THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
    46.
    发明申请
    THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS 有权
    作为MEK抑制剂的三苯基吡啶衍生物

    公开(公告)号:US20130150573A1

    公开(公告)日:2013-06-13

    申请号:US13760788

    申请日:2013-02-06

    CPC classification number: C07D495/04

    Abstract: Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

    Abstract translation: 提供了通过取代的苯胺基部分在2-位上被取代的噻吩并[2,3-b]吡啶衍生物的制备方法及其中间体。 通过本方法制备的化合物可用作例如人MEK(MAPKK)酶的选择性抑制剂,因此在医学中有益,例如在治疗炎症,自身免疫,心血管,增殖(包括肿瘤) 和伤害感受条件。 本方法可以提供改进的产率,化学或立体化学纯度,中间体和最终产物的制备和/或分离的容易程度,以及更具有工业上有用的反应条件和可加工性。

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