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US09174993B2 N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals 有权
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

  • Patent Title: N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals
  • Patent Title (中): 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
  • Application No.: US14345488
    Application Date: 2012-09-18
  • Publication No.: US09174993B2
    Publication Date: 2015-11-03
  • Inventor: Marc Nazare , Nis Halland , Friedemann Schmidt , Tilo Weiss , Uwe Dietz , Armin Hofmeister
  • Applicant: SANOFI
  • Applicant Address: FR Paris
  • Assignee: SANOFI
  • Current Assignee: SANOFI
  • Current Assignee Address: FR Paris
  • Agency: Morrison & Foerster LLP
  • Priority: EP11306179 20110919
  • International Application: PCT/EP2012/068291 WO 20120918
  • International Announcement: WO2013/041502 WO 20130328
  • Main IPC: C07D487/04
  • IPC: C07D487/04
N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals
Abstract:
The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n 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.
Abstract(Chinese):

本发明涉及式（I），（R2）n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具有权利要求中所示的含义。 式（I）的化合物是调节蛋白激酶活性的有价值的药理活性化合物，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， 并且适用于治疗SGK活性不合适的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。 本发明还涉及制备式（I）化合物，其作为药物的用途以及包含它们的药物组合物的方法。

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