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    N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
    1.
    发明申请
    N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
    N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途

    公开(公告)号：US20130072493A1

    公开(公告)日：2013-03-21

    申请号：US13236027

    申请日：2011-09-19

    申请人： Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

    发明人： Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

    IPC分类号： A61K31/4985 ,  A61P19/02 ,  A61P19/04 ,  A61P9/10 ,  A61P9/00 ,  A61P43/00 ,  A61P29/00 ,  A61P35/00 ,  C07D487/04 ,  A61P3/10

    CPC分类号： A61K31/4985 ,  C07D487/04

    摘要： The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺，其中Ar，R 1，R 2和n具有如 索赔。 式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性的有价值的药理活性化合物，并且是 适合于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。 本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。