合物,以及其用于治疗JAK相关疾病的用途。